POLYMERIC NANOPARTICLES FOR IMPROVED BIOAVAILABILITY OF CILNIDIPINE
DOI:
https://doi.org/10.22159/ijpps.2017v9i4.15786Keywords:
Polymeric nanoparticles, Bioavailability, Solvent evaporation, PolymersAbstract
Objective: In the present study, we aimed to optimize, characterize and evaluate poly lactic-glycolic acid nanoparticles of cilnidipine for improved permeation across the gastrointestinal tract.
Methods: Poly lactic-glycolic acid-cilnidipine (PLGA-CIL) nanoparticles were prepared by an emulsification solvent evaporation/diffusion method using polyvinyl alcohol (PVA) as a surfactant. The prepared nanoparticles were successfully characterized for particle size, shape, drug release and pharmacological effect.
Results: Polymeric nanoparticles of cilnidipine at a dose of 10 mg had a small particle size of 272 nm with smooth morphology. Nearly 81% of the drug was encapsulated in the polymeric structure and showed 18.99±0.59% of release at pH 1.2 within 3h, however, at pH 6.8 the release was 80.89±1.59%. The formulation had a better antihypertensive effect on methylprednisolone-induced hypertensive rats. The relative bioavailability of the nanoparticles was found to be 2.44 and 2.94 fold higher than the tablet and drug suspension respectively.
Conclusion: The results demonstrated that the novel delivery system offers an effective strategy for treatment of hypertension.
Downloads
References
Tandel H, Raval K, Nayani A, Upadhay M. Preparation and evaluation of cilnidipine microemulsion. J Pharm Bioallied Sci 2012;4 Suppl 1:114-5.
Prajapati ST, Maheshwari PD, Patel CN. Formulation and evaluation of orodispersible tablets of cilnidipine by spray drying technique. World J Pharm Sci 2015;4:1526-39.
des Rieux A, Fievez V, Garinot M, Schneider YJ, Préat V. Nanoparticles as potential oral delivery systems of proteins and vaccines: a mechanistic approach. J Controlled Release 2006;116:1-27.
Semete B, Booysen L, Lemmer Y, Kalombo L, Katata L, Verschoor J, Swai HS. In vivo evaluation of the biodistribution and safety of PLGA nanoparticles as drug delivery systems. Nanomedicine 2010;6:662–71.
Jawahar N, Venkatesh DN, Sureshkumar R, Senthil V, Ganesh GNK, Vinoth P, et al. Development and characterization of PLGA-nanoparticles containing carvedilol. J Pharm Sci Res 2009;1:123-8.
Kim TH, Jeong YI, Jin SG, Pei J, Jung TY, Kim IY, et al. Preparation of polylactide-co-glycolide nanoparticles incorporating celecoxib and their antitumor activity against brain tumor cells. Int J Nanomed 2011;6:2621-31.
Tomoda K, Terashima H, Suzuki K, Inagi T, Terada H, Makino K. Enhanced transdermal delivery of indomethacin-loaded PLGA nanoparticles by iontophoresis. Coll Surf B 2011;88:706–10.
Kokilambigai KS, Lakshmi KS. Analytical methodologies for determination of cilnidipine: an overview. Int J Pharm Pharm Sci 2014;6:36-8.
Geckeler KE, Rao JP. Polymer nanoparticles preparation techniques and size control parameters. Prog Polym Sci 2011;36:887-913.
Alshamsan A. Nanoprecipitation is more efficient than emulsion solvent evaporation method to encapsulate cucurbitacin I in PLGA nanoparticles. Saudi Pharm J 2014;22;219–22.
Li Z, Tao W, Zhang D, Wu C, Song B, Wang S, et al. The studies of PLGA nanoparticles loading atorvastatin calcium for oral administration in vitro and in vivo. Asian J Pharm Sci 2016. Doi:10.1016/j.ajps.2016.08.006.
Halayqa M, Domanska U. PLGA biodegradable nanoparticles containing perphenazine or chlorpromazine hydrochloride: effect of formulation and release. Int J Mol Sci 2014;15:23909-23.
DeMerlis CC, Schoneker DR. Review of the oral toxicity of polyvinyl alcohol (PVA). Food Chem Toxicol 2003;41:319–26.
Vineetha P, Vadaparthia PRR, Kumara K, Dileep B, Babu J, Veerabhadra Rao A, et al. Influence of organic solvents on nanoparticle formation and surfactants on release behaviour in vitro using costunolide as a model anticancer agent. Int J Pharm Pharm Sci 2014;6:638-45.
Zhang X, Yuan Y, Shan X, Sheng Y, Xu F, Liu C. Effects of surfactant and solvent on the encapsulation efficiency and size in using double emulsion method for preparing bovine hemoglobin loaded nanoparticles as blood substitutes. J Biomed Eng 2009;26:116-21.
Makadia HK, Siegel SJ. Poly lactic-co-glycolic acid as biodegradable controlled drug delivery carrier. Polymers 2011;3:1377–97.
Rossetti FC, Depieri LV, Bentley MVLB. Confocal laser scanning microscopy as a tool for the investigation of skin drug delivery systems and diagnosis; 2013. Available from: http: cdn.intechopen.com/pdfs-wm/43810. [Last accessed on 15 Sep 2016].
Karolewicz B. A review of polymers as multifunctional excipients in drug dosage form technology. Saudi Pharm J 2016;24:5525–36.
Gandhi A, Jana S, Kumar K. In vitro release of acyclovir-loaded Eudragit RLPO®nanoparticles for sustained drug delivery. Int J Biol Macromol 2014;67:478-82.
Ahmad J, Mir SR, Kohli K, Chuttani K, Mishra AK, Panda AK, et al. Solid nanoemulsion preconcentrate for oral delivery of paclitaxel: formulation, design, biodistribution and scintigraphy imaging. Biomed Res Int 2014;14:1-12.
Seju U, Kumar A, Sawant KK. Development and evaluation of olanzapine-loaded PLGA nanoparticles for nose-to-brain delivery: In vitro and in vivo studies. Acta Biomaterial 2011;7:4169-76.
Hua Y, Jianga X, Ding Y, Zhang L, Yang C, Zhang J, et al. Preparation and drug release behaviours of nimodipine-loaded poly(caprolactone)-poly(ethylene oxide)-polylactide amphiphilic copolymer nanoparticle. Biomaterials 2003;24: 2395-404.
Ruan LP, Chen S, Yu BY, Zhu DN, Cordell GA, Qiu SX. Prediction of human absorption of natural compounds by the non-everted rat intestinal sac model. Eur J Med Chem 2006;41:605-10.
Zakeri-Milani P, Delf Loveymi B, Jelvehgari M, Valizadeh H. The characteristics and improved intestinal permeability of vancomycin PLGA-nanoparticles as colloidal drug delivery system. Colloids Surf B 2013;103:174-81.
MaY, Zhao X, Li J, Shen Q. The comparison of different daidzein-PLGA nanoparticles in increasing its oral bioavailability. Int J Nanomed 2012;7:559-70.
Kadam RS, Bourne DWA, Kompella UB. Nano-advantage in enhanced drug delivery with biodegradable nanoparticles: contribution of reduced clearance. Drug Metab Dispos 2012;40:1380-8.
Mittal G, Kumar MN. The impact of polymeric nanoparticles on oral pharmacokinetics: a dose-dependent case study with estradiol. J Pharm Sci 2009;98:3730-4.
Ahmad J, Kohli K, Amin S. Formulation of self-nano emulsifying drug delivery system for telmisartan with improved dissolution and oral bioavailability. J Dispersion Sci Technol 2011;32:958-68.
Published
How to Cite
Issue
Section
