International Journal of Applied Pharmaceutics

DEVELOPMENT AND OPTIMIZATION OF THE WOUND HEALING ELECTROSPUN POLYURETHANE/COLLAGEN/PHYTOCERAMIDES NANOFIBERS USING THE BOX-BEHNKEN EXPERIMENTAL DESIGN) QUALITY BY DESIGN)

Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study aimed to develop and optimize polyurethane/collagen/phytoceramides nanofibers, a wound-healing drug delivery approach, using the electrospun technique. The objective was to enhance the effectiveness of nanofibers by optimizing the preparation process.

Methods: The box-behnken design was established to optimize the electrospinning instrument performance and, consequently, the nanofiber effectiveness. Response variables were diameter, zeta potential, and diffusion coefficient, while the experimental key factors were applied voltage, flow injection rate, and rotary collector speed of the electrospinning instrument. The optimized nanofibers were examined to ensure the validity of the optimization process.

Results: The study built prediction models for each response and employed a desirability function to suggest an optimum working level of each factor that guarantees minimum diameter, maximum zeta potential, and maximum diffusion coefficient. The desirability function suggested experimental conditions of 12.9 KV for the applied voltage, 1.3 ml/h for the injection flow rate, and a speed of 920 rpm for the rotary collector speed. The optimized formula proved satisfactory physicochemical properties regarding the nanofiber's infrared spectrum and wettability characteristics. The biomedical effectiveness of the optimized nanofibers showed increased anti-inflammatory potency up to 82.8±2.6% and a high wound closure rate of about 79%. Also, the stability study showed a nonsignificant change in response over the studied points.

Conclusion: The optimized nanofiber formula achieved the desired diameter, zeta potential, and diffusion coefficient. The results proved the Box-Behnken design approach's efficacy in enhancing the nanofiber formula's effectiveness and stability.

UNLOCKING THE POTENTIAL: ENHANCING SOLUBILITY AND BIOAVAILABILITY OF ACYCLOVIR THROUGH SOLID DISPERSION FORMULATIONS

RUBA MALKAWI, SULEIMAN AL-OLIMAT, JUMANA TAWALBEH — Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study aimed to formulate and evaluate solid dispersions of acyclovir using Polyethylene Glycol (PEG) polymers (PEG 3350, PEG 4000, and PEG 6000) in varying ratios to improve their oral bioavailability.

Methods: Solid dispersions of acyclovir with PEG 3350, PEG 4000, and PEG 6000 were prepared at different weight ratios (1:5, 1:20, and 5:1) using the solvent evaporation method. Physical mixtures were also prepared for comparison purposes. Characterization involved Differential Scanning Calorimetry (DSC) to study thermal behavior, X-ray powder Diffraction (XRPD) to assess the crystalline state, Fourier Transform Infrared Spectroscopy (FTIR) for molecular interactions, and dissolution studies using USP apparatus type 2 to evaluate drug release profiles.

Results: Among the tested formulations, the solid dispersion of acyclovir with PEG 4000 at a 20:1 ratio demonstrated the most favourable dissolution profile, with over 50% drug release within the first 10 min. DSC analysis indicated a significant reduction in the crystallinity of acyclovir within the solid dispersions, particularly with PEG 4000. XRPD confirmed the transformation of acyclovir to an amorphous state, while FTIR spectroscopy revealed molecular interactions between acyclovir and PEG, indicative of enhanced solubility. Dissolution studies further corroborated the superior performance of the 20:1 PEG 4000 formulation, which showed a remarkable increase in solubility compared to other ratios and physical mixtures. Mathematical modeling using the Weibull and Logistic models suggested controlled and predictable release kinetics for the optimized formulation.

Conclusion: Overall, this study underscores the potential of solid dispersion formulations, particularly the 20:1 ratio of PEG 4000 to acyclovir, in enhancing the oral bioavailability of poorly water-soluble drugs, such as acyclovir, offering valuable insights for pharmaceutical formulations and drug delivery systems.

FORMULATION AND EVALUATION OF ETODOLAC AND TRIAMCINOLONE ACETONIDE LOADED NANO LIPID CARRIER GELS FOR THE THERAPEUTIC MANAGEMENT OF OSTEOARTHRITIS PAIN THROUGH TOPICAL ADMINISTRATION: A COMPARATIVE STUDY

SOUVIK CHAKRABORTY, N. VISHAL GUPTA, VIKAS JAIN, BALAMURALIDHARA V. — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The present study aims to prepare carbopol-based hydrogels loaded with Etodolac (EDT), and Triamcinolone Acetonide (TCA) incorporated Nanolipid Carriers (NLCs) (EDTg and TCAg) to compare the efficacy and potency of both drugs for Osteoarthritis (OA) pain management.

Methods: EDT-NLCs and TCA-NLCs were prepared with the help of the solvent evaporation method after screening the lipids, and the NLCs were optimized. The optimized NLC formulations EDT-NLC and TCA-NLCs were examined for particle size, PDI, zeta otential, Differential Scanning Calorimetry (DSC), Powder X-ray Diffraction (PXRD), Transmission Electron Mcroscopy (TEM) and in vitro release. The prepared EDTg and TCAg have been evaluated with in vitro drug release, ex-vivo skin permeation, and in vivo pharmacokinetic and pharmacodynamic parameters.

Results: DSC and PXRD graphs showed a decrease in melting point and the amorphous form of the optimized NLC formulation. Different evaluation tests revealed that the EDT-NLCs and TCA-NLCshad particle size of 161±0.0021 nm and 167.4±0.0010 nm, PDI of 0.148±0.023 and 0.130±0.01, and zeta potential of-14 mV and-15 mV respectively, indicating their distinct nature. In vitro drug release study, ETDg showed 89.84±1.71 % release, while TCAg released 94.75±1.79 % after 24 h of application. ETDg permeated 86.5±1.68% of EDT-NLCs through the dorsal skin, compared to TCA-NLCs 76.5±1.13 %in an ex vivo skin permeation investigation. A pharmacokinetic study identified 76.3±1.98 % of EDT-NLCs and 63.25±2.003 of TCA-NLCs in drug plasma. Pharmacodynamic characteristics like X-ray analysis, Immuno Histochemistry (IHC), and histopathology indicated that EDTg and TCAg managed OA pain. All evaluation tests carried out in this research showed that formulated hydrogels could manage OA.

Conclusion: The results suggested in this research prove EDTg to have a higher potentiality than TCAg for the management of OA pain

COMBINING LIQUID CHROMATOGRAPHY WITH TANDEM MASS SPECTROMETRY (LC-MS/MS) TECHNIQUE, SPECTROPHOTOMETERVALIDATION AND AN IN SILICO STUDY OF 96% ETHANOL EXTRACT OF SPIRULINA PLATENSIS

TIWUK SUSANTININGSIH, FADILAH FADILAH, ANI RETNO PRIJANTI, NOVI SILVIA HARDIANY — Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study was to analyze the component sofa 96% ethanol extract of Spirulina platensis by the LC-MS/MS technique, then validate them with the spectrophotometer technique using the C-phycocyanin standard and an in silico study approach as an antioxidant property of S. platensis against inflammatory.

Methods: Chromatographic resolution was attained with a Phenominex C18 (50 mm×2.6 mm, 3 µm) stationary column technique, validation using C-phycocyanin standard using the spectrophotometer technique, and an in silico study of c-phycocyanin using molecular docking analysis.

Results: Tentative active compounds such as flavonoid (Maltol and Morin), peptide (Cyclo Pro-Ala, Cyclo Pro-Pro, and Thymine), and phenol (m-Aminophenol, N-Methyltyramine, and Tyramine) have been identified from a 96% ethanol extract of S. platensis by LCMS/MS analysis. The concentration of c-phycocyanin in the 96% ethanol extract of S. platensis is 229, 2µg/ml. According to our in silico study, c-phycocyanin demonstrates potential as an anti-inflammatory agent.

Conclusion: The LC-MS/MS technique can detect flavonoid, peptide, and phenolic components in the 96% ethanol extract of S. platensis. A spectrophotometer can identify the validation equation of c-phycocyanin in a 96% ethanol extract of S. platensis. Based on our in silico study, c-phycocyanin demonstrate the capability to prevent inflammatory activity.

ANALYTICAL QUANTIFICATION OF BOSUTINIB IN NANOCARRIER USING UV AND HPLC: METHOD DEVELOPMENT AND VALIDATION

RISHABH AGADE, UJBAN HUSSAIN, SAGAR TRIVEDI, VEENA BELGAMWAR — Sat, 07 Sep 2024 00:00:00 +0530

Objective: Bosutinib, a potent tyrosine kinase inhibitor, holds significant promise in cancer therapy, particularly in Breast Cancer treatment. This study focuses on the analytical quantification of Bosutinib in Nanocarriers (BNCs) essential for quantification in terms of targeted delivery.

Methods: A comprehensive method development and validation process was undertaken utilizing UV-visible spectroscopy and High-Performance Liquid Chromatography (HPLC). Preformulation studies confirmed the purity and physicochemical properties of bosutinib. UV-visible spectroscopy established a calibration curve for bosutinib and BNCs, with precision, accuracy, Limits of Detection (LOD), and Limits of Quantification (LOQ) determined. HPLC analysis further validated bosutinib quantification, ensuring the robustness and reliability of the analytical method.

Results: Bosutinib and BNCs were evaluated using UV-visible spectroscopy, revealing λ max at 263 nm and 277 nm, respectively, showing a strong correlation with the regression coefficient (R²) being 0.9969 and 0.9994, respectively. The precision (intra-day and inter-day) data shows strong reproducibility with a Percentage Relative Standard Deviation (%RSD) of less than 1.5%. Completely distinguished sharp peaks of bosutinib and BNCs were developed using HPLC under ambient settings; 3.974±0.006 and 3.083±0.004 was the Resolution Time (Rt) at which bosutinib and BNCs were discovered, respectively. The Theoretical Plate (TP) values of 5179±93 and 2598±85 and the Tailing Factor (TF) of1.00±0.002 and 1.10±0.004 were both within the predetermined bounds.

Conclusion: The developed UV and HPLC methods offer accurate and reliable quantification of bosutinib in a nanocarrier, essential for optimizing drug delivery strategies and therapeutic outcomes in cancer treatment. This analytical approach contributes to advancing pharmaceutical research in precision medicine and targeted drug delivery systems.

DEVELOPMENT OF NANOSPONGES-BASED TOPICAL FORMULATION FOR THE EFFECTIVE DELIVERY OF SELECTED ANTIFUNGAL DRUG

RUDROJU ANUSHA, MOTHILAL M. — Sat, 07 Sep 2024 00:00:00 +0530

Objective: To increase luliconazole's therapeutic impact, distribution, and preservation, this project is aimed to prepare cyclodextrin-based nanosponge gel and test its topical skin administration.

Methods: The convection heating method produced cyclodextrin-diphenylcarbonate nanosponges, which later loaded with luliconazole by freeze-drying. Response Surface Methodology (RSM) was used to examine the association between procedure parameters and quality variables. Pilot study findings were analyzed using Analysis of variance. Key technique factors affect quality metrics in contour, RSM, and perturbation graphs.

Results: The mean medication payload was 42.19±1.45 mg of luliconazole/g of lyophilized powder. The remarkable encapsulation efficiency of luliconazole (90.12±0.92%) supports an inclusion complex. Laser light scattering evaluation of luliconazole-loaded-nanosponges shows an unimodal and narrow particle size distribution of 60-73 nm. Drug encapsulation does not change a typical nanosponge's spherical form, according to microscopic investigations. Physico-chemical characterized verified the nanosponge-luliconazole inclusion complex. The complex release is faster than pure medication in vitro. Pure luliconazole dissolves 12% in 12 h, whereas nanosponge encapsulated medicine is absorbed faster and better. After 12 h, nanosponge formulations released 93-95% luliconazole. A model carbopol gel formulation with nanosponge formulations examined skin permeability, antifungal effectiveness, and stability. In 12 h skin permeation trials, nanosponge-encapsulated luliconazole leaked slowly across rat skin.

Conclusion: The slow drug release, greater skin penetration, and superior storage stability of the gel formulation based on cyclodextrin nanosponges of luliconazole imply that it has great potential as a topical delivery system.

INTEGRATIVE QSAR ANALYSIS OF OXADIAZOLE DERIVATIVES: RESOLVING MOLECULAR DETERMINANTS FOR ANTI-TUBERCULAR ACTIVITY AND RATIONAL DRUG DESIGN

Sat, 07 Sep 2024 00:00:00 +0530

Objective: In this study, we conducted a comprehensive Quantitative Structure-Activity Relationship (QSAR) analysis of an oxadiazole derivative exhibiting potent anti-tubercular activity by inhibiting synthesis.

Methods: Our investigation employed both 3D atom-based and field-based Comparative Molecular Field Analysis/Comparative Molecular Similarity Indices Analysis (CoMFA/CoMSIA) techniques, along with auto QSAR analysis using a 2D canvas. The CoMFA and CoMSIA methodologies allowed for the exploration of molecular interactions and structural features contributing to the molecule's inhibitory potency. Utilizing these 3D approaches, we delineated the steric, electrostatic, hydrophobic, and hydrogen bond acceptor/donor fields influencing the molecular activity. Furthermore, the auto QSAR analysis provided valuable insights into the 2D structural descriptors governing the anti-TB efficacy of the oxadiazole compound.

Results: Our findings not only elucidate the molecular determinants essential for inhibitory activity but also provide a robust predictive model for assessing the anti-TB activity of structurally related compounds. Both 3D QSAR and 2D QSAR models were designed and generated. These models were found to be useful in predicting the anti-TB activity of oxadiazole derivatives. The best model for accurately predicting activity was found to have a Q² value of 0.9558 and an R² value of 0.979.

Conclusion: This integrative QSAR study contributes to the rational design and optimization of novel oxadiazole-based therapeutics against tuberculosis, addressing the urgent need for effective treatment strategies against this global health threat.

FORMULATION AND EVALUATION OF LICORICE OIL-BASED EMULGEL FOR THE TREATMENT OF PSORIASIS

PRIYANKA JUREL, SHIV BAHADUR, MEENAKSHI BAJPAI — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The aim of the present research work was to develop and evaluate the topical emulgel incorporated with licorice oil for the effective management of psoriasis.

Methods: The present study involves the preparation and optimization of licorice oil-based emulsion using tween 80, span 20, propylene glycol and was loaded in gel base (carbopol 940 was used as gelling agent). The prepared emulgel were evaluated for various parameters such as particle size, zeta potential, entrapment efficiency, spreadibility, pH, viscosity, Fourier-Transform Infrared Spectroscopy (FTIR), in vitro release studies and in vitro cell line study.

Results: The optimized formulation was found to have droplet size of 54.50 nm,-14.1 V zeta potential, entrapment efficiency of 59.53±8.42 % and spreadibility of 2.901±0.12 mm. The pH and viscosity of optimized licorice oil-based emulgel was found to be 6.0±0.467 and 93,500±832 cps, respectively. Cumulative in vitro release was found to be 95.15±0.26 % has shown by the optimized formulation for 10 h. In (3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) MTT cytotoxicity study indicated non-toxic potential properties of licorice oil and its emulgel at lower level and caused moderate toxicity at higher level against Human Epidermal Keratinocytes (HaCaT) cell lines after the incubation period of 24 h respectively.

Conclusion: This study showed that the emulgel formulation has the potential to significantly enhance the efficacy of licorice oil in the treatment of psoriasis. These findings provide exciting new possibilities for improving psoriasis treatment and explores importance of continued research in this area.

INVESTIGATING MULTITARGET POTENTIAL OF MUCUNA PRURIENS AGAINST PARKINSON'S DISEASE: INSIGHTS FROM MOLECULAR DOCKING, MMGBSA, PHARMACOPHORE MODELLING, MD SIMULATIONS AND ADMET ANALYSIS

Sat, 07 Sep 2024 00:00:00 +0530

Objective: Mucuna pruriens (Velvet beans) is a leguminous plant recognised in Vedic therapy as an anti-Parkinsonism agent. The plant is known as the natural reservoir for levodopa. The study aims to evaluate the multitarget inhibitory potency of active constituents present in Mucuna pruriens using in silico tools.

Methods: The phytoconstituents present in Mucuna pruriens were retrieved from the IMPPAT database. The physicochemical and toxicity parameters of phytoconstituents were evaluated using Qikprop and ProTox-3. The inhibitory potential of phytoconstituents on the enzymes Monoamine Oxidase-B (MAO-B), Acetylcholinesterase (AChE), and Catechol-O-Methyltransferase (COMT) was evaluated using in silico techniques, including molecular docking, pharmacophore modelling, and molecular dynamics simulations, conducted with Schrödinger software programs.

Results: The active constituents comply with Lipinski’s rule for drug-likeness. Further, the molecular docking studies revealed the phytoconstituent luteolin and acacetin showed promising multitargeted inhibitory properties. Especially luteolin (-11.504 kcal/mol) and acacetin (-10.620 kcal/mol) have obtained excellent docking scores with MAO-B, whereas the known drug levodopa showed a docking score of-8.501 kcal/mol. The pharmacophore modelling revealed that donor, acceptor, and aromatic features present in luteolin and acacetin are the essential pharmacophoric features accountable for biological activity. The simulation study generated the stability of the protein-ligand complex and found that luteolin showed a stable complex with MAO-B.

Conclusion: Based on these findings, the result of the current study can be used to develop a novel luteolin-based drug for treating Parkinson’s disease with preferred structural modification. However, additional and more comprehensive research is required on this compound.

THE DEVELOPMENT OF METHOD FOR ACTIVATING PHARMACEUTICAL SUBSTANCES WITH SUBSEQUENT IN SITU STUDY OF MODIFIED POWDER PROPERTIES

Sat, 07 Sep 2024 00:00:00 +0530

Objective: The aim of this work is to develop a method of activation of pharmaceutical substances by means of a mechanical load on the powder of the substance with the subsequent evaluation on site of the modified preparation. A complex of analytical methods and biotesting were used to characterize the solid-state phase transformation product.

Methods: The object of study was powder of the antiepileptic substance Lacosamide (Lcs); Mechanical Activation (MA) of Active Pharmaceutical Ingredient (API) was carried out using the Stegler LM-250 rotary knife mill; Fourier-Transform Infra-Red (FT-IR) spectroscopy in the range of 4000-400 cm^-1 was used to analyses the band shift in the spectrum; Dynamic Laser Scattering (DLS) has been used to detect groups of particles ranging in size from 0 to 1000 nm; an innovative method of Two-Dimensional Diffuse Light Scattering (2D-DLS) was used to detect differences in the speckle structure of powder samples before and after modification; Scanning Electron Microscopy (SEM) was used to evaluate particle morphology; X-Ray Fluorescence analysis (XRF) was used to determine the elemental composition of the samples; polarimetry was used to determine the optical activity and Spirotox biotesting has been used to evaluate the biological activity.

Results: SEM images of the sample after activation represent a glassy, structurally amorphous state in contrast to the native state. Chemometric processing of FT-IR spectra allowed us to identify the regions of the samples at different activation times on the 2D-diagram of Principal Components Analysis (PCA). According to the XRF data, the elements Fe, Cu, and Zn are predominant in the Lcs-activated sample. The 2D-DLS method revealed differences in speckle structure between samples before and after mechanical activation. The same optical activity of the solutions of the studied samples with preservation of the chiral center was revealed. The Spirotox method showed a 1.6-fold (P≤0.05) increase in biological activity of the activated Lcs sample based on the calculated values of activation energy (^bsE_a) of the process of cellular transitions to the immobilized state.

Conclusion: The developed method of activation of pharmaceutical substances includes a full cycle of 90 min mechanical load chemistry duration with the description of technical equipment and conditions. The results of this study can be used in the pharmaceutical industry to produce preparations with improved physical-chemical and biopharmaceutical properties.

FORMULATION AND IN VIVO EVALUATION OF NANOEMULGEL-CONTAINING COCOA POD HUSK (THEOBROMA CACAO L.) EXTRACT AS TOPICAL ORAL PREPARATION

Sat, 07 Sep 2024 00:00:00 +0530

Objective: Cocoa pod husk (Theobroma cacao L.) extract was applied to enhance bioavailability and drug effects due to antibacterial, antioxidant and anti-inflamation agents. Recent years have seen significant development of nanomedicine in non-invasive therapy of oral infection. The aim of this study was to develop the formula of nanoemulgel of Cocoa Pod Husk (CPH) extract for topical oral therapy compared its stability and evaluation in gingivitis rats with gels preparations on different gelling agents. Methods: The topical oral preparation were made in 4 formulations: F1 (CPH gel with gelling agent Sodium Carboxy Methyl Cellulose (Na-CMC) 3%); F2 (CPH gel with gelling agent Carbomer 1%); F3 (CPH nanoemulgel with gelling agent Na-CMC 3%); and F4 (CPH nanoemulgel with gelling agent Carbomer 1%. The physical characterization test of preparations were evaluated the pH, homogeneity, viscosity, spreadability and adhesion test. In vivo evaluation of gingivitis rats were observed using histological analysis of the fibroblast number and gingival collagen density in experimental Wistar rats by Hematoxylin eosin and Masson trichrome staining.Results: Four formulation (F1-F4) showed good stability in pH, viscosity, spreadability and adhesivity (p<0.05). The observation for 7 d after gel application to gingivitis rats, showed that the number of fibroblast and collagen density increasing in the treatment group compared to the control group (p<0.001). In the LSD test, F3 and F4 indicated the highest increase, however no significantly different (p>0.05).Conclusion: Nanoemulgel with Na-CMC as gelling agent potential to be used as an effective carrier for the active ingredients of CPH extract.

MOLECULAR TARGETS AS POTENTIAL PI3Kα INHIBITORS AGAINST AGGRESSIVE METASTATIC DUCTAL AND LOBULAR CARCINOMA

Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study aimed to identify active compounds among existing molecules by drug repositioning as potential hits of Phosphoinositide 3-Kinase (PI3Kα) inhibitors. FDA-approved ligands were docked using structure-based in silico screening, and the top ten molecules based on docking score were studied for their in silico pharmacokinetic and ligand-receptor interactions.

Methods: FDA-approved ligands were docked with the protein PI3Kα enzyme (PDP ID: 4JPS) and were checked for their molecular interactions and docking scores using the GLIDE program of Schrödinger software. The top 10 ligands were subjected to ADMET and MMGBSA studies to predict pharmacokinetic properties and binding affinity. The best two molecules and the standard alpelisib were subjected to Molecular dynamics with 100 nsec simulation time to deduce interaction at the atomic level.

Results: Two molecules, ZINC000003794794 (Mitoxantrone) and ZINC000004098633 (Polydatin), were found to be promising based on docking score, ligand interaction diagram, and MMGBSA scores of-13.084 and-11.364 and-75.38 and-58.88 respectively and were in a comparable range to the standard alpelisib. These two molecules were then subjected to Induced Fit Docking (IFD) and molecular dynamics to better understand protein stability and inhibitor activity in physiological conditions. The IFD values of these molecules were very close to the standard, and the residues of the best poses coincided with the desired residues, such as V851, S854, and Q859, seen in the alpelisib.

Conclusion: However, further in vitro and in vivo screening is needed to confirm the PI3Kα inhibitory activity of these ligands, which could serve as promising lead molecules in treating TNBC with fewer side effects compared to existing drugs.

AUTHENTICATION OF GRAPE SEED FACE OIL USING FTIR SPECTROSCOPY COMBINED WITH CHEMOMETRICS TECHNIQUES

Sat, 07 Sep 2024 00:00:00 +0530

Objective: This research aims to authenticate grape seed oil products using FTIR spectroscopy combined with chemometric methods.

Methods: In the initial stage, exploratory data analysis was carried out by applying the main components with the Principal Component Analysis (PCA) model. Second derivative spectra resulting from preprocessing of the original spectra are used to create multivariate Principal Component Regression (PCR) and Partial Least Squares (PLS) calibration models. The second derivative spectra of Grape Seed Oil (GO), Olive Oil (OO), and the binary mixture GO+OO are utilized to generate a sparse partial least squares-discriminant analysis (SPLS-DA) model.

Results: The PCA model was successfully obtained with visualization that depicted a total of 93.8% in the first and second dimensions. Multivariate calibration produced the best model in PLS with second derivative spectra for both GO and OO. PLS model for GO resulted the value of R_cal², R_CV², R_val², RMSEC, RMSECV, and RMSEP of 0.998, 0.992, 0.982, 0.700, 1.557, and 2.331, respectively. The SPLS-DA model was successfully built and discriminated with AUC-ROC values of 1.000, 1.000, and 0.994 for GO, OO, and GO+OO, respectively.

Conclusion: Authentication of grape seed face oil can be undertaken using FTIR spectroscopic methods and chemometric techniques, which can produce high sensitivity and specificity values.

HESPERETIN DERIVATIVES AS PPAR γ AGONIST: A PHARMACOPHORE APPROACH

RAMANATHAN MUTHIAH, VIJAYALAKSHMI CHINNIAH, MAIDA ENGELS. S. E. — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The study focuses on enhancing the pharmacological activity of hesperetin, a bioflavonoid, to develop novel derivatives with improved efficacy and reduced side effects compared to existing Thiazolidinediones (TZDs) as PPAR g agonist.

Methods: The Methodology involves various computational approaches, including pharmacophore modelling, molecular docking, Molecular Mechanics with Generalised Born and Surface Area Solvation (MMGBSA), and molecular dynamics simulations. Pharmacophore modelling identifies essential binding features validated by Quantitative Structure-Activity Relationship (QSAR) models. Database screening and docking confirm lead compounds' binding affinity, with MMGBSA aiding lead optimization. Toxicological assessment ensures drug likeness and bioavailability. Molecular dynamics simulations explore protein-ligand complex stability and dynamics, revealing insights into their interactions.

Results: The results indicate MOL-297 exhibits improved properties over hesperetin, including ADME properties, solubility, blood-brain barrier permeability, docking score, and binding energy. Molecular dynamics simulations confirm Mol-297-PPAR γ complex stability, with favourable ligand-amino acid interactions.

Conclusion: The developed new molecule MOL 297, is a novel Peroxisome Proliferator-Activated Receptor (PPAR) gamma agonists with enhanced pharmacological properties, warranting further experimental validation and drug development.

QUANTITATIVE DETERMINATION OF METHYL-4-CHLOROBUTYRATE, A POTENTIAL GENOTOXIC IMPURITY, CONTENT IN MOXIFLOXACIN HCL BY GC-EI-MS

K. APARNA, K. VIJAYA RACHEL, K. M. V. NARAYANA RAO — Sat, 07 Sep 2024 00:00:00 +0530

Objective: Methyl-4-Chlorobutyrate (M4CB), a genotoxic impurity, was identified in the active pharmacological components of the fourth-generation fluoroquinolone, moxifloxacin (MXFN). There has not yet been a report on the analysis of the M4CB impurity content in the MXFN molecule. Consequently, a Gas Chromatography-Electron Ionization-Mass Spectrometry (GC-EI-MS) method was established that has the ability to identify and measure M4CB impurity content at ppm level.

Methods: The column exploited in M4CB impurity assay was a Dura Bond 624 (DB-624) type stationary column. Temperatures of 220 °C and 280 °C were consistently maintained at the injection and detection sites, respectively. The helium, as carrier gas, in split mode with ratio of 1:7 was used. The column's flow rate remained steady around 2.0 ml/min. The mass spectrometer was operated in Single Ion Monitoring (SIM) mode at m/z = 74.

Results: The impurity M4CB is generated during the manufacturing process of cyclopropanamine, which is an intermediary molecule in the manufacturing process of MXFN. This new GC-EI-MS approach can measure the M4CB at 0.9452 ppm in MXFN samples with a 500 mg/ml concentration following International Council for Harmonisation (ICH) standards. Very low quantification limits (0.9452 ppm), high linearity (range=0.945 ppm to 5.625 ppm; regression coefficient= 0.9999), and a reasonable recovery range (94.60-94.63%) were all provided by this new validated GC-EI-MS approach. Three batches were analysed for M4CB content by new GC-EI-MS approach and found that none of the batches contained M4CB impurity.

Conclusion: The GC-EI-MS approach has excellent applicability in the quality assurance testing of MXFN for M4CB content since it was adequate in terms of linearity, precision, sensitivity, accuracy, specificity, and robustness.

DEVELOPMENT OF GUGGULSTERONE-LOADED PHYTOSOMES: A QUALITY BY DESIGN-BASED CHARACTERIZATION AND OPTIMIZATION STUDIES

JAMAL BASHA DUDEKULA, JEBASTIN KOILPILLAI, DAMODHARAN NARAYANASAMY — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The primary objective of this study was to enhance drug delivery efficiency through the design and optimization of guggulsterone-pyrosomes, employing a 3-factor, 3-level box-behnken design.

Methods: The methodology involved a solvent evaporation technique utilizing guggulsterone and soy lecithin, with a systematic variation and optimization of critical factors such as soy lecithin and guggulsterone concentration, alongside temperature adjustments to refine the phytosome formulations. The characterizations of these formulations were extensive, with a particular emphasis on key quality attributes, notably percentage entrapment efficacy and drug release.

Results: The optimized guggulsterone-pyrosomes demonstrated impressive outcomes, showcasing a remarkable entrapment efficiency of 92.64% and a noteworthy drug release rate of 91.69% at 24 h. These formulations displayed heightened viability in selected cell lines, exhibiting cellular toxic c concentrations ranging from 253.39 to 330.44 µg/ml. Moreover, they exhibited stability under stressed conditions from a physicochemical perspective. The particle size was measured at 137.8 nm, with a zeta potential of-25.3 mV.

Conclusion: Significantly, the extended drug release from guggulsterone-pyrosomes adhered to first-order kinetics with Fickian diffusion. In summary, this study underscores the efficacy of the box-behnken design in crafting optimized guggulsterone-pyrosomes, showcasing their potential as promising drug delivery carriers. The enhanced drug delivery platform exhibits significant promise in amplifying antihyperlipidemic effects, attributed to the improved performance and stability of these innovative phytosomes

SYNTHESIS, CHARACTERIZATION AND IN VITRO EVALUATION OF VATERITE MICROPARTICLES

DEENA JOSE, D. KUMUDHA — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The aim of this research is to synthesize submicron-sized calcium carbonate vaterite particles of elliptical shape with different reaction durations. We also aim to assess their antioxidant and anti-inflammatory properties, which may be beneficial for treating diseases such as asthma and rheumatoid arthritis.

Methods: Calcium carbonate vaterite particles were prepared using the co-precipitation method with varying reaction times, characterized by Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), Fourier Transformation Infrared Spectroscopy (FTIR), and Poly-Dispersity Index, with antioxidant activity assessed by the 2,2-Diphenyl-1-Picrylhydrazyl (DPPH) method and anti-inflammatory activity by the protein denaturation method.

Results: SEM and TEM analysis revealed that the synthesized vaterite particles had an elliptical shape with nano-crystalline particles of around 50 nm size. FTIR verified the production of vaterite particles. Research on antioxidants and anti-inflammatory agents revealed that the crystalline particles exhibited DPPH scavenging action, with an IC₅₀ of 12.6 µg/ml, and a noteworthy reduction in protein denaturation in the albumin protein denaturation test, with an IC₅₀ of 222.49 µg/ml, in comparison to the reference value.

Conclusion: The results highlight the potential of elliptical vaterite submicron micro-particles as versatile platforms with anti-inflammatory and antioxidant properties, paving the way for future advancements in drug delivery systems, food additives, and natural supplements by efficiently encapsulating drugs and proteins.

DESIGNING, DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING HBS SYSTEM OF METFORMIN: IN VITRO IN VIVO STUDIES

RADHESHYAM SAMANTA, GAURAV TIWARI, NAVEEN GUPTA, DHARMENDRA SINGH RAJPUT — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The main objective of this study is to formulate, characterized and evaluate the Medium Molecular Mass Chitosan (MMMCH) – Xanthan Gum (XG) based polymeric carrier mediate of non-effervescent floating hydrodynamically Balanced System (HBS) capsule of metformin for developed stomach specific sustain drug delivery over a prolong periods of time.

Methods: Different capsules of metformin were formulated by physical blending of metformin with polymeric mixture to encapsulate in 000 a single unit hard gelatine capsule, than evaluate the different parameters like micromeritics properties, weight uniformity, drug content uniformity, in vitro drug release with their kinetics model, DSC and FTIR study, in vitro in vivo floating characteristic.

Results: After evaluating the characteristic properties, it was clearly indicated that excellent value ranges, coefficient of weight variation in between 1.39-2.06%, content uniformity of drug in between 98.23-100.05%, in vitro drug release in between 60–80 % after 12h that can follow Korsmeyer-Peppas model to release the drug no-fiction diffusion method. FTIR and DSC study exhibit no much more incompatibility between drug and polymer and formation of electrolyte complex help to sustaining release over a prolong periods of time. In vitro and in vivo floatation study, it was clearly indicated that all formulation (especially MC4) floated in gastric content more than 12h without any floating lag time and excellent in vivo buoyancy by the help of x ray images of animal model by replacing the drug with barium sulphate.

Conclusion: So this type of formulation showing great gastroretentive floating drug delivery system in future with another drugs for a prolong periods of time.

FORMULATION, CHARACTERIZATION, AND TYROSINASE INHIBITORY ASSAYS OF NIACINAMIDE-LOADED NANOPARTICLE GEL AS A SKIN WHITENING AGENT

RISA AHDYANI, NOR LATIFAH, HAYATUS SA’ADAH, ERLINA FATMASARI, IRFAN ZAMZANI — Sat, 07 Sep 2024 00:00:00 +0530

Objective: This research aims to formulate a nanoparticle gel of Niacinamide (N) using Chitosan (C) and Sodium Alginate (SA) and determine its tyrosinase inhibitory activity as a skin whitening.

Methods: N nanoparticle was carried out using C (0.01%), SA (0.1%), and Calcium Chloride (CC 0.25 %). N was incorporated into the nanoparticle system by different concentrations in each Formula (F): F1(2.5 %), F2 (5%), F3 (7.5%), and F4 (10%). Each formula was characterized for particle size, Polydispersity Index (PI), and Zeta potential by Zetasizer, entrapment efficiency using Spectrophotometer Uv-Vis, and molecular structure using Fourrier Transform Infrared (FTIR). Then, Hydroxy Propyl Methyl Cellulose (HPMC) was incorporated to form a nanoparticle gel of N. N-loaded nanoparticle gel was determined tyrosinase inhibitory using L-tyrosine to obtain Inhibitory Concentration of 50 (IC₅₀) value. Furthermore, data was analyzed using one-way ANOVA (p-value<0.05).

Results: The particle size, PI, Zeta potential, and entrapment efficiency obtained for all formulations were found to be F1 (217±7.21 nm, 0.49±0.0521,+8.24±1.75 mV, and 61.22±2.88 %); F2 (225±11.37 nm, 0.51±0.0246,+9.12± 1.97 mV, and 64.01±4.12%); F3 (289±15.26 nm, 0.26±0.0152,+10.55± 1.56 mV, and 68.71±3.86 %); F4 (428±9.44 nm, 0.38±0.0347, 12.33±1.80 mV, and 72.59±3.01%) respectively. The result of FTIR spectra indicated N-loaded in the nanoparticles system. Tyrosinase inhibitory activity of N-loaded gel nanoparticles obtained IC₅₀ 99.9775, 73.5605, 52.7187, and 42.3145 μg/ml, respectively.

Conclusion: N-loaded nanoparticle gel was successfully prepared and could be a promising candidate for skin whitening agent.

VALIDATED REVERSED-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD FOR THE ESTIMATION OF TETRABENAZINE IN SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEMS

Sat, 07 Sep 2024 00:00:00 +0530

Objective: Self-Nano-Emulsifying Drug Delivery System (SNEDDS) of tetrabenazine (TBZ) was analysed using reverse-phase high-performance liquid chromatography.

Methods: Optimized chromatographic condition was consisted of Acetonitrile (ACN) and 0.1% v/v formic acid in the ratio of 90:10 as a mobile phase in isocratic mode at 25±1 °C. In this C-18 (250 mm×4.6 mm, 5 µm) column was used and absorbance was recorded at 283 nm.

Results: The compound was eluted at a flow rate of 1.0 ml/min and retention time (RT) was observed as 4.34±0.03 min. TBZ showed linearity over 2-10 µg/ml conc. and the value of regression was obtained as 0.9992. The developed method was found precise due to Percentage Relative Standard Deviation (%RSD) was less than 2 %. On the other hand, 0.31 and 0.96 were investigated value for Limit of Detection (LOD) and Limit of Quantification (LOQ), respectively.

Conclusion: The method adopted was found to be robust and can be apply for the determination of drug in different oil, surfactants and co-surfactants for the calculation of drug loading of pharmaceutical product formulation.

NANOCREAM FOUNDATION FORMULATION LOADED WITH ETHYL ACETATE FRACTION FROM MELASTOMA MALABATHRICUM l.

LIZA PRATIWI, RAFIKA SARI, PRATIWI APRIDAMAYANTI — Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study aimed to create a nanocream formula of the ethyl acetate fraction of Melastoma malabathricum using Design-Expert software. The objective was to obtain an optimal nanocream formula, analyze its characteristics, test its real-time stability, and measure its free radical scavenging ability using the DPPH method.

Methods: The study began by manufacturing 70% ethanol extract from Melastoma malabathricum leaves and fractionating it with ethyl acetate to obtain the desired fraction. The fraction was then used to create a nanocream using cetyl alcohol, liquid paraffin, and propylene glycol in a ratio of 5:5:15. The optimal formula was tested for real-time stability and antioxidant effectiveness using the DPPH method.

Results: Based on the results of the study, the optimal formula of the nanocream foundation preparation of the ethyl acetate fraction of Melastoma malabathricum was a combination of cetyl alcohol, liquid paraffin and propylene glycol in a ratio of 5:5:15. The results showed that the optimal nanocream formula had a pH value of 6.1±0.36, a spreadability of 6.57 cm ±0.06, and an adhesion of 22.20 minute±0.03. The particle size was determined to be 47 nm±0.78. The optimal formula also showed practical free radical scavenging ability, with an IC50 value of 556,29±0,155. The nanocream was stable for 28 d of real-time testing, and the honey extract remained stable during freeze-thaw.

Conclusion: In conclusion, using the design-expert software, the study successfully created a nanocream formula from the ethyl acetate fraction of Melastoma malabathricum (NFMM). The resulting nanocream had physical characteristics that met the requirements for pH, spreadability, adhesion, and particle size. It was stable for 28 d of real-time testing and showed antioxidant activity when tested with the DPPH method.

MOLECULAR DOCKING OF BIFLAVONOIDS FROM GENUS ARAUCARIA AS DENV NS5 RNA-DEPENDENT RNA POLYMERASE INHIBITOR USING YASARA AND PLANTS PROGRAMS

Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study aimed to screen 23 biflavonoids (23 BF) from the Araucaria genus to identify the most promising compound for anti-dengue fever antivirus treatment using in silico techniques with yet another scientific artificial reality application (YASARA) Structure and the Protein-Ligand ANT System (PLANTS) programs.

Methods: Predictions of conserved amino acids and potential pockets of the virus dengue NS5 RNA-dependent RNA polymerase (DENV NS5 RdRp) (PDB ID: 5K5M) were examined, while co-crystal ligands were prepared along with 23 biflavonoids. Molecular docking of ligands on the target protein was carried out using the YASARA Structure and PLANTS programs. The interactions were visualized with LigPlot+, Pymol, and Discovery Studio 2021 Client in. pdb format.

Results: The results showed that based on the molecular docking of 23 biflavonoids from the Araucaria genus against the selected DENV NS5 RdRp, the top nine compounds with great potential as antiviral drug candidates were identified. Among these compounds, 7,4’,7’’-tri-O-methylagathisflavone (BF3) was distinct as the best choice based on the analysis conducted using the YASARA Structure and PLANTS programs. Other compounds, including 7,4',4'''-tri-O-methylamentoflavone (BF10), 4',4'''-di-O-methylamentoflavone (BF11), 7,4',7'',4'''-tetra-O-methylamentoflavone (BF12), 7''-O-methylamentoflavone (BF13), and 7,7''-di-O-methylamentoflavone (BF14), were selected through the YASARA Structure program, while 7,4',7'',4'''-tetra-O-methylagathisflavone (BF8) and 7''-O-methylrobustaflavone (BF23) were selected from the PLANTS program. All compounds had lower free energy (∆G), dissociation constant (Kd), and docking scores compared to the reference ligand, balapiravir. Hydrogen and hydrophobic bonds were formed with the protein through conserved amino acid residues, the N-pocket, and the catalytic Gly-Asp-Asp (GDD) site.

Conclusion: The algorithm differences between the YASARA Structure and PLANTS programs led to the selection of the best compound 7,4',7''-tri-O-methylagathisflavone (BF3) as a candidate antiviral drug for dengue hemorrhagic fever.

BIO-ANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF FINASTERIDE, TADALAFIL, AND ITS APPLICATION TO PHARMACOKINETIC STUDIES IN RAT PLASMA BY USING LC-MS/MS

YESUPADAMU RAYINUTHALA, DAVID RAJU MEDEPALLI, A. LAKSHMANARAO — Sat, 07 Sep 2024 00:00:00 +0530

Objective: An easy, quick, precise, active and reproducible LC-MS/MS (Liquid Chromatography Tandem Mass Spectrometry) technique was developed for the bio-analytical method of Finasteride and Tadalafil using Avanafil as internal standard (IS).

Methods: This article summarizes the recent progress on bioanalytical liquid Chromatography Tandem Mass Spectrometry (LC-MS/MS) methods using waters Symmetry C₁₈ column (150x4.6 mm, 3.5µ) column and mobile phase of 0.1% Perchloric acid and Acetonitrile (ACN) in 60:40.

Results: The calibration curve was linear in the range of 12.5-100 ng/ml for Finasteride and 12.5-100 ng/ml Tadalafil. The recovery results of Accuracy and Precision of Finasteride and Tadalafil were 95.10, 96.85, 98.76, 98.81% and 95.77, 97.46, 97.99, 97.01% at different QC (Quality Control) concentration levels. Matrix effect results were within the acceptable limit. An electro-spray ionization source was used to study of Finasteride and Tadalafil at m/z 373.5497→142.0085, m/z 390.4047→128.1138 for Finasteride and Tadalafil, m/z 484.9516→104.5326 for Avanafil were ion pairs of mass analysis.

Conclusion: The application denotes all the parameters of system suitability, specificity, linearity and accuracy are in good agreement with USFDA (United States of Food and Drug Administration) guidelines and applied effectively for the investigation of pharmacokinetic studies in rat.

COMPUTATIONAL ASSESSMENT OF UNDARIA PINNATIFIDA AND MORINGA OLEIFERA COMPOUNDS AS ANTI-OBESITY AGENTS

Sat, 07 Sep 2024 00:00:00 +0530

Objective: The objective of this topic is to discuss the potential of using bioactive substances of Undaria Pinnatifida Ethanolic Extract of (UPEE) and Moringa Oleifera Methanolic Extract of (MOME) extracts as pharmacological agents and inhibitors of Peroxisome Proliferator-Activated Receptor gamma (PPAR-γ), Fat Mass and Obesity-Associated (FTO), Resistin and leptin to counter obesity.

Methods: The study uses Gas Chromatography-Mass Spectrometry (GC-MS) and Fourier-Transform InfraRed (FTIR) Spectroscopy techniques to identify the bioactive components of these extracts and evaluates their efficacy through in silico assessments and molecular docking analysis.

Results: Analysis of docking results revealed that ligand interaction with FTO (ID: 3LFM) docking complex showed good binding affinity, binding oreintation, pharmocological properties. Hence, the best ligands were proposed as the best antagonist to block PPAR-γ, FTO, Resistin and leptin, which plays major role in the drug devolopment pathways.

Conclusion: UPEE and MOME extracts acts as pharmacological agents for anti-obesity genes. PPAR-γ-4CI5 has a best docking score (-7.716 kcal/mol), as a result. As a result, the standard was recommended as the best antagonist to block the key enzyme involved in the drug development pathways.

INVESTIGATING THE ROLE OF NANOPARTICLE-BASED CURCUMIN IMPLANTS IN PREVENTION OF POST-LAPAROTOMY PERITONEAL ADHESION: AN IN VIVO STUDY

Sat, 07 Sep 2024 00:00:00 +0530

Objective: The objective of this research is to develop a controlled-release drug delivery system for relieving peritoneal adhesion. The system is designed to utilize a polymer hydrogel incorporating Curcumin (cur) loaded Mesoporous Silica Nanoparticles (Msn). Its objective is to improve the properties of curcumin and reduce peritoneal adhesion after laparoscopic surgery.

Methods: The rats in each group underwent intra-abdominal adhesion modeling surgery and received the following implants: implants containing Msn loaded with cur (imp/Msn@cur), Implants Containing Cur (imp/cur), implants containing Msn without cur (imp/Msn), Implants without Msn and cur (imp) and group only modeled (contrl). After 14 d, the surgical site was reopened and the specimens were evaluated by gross processing and histology staining for adhesion band formation, fibrosis, and inflammation. Data were analyzed by SPSS v.22 using Fisher's exact test, one-way ANOVA, and Tukey's test and P˂0.05 was considered statistically significant.

Results: The number of vascularized or non-vascularized adhesion bands was evaluated According to the results, the number of vascular bands in the control group was only significantly higher than the other groups (P<0.001). Also, the mean number of vascular adhesion bands in the imp group was significantly higher than the other intervention groups (P<0.001). All studied rats in the contrl group had adhesions and the severity of adhesions in this group was higher than the others. Also, in the imp/Msn@cur group, the severity of adhesion was the lowest than the other groups.

Conclusion: The research findings indicated that utilizing implants with cur-loaded Msn resulted in improved peritoneal adhesion and reduced collagen bandages following laparotomy.

DRUG EXCIPIENT ADSORPTION TECHNIQUE FOR THE PREPARATION OF LOW-DOSE TABLETING

NIKHITHA K. SHANMUKHAN, RAMYA G., ARUN RADHAKRISHNAN — Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study aimed to improve drug mixability and drug uniformity in personalized medicine low-dose tablet by developing a stable, easily mixable, drug-adsorbed filler.

Methods: The research involved adsorbing drug onto filler by using three solvents and drug-to-excipient ratios of 1:50 and 1:75. The drug adsorbed fillers, were analyzed for drug content uniformity and flow properties, which are crucial for accurate dosing and manufacturing of low dose tablet.

Results: Formulations T1, T2 and T3 showed similar flow properties, including bulk and tapped densities, Carr's indices, and Hausner ratios. T1 had better flowability with a lower angle of repose (23.97 degrees) compared to T2 (35.42 degrees), T3 (49 degrees), and T4 (39 degrees) and it also had higher drug uniformity (99.89%, 99.54%, 97.12%, 96.83%). Tablet evaluations of TS1, TS2, TS3 and TS4 met standard criteria for weight variation, friability, and hardness criteria, with TS1 showing a quicker disintegration time (2:58 min), indicating faster dissolution and potentially better bioavailability. Dissolution tests showed both exceeded 85% drug release within 30 min, with TS1 achieving a higher release (99.98), suggesting more efficient drug release.

Conclusion: The drug-adsorbed filler premix technique effectively ensures drug content uniformity and improves low-dose drug mixing, contributing to the development of safe, efficient low-dose pharmaceuticals.

MOLECULAR DOCKING STUDY AS THERAPEUTIC APPROACH FOR TARGETING CHOLECYSTOKININ IN PANCREATIC CANCER

OKTAVIAN ARYA PUTRA, TESIA AISYAH RAHMANIA, EDITHA RENESTEEN — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The Cholecystokinin A receptor (CCK-ARs), also known as CCK1 receptor, is a type of G protein-coupled receptor that is primarily responsive to the hormone Cholecystokinin (CCK). CCK-ARs is one of the receptors characterized and validated to promote pancreatic cancer progression. Devazepide is a selective antagonist of the CCK-ARs. This study aims to find a potential ligand that has the most effective and representative interaction with cancer receptors, becoming a new therapeutic effect using molecular docking Molecular Operating Environment (MOE) with receptor code 7F8U.

Methods: We conducted an in silico study by docking candidate ligands with Cholecystokinin Receptor (CCKRs) using the MOE 2015 V.10 application. The ligands of choice come from natural ingredients such as curcumin, resveratrol, berberine, baicalein, dioscin, wogonin, and piperine. Validate the receptor with the Root mean Square Deviation (RMSD) value and docking results with the GIBBS S value.

Results: 6 compounds, such as curcumin, resveratrol, berberine, baicalein, wogonin, and piperine, were selected for docking as candidates to determine whether they have interactions with CCK-ARs. Based on the docking results, the Gibbs values obtained were -14.9522;-12.4566;-15.5033;-12.6961;-13.4234;-11,6130 joules/kg. mol, berberine is the compound with the lowest Gibbs energy, namely -15.5033 joules/kg. mol and is one of the strongest. The interactions that occur include Methionine A121-side chain donor, Methionine B121-side chain donor, asparagine A333-amine group and nitrogen atom, B333-amine group and nitrogen atom, Arginine A336-negative oxygen atom, and B336-negative oxygen atom.

Conclusion: Berberine which is a natural alkaloid, is suitable for devazepide, which is a positive control for ligand interactions when tethered to the CCKRs. This finding could be a potential new drug for pancreatic cancer. However, further studies, such as in vitro, in vivo, and clinical trials need to be conducted for ordering activity, safety, and safety of new drugs.

DEVELOPMENT AND VALIDATION OF A SPECIFIC AND UNIQUE DUAL POLARITY ESI-LC-MS/MS METHOD FOR SIMULTANEOUS DETERMINATION OF SEMAGLUTIDE AND DAPAGLIFLOZIN IN HUMAN PLASMA

JAGAPATHI RAJU VATSAVAYI, NALANDA BABY REVU — Sat, 07 Sep 2024 00:00:00 +0530

Objective: To develop a method capable of simultaneous quantification and estimation of semaglutide and dapagliflozin which are being studied as a prospective combination therapy for treating Diabetes.

Methods: An intricate protein precipitation extraction technique was employed using verapamil and tolbutamide as internal standards for semaglutide and dapagliflozin, respectively. The two compounds were separated on a Kinetex C18 (50 mm x 2.1 mm, 5 µ Particle size) column, with a dual polarity ionization Electro Spray Ionization (ESI) on a Liquid chromatograph Tandem Mass Spectrometry (LC-MS/MS) instrument. The detection was carried out with a Multiple Reaction Monitoring (MRM) method, and a gradient program utilizing Acetonitrile and water as mobile phases to achieve a separation in 3 min.

Results: The method established was proved linear over a working range of 1.00 ng/ml to 1000 ng/ml and 2.00 ng/ml to 2000 ng/ml for semaglutide (r²>0.98) and dapagliflozin (r²>0.98) respectively in human plasma. The accuracy, recovery, and matrix effects were within acceptable limits. The stability was also established under various conditions as necessitated by the International Council for Harmonisation of Technical Requirements of Pharmaceuticals for Human Use (ICH) M10 guideline on Bioanalytical method validation.

Conclusion: This highly selective and sensitive method where 1.00 ng/ml for semaglutide and 2.00 ng/ml for dapagliflozin as the Lower Limit of Quantification (LLOQ) can be utilized for estimation in human plasma will facilitate the further application to pharmacokinetic and bioequivalence studies for combination of these two drugs in pharmaceutical dosage forms.

FABRICATION, OPTIMIZATION AND IN VITRO CYTOTOXICITY EVALUATION OF DASATINIB MONOHYDRATE-LOADED NANOPARTICLES

AJAY SAROHA, RAVINDER VERMA, VINEET MITTAL, DEEPAK KAUSHIK — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The present research aimed to formulate, optimize and evaluate dasatinib monohydrate-loaded nanoparticles using the ionic gelation method as a potential anticancer drug delivery system for enhancing its dissolution rate.

Methods: Box-Behnken design was implemented to study the effects of selected parameters chitosan concentration (X₁), Sodium Tripolyphosphate (NaTPP) concentration (X₂), and NaTPP volume (X₃) on the drug release from developed nanoparticles. Moreover, optimized formulation was evaluated for various parameters, including X-ray diffraction, differential scanning calorimetry, fourier transform infra-red, in vitro drug release and drug kinetics. Then, in vitro cytotoxicity was executed via MTT assay method on leukemia cell lines (RPMI 8226).

Results: The results showed optimal conditions for maximum encapsulation efficiency and minimum particle size were a low chitosan concentration, a medium NaTPP concentration, and a high NaTPP volume. The optimized batch (NP-7) demonstrated promising results with an encapsulation efficiency of 83.12±0.17%, particle size of 96.8 nm, and an in vitro cumulative drug release of 91.37±0.49% after 24 h. The cytotoxicity of dasatinib monohydrate was higher when administered in polymeric nanoparticles (NP-7) as compared to its pure form.

Conclusion: From this research, it can be concluded that the drug release was enhanced when dasatinib monohydrate was loaded into chitosan nanoparticles.

THE BINARY AND TERNARY AMORPHOUS SYSTEMS OF CANDESARTAN CILEXETIL PREPARATION TO IMPROVE ITS SOLUBILITY

FIKRI ALATAS, HESTIARY RATIH, TITTA HARTYANA SUTARNA, MUHAMAD LUTHFI FAUZI — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The objectives of this work was to prepare the binary and ternary amorphous systems of Candesartan cilextil (CAN), characterize these, and evaluate their influence on solubility.

Methods: CAN was prepared in three amorphous systems, namely Candesartan cilexetil-l-Arginine (CAN-ARG) binary Co-Amorphous System (CAMS), CAN with 10, 20, and 30% of Polyvinylpyrrolidone K25 (CAN-PVP K25) Amorphous Solid Dispersion (ASD), and CAN-ARG with 10, 20, and 30% of PVP K25 (CAN-ARG-PVP K25) ternary CAMS. All amorphous systems were characterized by polarizing microscopy and differential scanning calorimetry (DSC) methods, while the degree of crystallinity was calculated based on powder X-ray diffraction (PXRD) patterns. The solubility test of all amorphous systems of CAN was carried out respectively in water solvent (25±0.5 °C) and phosphate buffer solution with a pH of 6.5 that contained 0.70% polysorbate 20 at 37±0.5 °C.

Results: Polarization microscope images showed no birefringence in CAN-ARG and CAN-ARG-PVP K25 CAMS, but strong birefringence in CAN-PVP K25. DSC thermograms show the glass transition of CAN-ARG-PVP-K25 was in the range 101-120.8 °C higher than CAN-PVP-K25 (84.1-87.5 °C) and CAN-ARG (53.5 °C). The crystallinity degrees of CAN, CAN-ARG, CAN-PVP K25, and CAN-ARG-PVPK25 calculated based on powder X-ray diffractogram data were 73.68, 7.52, 17.20, and 0.02%, respectively. The order of solubility of CAN in water and phosphate buffer solution with a pH of 6.5 that contains 0.70% polysorbate 20 was CAN-ARG-PVP-K25>CAN-ARG>CAN-PVP-K25>CAN.

Conclusion: The synthesis of binary and ternary amorphous CAN has resulted in positive outcomes, enhancing its solubility.

PULMONARY DRUG DELIVERY SYSTEMS OF POSACONAZOLE: DEVELOPMENT AND OPTIMIZATION THROUGH QUALITY BY DESIGN

INDIRAMUZIB YALLAMALLI, SREEVIDYA PUVVALA — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The main objective of this work is a formulation of nano-embedded microparticles of posaconazole for targeted delivery into lungs through pulmonary route.

Methods: Posaconazole Nano-Crystals (PNCs) were developed through quality by design approach. Influences of sonication time, sonication power, stabilizer type and its concentration on the solubility and time for 90% drug dissolution (T90%) of the PNC were studied through central composite design. Nanoembedded Microparticles of Posaconazole (NMPs) were developed by nano-crystallization using surfactants to enhance the solubility of posaconazole and then the optimized PNCs were embedded into lactose matrix to enhance the size through lyophilization to obtain NMPs that were suitable for inhalational administration.

Results: The optimized formulation of PNCs was found to exhibit a particle size of 159.2 nm, solubility of 0.29 mg/ml and T90% of 24.7 min. This optimized PNCs were embedded into lactose using lyophilization. The lyophilized product was sieved to obtain NMPs with a size below 5 µm.

Conclusion: The optimized formulation is highly suitable for delivering the drug to lungs through inhalation in which drug particles reach secondary bronchi where they can dissolve readily to yield PNCs. These PNCs can easily escape into alveolar fluids for immediate local action.

SMART CHITOSAN-BASED MICROBEAD FORMULATION FOR COLON-TARGETED DELIVERY OF LACTOFERRIN

LUQMAN OLAOYE, AZAD SADRADDIN, SHWANA BRAIM — Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study aims to develop a novel smart formulation based on dual-responsive Polyethylene Glycol Methacrylate-Grafted-Chitosan (PEGMA-g-Cs) copolymers for the controlled delivery of Lactoferrin. The goal is to enhance the bioavailability and therapeutic efficacy of Lactoferrin in treating colorectal cancer, addressing its rapid degradation in a highly acidic gastric environment.

Methods: Gold-coated Superparamagnetic Iron Oxide Nanoparticles (Au-SPIONs) were synthesized and loaded into PEGMA-g-Cs microspheres. Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM), Proton Nuclear Magnetic Resonance (HNMR), X-Ray Diffraction (XRD), Infrared Spectroscopy (IR), UV-visible spectrophotometry (UV-Vis), optical microscopy, and Dynamic Light Scattering (DLS) were used to characterise the synthesized materials. Drug loading and release studies of lactoferrin-loaded microbead formulations were conducted to evaluate encapsulation efficiency, loading capacity, and release profiles.

Results: The lactoferrin-loaded microbead formulations demonstrated excellent encapsulation efficiency and loading capacity. Specifically, Encapsulation Efficiency (EE) was 77% and Loading Capacity (LC) was 4.99% for the homogenizer batch, while the magnetic stirring batch achieved 86% EE and 3.12% LC. The formulation exhibited minimal release (<20%) in Simulated Gastric Fluid (SGF) and almost complete release in Simulated Colonic Fluid (SCF). The 3-[4,5-Dimethylthiazol-2-Yl]-2,5-Diphenyl Tetrazolium Bromide (MTT) cell cytotoxicity assay in human CaCo-2 colon cancer cells revealed a significant reduction in cell proliferation following treatment with the new formulations.

Conclusion: The findings suggest that the new formulation can be a promising approach for the targeted delivery of Lactoferrin, thereby improving the efficacy of colorectal cancer treatment by enhancing the bioavailability of lactoferrin.

INHIBITION ACTIVITY OF LIQUID SMOKE COCOS NUCIFERA L. ON DPP-IV AND AGE-RAGE IN SILICO AND IN VITRO: ANTIDIABETIC AND ANTI-INFLAMMATORY ACTIVITY

MASFRIA, HENNY LUCIDA, YUSI ATIFAH, HAFID SYAHPUTRA, HANNA MURTI SIHOMBING — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The research aims to predict the inhibitory activity of liquid smoke compounds from coconut shells (Cocos nucifera L.) In silico and to determine the activity on reduction of glucose levels by the Nelson-Somogyi method and anti-inflammatory effect on the inhibition of protein denaturation in vitro.

Methods: This research used biological activity prediction, physicochemical prediction, molecular docking, and in vitro analysis using a UV-Vis spectrophotometer.

Results: There were 13 liquid smoke compounds from Gas Chromatography-Mass Spectrometry (GCMS) result and shows that every liquid smoke compound has wound-healing activity and complies with Lipinski's Rule of Five. Urea did not fulfil the AMES Toxicity parameter, and four compounds had the highest level of toxicity. From the docking results, the binding affinity score between liquid smoke compounds and DPP4 inhibitors ranged from-5.3 to-3.0. Meanwhile, the Advance Glycation End Products Receptors (AGE-RAGE) receptor went from -2.5 to -1.5. 13 compounds had inhibitory activity on Dipeptidyl Peptidase 4 (DPP4); meanwhile, there are 12 compounds on AGE-RAGE In silico. The activity of liquid smoke antidiabetic at 10 µg/ml was 31.26%, while quercetin was 46.36%. In the anti-inflammatory analysis, the IC50 value of the liquid smoke compound was 22.41 µg/ml, while diclofenac sodium was 0.42 µg/ml.

Conclusion: The result shows that 13 liquid smoke compounds had inhibitory activity on DPP4, while 12 compounds on AGE-RAGE were In silico. The in vitro results found that liquid smoke compounds have glucose-reducing activity, and from the IC50 value, it is concluded that both compounds have potent anti-inflammatory activity.

BRINZOLAMIDE-LOADED ETHO-LECIPLEX FOR EFFECTIVE OCULAR MANAGEMENT OF GLAUCOMA: D-OPTIMAL DESIGN OPTIMIZATION AND IN VIVO EVALUATION

Sat, 07 Sep 2024 00:00:00 +0530

Objective: Brinzolamide (BRZ) is an active carbonic anhydrase inhibitor adopted for glaucoma management. The limited aqueous solubility of the drug restricts its potential for ocular administration. Therefore, the aim of this investigation was to design a nanocarrier system called Etho-Leciplex (Etho-LPs) for the delivery of BRZ.

Methods: Etho-LPs were fabricated by a simple one-step technique and then optimized by D-optimal design employing Phospholipon^®90G (PC): surfactant ratio and surfactant type (Cetyl Trimethyl Ammonium Bomide (CTAB) and Searylamine; SA) as independent variables, whereas the dependent variables were Entrapment Efficiency (EE%), Particle Size (PS), Polydispersity Index (PDI), and Zeta Potential (ZP). Design Expert^® statistically suggested the optimum Etho-LP, which consisted of PC: Surface Active Agent (SAA) molar ratio (X₁) of 1:1.27 and mixture of CTAB and SA (X₂) in 1:1 molar ratio.

Results: The optimum Etho-LPs particles had spherical morphology, and EE% of 91.12±0.2 %, PS of 76.21±1.21 nm, PDI of 0.421±0.001 and ZP of 35.88 ±0.10 mV. The in vitro release study results demonstrated that BRZ is rapidly liberated from the optimum Etho-LPs compared to BRZ-suspension. Further, the optimum Etho-LP showed good mucoadhesive properties besides potential safety on rabbits’ eyes tissues. The optimum Etho-LP was found to enhance the ocular bioavailability of the drug in rabbits’ eyes relative to the BRZ suspension. In addition, histopathological assessment indicated the safety of BRZ-loaded Etho-LPs.

Conclusion: Overall, the obtained outcomes indicated the effectiveness of employing Etho-LPs for the treatment of glaucoma.

ZAP-AIRTMMICRONIZER: IMPACT ON NEBULIZED SALBUTAMOL SULPHATE AND IPRATROPIUM BROMIDE PARTICLE SIZE

MUHAMMAD IZZUDDIN ZAMERY, SHARIZA SAHUDIN, SHAHARIZUAN ABDUL RAHMAN, ALBERT KOW — Sat, 07 Sep 2024 00:00:00 +0530

Objective: This study aimed to investigate the effect of the patented Zap-Air™ Micronizer on the particle size reduction of salbutamol sulphate (Ventolin), ipratropium bromide (Atrovent), and their combination (Combivent) nebulizing solutions.

Methods: The study used an Omron Compressor Nebulizer NE-C28 and compressed oxygen at flow rates of 3L and 6L per minute. Particle size analysis was conducted using Malvern Spraytec Laser Diffraction System to measure DV4 (4% of particles in the sample), DV50 (50% of particles in the sample), DV90 (90% of particles in the sample). Drug deposition analysis was performed using the Next Generation Pharmaceutical Impactor (NGI) with High-Performance Liquid Chromatography (HPLC) to analyze the content at each stage.

Results: The Zap-Air™ Micronizer effectively reduced the particle size of salbutamol sulphate and ipratropium bromide to less than 2 μm. Both Unit 1 and Unit 2 micronizers showed significant particle size reduction, with the average size of 50% of particles (DV50) being below 1 μm. Drug release intensity was significantly reduced when using the micronizers compared to the nebulizer alone.

Conclusion: The Zap-Air™ Micronizer has the potential to enhance drug delivery and therapeutic effects in the treatment of Asthma and Chronic Obstructive Pulmonary Disease (COPD) by improving the deposition of salbutamol sulphate and ipratropium bromide into the smaller airways of the lungs.

EVALUATION OF POPULATION PHARMACOKINETICS OF ORAL DIGOXIN IN VENOUS PLASMA

SIRAJUDEEN MAHABOOB, ARUN K. P., S. D. RAJENDRAN, GNK GANESH — Sat, 07 Sep 2024 00:00:00 +0530

Objective: Digoxin, a cardiac glycoside with extensive clinical usage, poses challenges due to its narrow therapeutic index and wide interindividual variability. Population pharmacokinetic studies in healthy individuals are scarce despite their importance in understanding drug kinetics. This study aimed to characterize the population pharmacokinetics of oral digoxin in healthy volunteers.

Methods: An open-label, single-dose pharmacokinetic study was conducted in 72 healthy Indian adults using digoxin tablets. Plasma samples were collected at various time points, and digoxin concentrations were quantified using Liquid Chromatography-Mass Spectrometry (LC-MS). Population pharmacokinetic analysis was performed using PUMAS^® software, incorporating covariates such as creatinine clearance.

Results: The two-compartment model best described the data, with a population estimate of clearance (CL/F) of 12.08 l/h in the base model and 8.3 l/h in the final model. Creatinine clearance significantly influenced digoxin clearance. Goodness-of-fit plots indicated model appropriateness, and Monte Carlo simulation validated model performance.

Conclusion: This study presents a novel population pharmacokinetic model for oral digoxin in healthy individuals. The model accurately predicts digoxin pharmacokinetics and can guide dosage regimen optimization for better therapeutic outcomes. Further research should explore drug interactions and validate the model in diverse populations.

NAVIGATING NITROSAMINES: ORIGIN, DETECTING, ANALYSING AND REGULATING IMPURITIES IN PHARMACEUTICALS

Sat, 07 Sep 2024 00:00:00 +0530

N-nitrosamines are carcinogenic impurities mostly found in groundwater, treated water, foods, beverages, and consumer products like processed meats, alcoholic beverages, cosmetics, and cigarette smoke. The recent discovery of N-nitrosamines in pharmaceutical products and subsequent recalls pose a significant health risk to patients. Nitrosamine impurities in drug products have appeared as a critical concern in pharmaceuticals prompting extensive scrutiny from regulatory agencies and stakeholders. To avoid carcinogenic and mutagenic effects in patients relying on these medications, authorities have established specific guidelines in risk assessment scenarios and proposed control acceptable limits for nitrosamine impurities in pharmaceuticals. This review provides an information on historical background of Nitrosamine impurities; its carcinogenic effect; the sources and formation of impurities; associated risks of nitrosamines in drug formulations; different analytical techniques for nitrosamine detection. It also gives an understanding of the general Quality Risk management (QRM) process, techniques for measuring nitrosamine impurities with control strategies as directed by the regulatory authorities and how to avoid them in pharmaceutical drug products. A brief review on recalls of drug classes including angiotensin II receptor antagonists, histamine-2 receptor antagonists, antimicrobial agents, and antidiabetic drugs by regulatory bodies due to its potential harm produced by nitrosamine have been discussed. Moreover, the regulatory landscape governing nitrosamine impurities are explored, encompassing recent guidelines from major regulatory bodies such as the United States Food and Drug Administration (USFDA), European Medicines Agency (EMA) and Health Canada (HC) in controlling/eliminating the nitrosamine impurities in pharmaceuticals.

BEYOND THE HORIZON: RECENT ADVANCES IN HOT MELT EXTRUSION TECHNIQUES AND TECHNOLOGIES

MAGED MOHAMMED ABDO MOHSEN, AMIT B. PATIL, MAGED ALKANAD, DARSHAN PATIL — Sat, 07 Sep 2024 00:00:00 +0530

This review article aims to explore the dynamic landscape of Hot Melt Extrusion (HME) technology, focusing on the spectrum of materials and machinery shaping innovation in the field. Polyethylene Oxide (PEO), Polyvinylpyrrolidones (PVP), Polypropylene (PP), Polyvinyl Acetate (PVA), and Polycaprolactone (PCL) play pivotal roles in HME and contribute to advancements in pharmaceutical manufacturing. This review sheds light on their unique contributions to HME tapestry. This review meticulously explored the machinery that orchestrates HME, including single- and double-screw extruders, as well as Extrusion Spheronization (ES). The search criteria were based on a comprehensive analysis of previous studies since the discovery of the HME, including new patented discoveries. We utilized various scholarly resources such as Google Scholar, Google Books, PubMed, Elsevier, Nature, Springer, ScienceDirect, and other indexed search engines. Case studies highlighted the real-world impact of HME in Continuous Manufacturing (CM) scenarios, emphasizing its importance in pharmaceutical production. The review also discusses the specifics of extrusion and co-extrusion, explaining how compound droplets are formed and collected, which is very important for making capsules-extrusion has emerged as a protagonist in the pharmaceutical industry, with 3D printing driving innovation beyond conventional boundaries. The amalgamation of HME and 3D printing offers new possibilities for drug delivery. This review sheds light on the diverse polymers involved in hot melt and emphasizes their importance in pharmaceutical manufacturing. This study provides valuable insights into the applications, methodologies, and future advancements of HME.

METALLOPROTEIN PARAMETERS IN MOLECULAR DYNAMICS SIMULATION FOR AMBER, CHARMM, GROMACS, AND NAMD: A SYSTEMATIC REVIEW

PURNAWAN PONTANA PUTRA, NAJMIATUL FITRIA, AIYI ASNAWI, AKMAL DJAMAAN — Sat, 07 Sep 2024 00:00:00 +0530

Objective: The selection of appropriate metal parameters for molecular dynamics simulations is a significant challenge. Therefore, this review aims to provide in-depth insights valuable for the optimization of parameter selection in the context of chemical simulations.

Methods: A total of 550 scientific articles were collected from pubmed and science direct databases from 2009 to 2024, resulting in the inclusion of 60 full studies for review. The selection process of preferred reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) was utilized, enabling the conduction of an initial screening of articles by use of the Rayyan web-based application.

Results: This study found that the modeling and parameterization of metal proteins were categorized into Bonded and Non-Bonded Models. The Bonded Model incorporates MCPB, a Python-based software that facilitates parameter construction for over 80 metal ions and force fields in molecular dynamics simulations. The Non-Bonded Model evaluates metals in proteins, such as zinc, nickel, magnesium, cobalt, iron, and cadmium by using AMBER force field and the Seminario method. The 12-6 lennard-Jones (LJ) non-bonded model is suitable for divalent, trivalent, and tetravalent metals, with Zinc parameters being compared for accuracy. Additionally, the force fields suitable for modeling unbound metal proteins include AMBER FF19SB, FF14SB, ff9X, CHARMM36, CHARMM22, CHARMM27, and CHARMM-Metal.

Conclusion: This study found that the modeling and parameterization of metal proteins were categorized into Bonded and Non-Bonded Models. Molecular Dynamics (MD) simulations can be conducted using various methods, such as classical molecular dynamics, Umbrella Sampling, Quantum Mechanics-Discrete Molecular Dynamics (QM/DMD), Stochastic Boundary Molecular Dynamics (SBMD), Steered Molecular Dynamics (SMD), Gaussian accelerated molecular dynamics (GaMD) and Random Acceleration Molecular Dynamics (RAMD).

STATINS: A NEW THERAPEUTIC APPROACH FOR THE TREATMENT OF NEUROPATHIC PAIN

Sat, 07 Sep 2024 00:00:00 +0530

Due to a lesion or chronic illness state that affects the somatosensory nerve system, Neuropathic Pain (NP) is a terrible ailment. NP has recently been a top problem for the pharmaceutical and medical industries. For the therapy of NP, stains may offer an additional source of illumination. By preventing 3-Hydroxy-3-Methylglutaryl-Coenzyme a (HMG-CoA), it prevents the rate-limiting step in cholesterol production. HMG-CoA reductase inhibitors, which have a pleiotropic impact in addition to the cholesterol-lowering effects of statins, have also been linked to neuropathic pain. According to reports, statins can worsen endothelial dysfunction by making more nitric oxide available. Antioxidant, antiproliferative, and immunomodulatory activities are known to exist in it. It primarily comes highly suggested for cardiovascular issues and helps to reduce inflammation. Atherosclerotic plaque is under its control. To the best of our knowledge, this subject has not yet been the subject of clinical research in humans. Up until now, most of the evidence pointing to a connection between statins and neuropathic pain has been speculative. As a result, this evaluation should be considered a synopsis of what is already known, what is being investigated, and where more research might be needed. This review assesses the statins for neuropathic pain in preclinical as well as clinical research.

DIAGNOSTIC AND THERAPEUTIC ROLE OF MESOPOROUS SILICA NANOPARTICLES IN COMBATING CANCER

NUPUR KATARIYA, ARVIND SINGH FARSWAN, NIDHI NAINWAL, GANESH KUMAR — Sat, 07 Sep 2024 00:00:00 +0530

Cancer is a global health problem of human beings that is growing day by day despite several advancements in the medical field. The main concern of cancer treatment is the timely and proper diagnosis of this disease and the targeting of therapeutic moieties to the cancer site. Nanotechnology has emerged as a boon for the healthcare system in treating various life-threatening diseases. Mesoporous Silica Nanoparticles (MSNs), have drawn interest in the diagnosis and treatment of cancers and various other diseases. MSNs can be easily adjusted to specifically target cancer cells, improve drug targeting and minimize the undesirable effects. In the imaging and diagnosis of cancer, MSNs can be altered with imaging agents or used as contrast agents in imaging techniques like Magnetic Resonance Imaging (MRI) and Computed Tomography (CT). MSNs can be used to deliver different types of therapeutic molecules alone or in combinations to provide a synergistic effect in eradicating cancer. The current review focused on highlighting the role of MSNs in combating cancer. In addition, the biodegradation, clearance and toxicity profile of MSNs is explained to evaluate their suitability for clinical applications.

CURRENT PERSPECTIVES ON USING NANOPARTICLES FOR DIABETES MANAGEMENT

NITESH KUMAR YADAV, RUPA MAZUMDER, ANJNA RANI, ARVIND KUMAR — Sat, 07 Sep 2024 00:00:00 +0530

If ignored, Diabetes Mellitus (DM), a chronic metabolic disease marked by high levels of blood glucose, can have serious negative effects on one's health. The efficacy, safety, and patient compliance of traditional treatment approaches, like insulin injections and oral medications, are frequently hampered. Nanoparticle-based methods have shown promise in recent years as improved diabetes management techniques. Enhanced bioavailability, prolonged therapeutic effects, and targeted drug delivery are just a few of the special benefits that come with using nanoparticles. An overview of current perspectives on using nanoparticles for diabetes control is given in this review. The properties, production processes, and potential uses of several types of nanoparticles, such as polymeric, lipid-based, and inorganic nanoparticles, in the management of diabetes are covered. These nanoparticles allow for the precise delivery of therapeutic agents, such as insulin or anti-diabetic medications, to specific target tissues, like the liver or pancreas. It discusses how inorganic nanoparticles, Polymeric Nanoparticles (PNPs), and Lipid-Based Nanoparticles (LNPs) contribute to improved drug solubility, targeted delivery, and controlled release. Several methods for synthesizing polymeric nanoparticles are described. It also discusses the potential anti-inflammatory and antioxidant properties of some nanoparticles and how crucial they are to lowering diabetes-related issues. By incorporating the most recent research, this review offers a comprehensive summary of the current developments in the use of nanoparticles for diabetes control, paving the way for enhanced therapeutic outcomes and tailored interventions.

THERAPEUTIC IMPACT OF NANOMEDICINE FOR THE TREATMENT OF NEUROPATHIC PAIN: PRINCIPLE, PROSPECTIVE AND FUTURE

Sat, 07 Sep 2024 00:00:00 +0530

Researchers in medicine and pharmacology are working to develop more effective and focused painkillers as a result of growing public awareness of chronic pain brought on by disease and injury. On the other hand, overreliance on medically prescribed painkillers has resulted in several unfavorable outcomes, including drug addiction, tolerance, and other severe side effects that can worsen pain and reduce their efficacy. Drug delivery has benefited from the use of nanotechnology in reducing adverse effects, increasing therapeutic efficacy, and delaying tolerance development. Neuropathic pain is pain that develops as a result of nerve malfunction as well as damage to the somatosensory nervous system. The exact cause of neuropathic pain is not specifically clear. However, many factors, including spinal cord damage, Chronic Constriction Injury (CCI), diabetes, cancer, alcoholism, and trauma, can cause neuropathic pain. There is no doubt that we have many options for conventional treatment, yet either very few patients receive pain relief, or their pain relief is only momentary. Numerous nanocarrier varieties and the accompanying neuropathic pain treatment modalities were also examined. These forms included those based on nonpolymeric nanoparticles, polymeric micelles, lipids, and emulsions. Comparing nanomaterials to other forms of therapy for chronic pain, there are several benefits: reduced side effects, regulated release, and prolonged circulation. Alongside nanotechnology, approaches to treating chronic pain are surface-modification-based and employ a variety of nanoparticles. The current state of the pain-relieving effect of nanomaterial design is covered in the present review article.

LEVERAGING THE SUCCESS OF MRNA LIPID NANOPARTICLE VACCINE IN COVID-19 TREATMENT: A NARRATIVE REVIEW ON ITS POTENTIAL APPLICATION IN MALARIA TREATMENT

FRANKLYN NONSO IHEAGWAM, ENIOLA DEBORAH ADEDOYIN — Fri, 07 Jun 2024 00:00:00 +0530

Malaria, which is caused by the Plasmodium parasite and transmitted by mosquitoes, continues to be a major global health issue. The worldwide health community continues to work toward finding a conclusive answer to the malaria problem, but it is still elusive. Developing a successful malaria vaccine has proven difficult due to the Plasmodium parasite’s complicated life cycle and ability to change and develop resistance to interventions rapidly. Amidst this backdrop, the advent of mRNA Lipid Nanoparticle (mRNA-LNP) vaccines, exemplified by their resounding success in mitigating the Coronavirus Disease 2019 (COVID-19) pandemic, has kindled newfound hope in vaccine development. This review examines the potential of leveraging mRNA technology to induce a robust immune response, thereby potentially revolutionising the landscape of malaria prevention through the development of breakthrough malaria vaccines. The intricate interplay between the efficacy of the mRNA-LNP vaccine against COVID-19 and its prospective utility in addressing malaria is also deliberated upon.

AQUASOMES UNVEILED: TRANSFORMING DRUG DELIVERY WITH CUTTING-EDGE THERAPEUTIC CARRIERS AND RECENT BREAKTHROUGHS

Sat, 07 Sep 2024 00:00:00 +0530

The study presented herein explores the groundbreaking utilization of aquasomes, which are sophisticated colloidal ceramic carbohydrate composites, as carriers for the transportation of hemoglobin. These aquasomes undergo strategic surface modification with carbohydrates, leading to the development of a protective molecular layer characterized by a resilient glassy texture. This innovative approach effectively safeguards therapeutic proteins by forming a molecular shield, thus mitigating potential structural damage during transit. Crucially, aquasomes demonstrate remarkable efficacy in preserving encapsulated drugs within aqueous environments. This is achieved by shielding the drugs from the adverse effects of fluctuating pH levels and temperature variations, which could otherwise induce denaturation. Importantly, the protective capability of aquasomes remains intact, exhibiting no alterations in swelling or porosity despite changes in external conditions.

Furthermore, this article sheds light on recent breakthroughs in aquasomes research, highlighting their diverse applications and promising future avenues. In particular, the focus is on the use of aquasomes for the transport of hemoglobin and therapeutic proteins, underscoring their potential transformative impact in the field of biomedical sciences. The incorporation of aquasomes as carriers for hemoglobin transportation represents a significant advancement in drug delivery technology. By harnessing the unique properties of aquasomes, researchers have opened up new possibilities for the safe and efficient transport of therapeutic proteins, offering hope for the development of novel treatments for a range of medical conditions. Overall, this study underscores the immense potential of aquasomes in revolutionizing biomedical research and improving patient outcomes.

EMERGING FRONTIERS: ADVANCEMENTS IN BIO-NONMATERIAL’S AND NON-INVASIVE STRATEGIES FOR COMBATING CANCER THROUGH PHOTO THERMAL THERAPY

YOKESH S., TEEJESWARI R., JALANIY V., LOKESHVAR R. — Sat, 07 Sep 2024 00:00:00 +0530

Cancer remained a global health challenge in 2020 and claimed approximately 10 million lives, thus rendering it the main reason for demise. Photo Thermal Therapy (PTT) has emerged as a promising approach among the various cancer therapies. PTT offers several advantages over traditional treatments such as surgery, chemotherapy, and Radiotherapy due to its precise tumor targeting and reduced damage to healthy tissues. Photo Thermal Agents (PTAs) are central to PTT and selectively kill cancer cells by converting near-infrared light into heat. However, some PTAs exhibit toxicity and remain in the body's Reticulo Endothelial System (RES), limiting their clinical utility. To address this issue, scientists are looking at putrescible nano-photothermal compounds. This study talks about the effects of PTT and other cancer treatment techniques on patient health, stares at the process beneath PTT, and highlights recent bio-nonmaterial’s utilized in PTT. It also looks at how low temperatures and brightly coloured light might be used to improve PTT efficacy.