DEVELOPMENT, OPTIMIZATION AND ASSESSMENT OF NAPROXEN MICROSPONGES BY BOX-BEHNKEN DESIGN AS A TARGETTED AND CONTROLLED RELEASE DRUG DELIVERY
DOI:
https://doi.org/10.22159/ijap.2024v16i6.51765Keywords:
Naproxen microsponges, Ethyl cellulose, Quasi emulsion technique, Box behnken design, In vitro drug release, Kinetic studyAbstract
Objective: Due to weak physical, chemical stability and poor bioavailability of Naproxen conventional dosage form; the purpose of this work is to improve formulation stability, additionally to accomplish highest possible concentration of the drug in the blood by preparing Naproxen loaded microsponges.
Methods: Naproxen Microsponge (NM) was created utilising the quasi emulsion technique. In this process Ethyl Cellulose (EC) acts as a polymer, Poly Vinyl Alcohol (PVA) acts as the emulsifier, and Dichloromethane acts as the solvent. To investigate how changes in different formulation and processing parameters affect important product qualities, a Box Behnken Design (BBD) was used. Particle Size, Percentage Yield, and Entrapment Efficiency (%EE) were selected as response factors, whereas independent variables including EC quantity (X1), PVA concentration (X2), and Stirring Speed (X3) were selected as independent variables.
Results: The microsponges underwent thorough analysis using Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FT-IR), X-Ray Diffraction (XRD), and Particle Size analysis. The evaluation included studying the morphology, drug loading, and in vitro drug release. The compatibility studies showed no chemical interactions between the drug and the polymers used. It was observed that the ratio of drug to polymer had a significant impact on drug content, EE and particle size. The SEM results revealed that the microsponges were spherical with a porous surface and had a mean particle size of 15.15 µm. The in vitro drug release studies demonstrated that the optimized Naproxen Microsponge Formulation (NMF2) achieved over 80% extended drug release by the end of 8 h, following the Corsmeyer Peppas Model.
Conclusion: The Naproxen loaded microspheres possessed a sustained release with improved bioavailability and better stability.
Downloads
References
Kadhim ZM, Mahmood HS, Alaayedi MA, Ghareeb MM. Formulation of flurbiprofen as microsponge drug delivery system. Int J Pharmacol Res. 2020;12(3):748-53.
Jain V, Jain D, Singh R. Factors effecting the morphology of Eudragit S-100 based microsponges bearing dicyclomine for colonic delivery. J Pharm Sci. 2011;100(4):1545-52. doi: 10.1002/jps.22360, PMID 20960455.
D’souza JI, More HN. Topical anti-inflammatory gels of fluocinolone acetonide entrapped in eudragit based microsponge delivery system. Res J Pharm Technol. 2008;1(4):502-6.
Osmani RA, Aloorkar NH, Ingale DJ, Kulkarni PK, Hani U, Bhosale RR. Microsponges based novel drug delivery system for augmented arthritis therapy. Saudi Pharm J. 2015;23(5):562-72. doi: 10.1016/j.jsps.2015.02.020, PMID 26594124.
Rajab NA, Jawad MS. Formulation and in vitro evaluation of piroxicam microsponge as a tablet. Int J Pharm Pharm Sci. 2016;8(2):104-14.
Jangde R. Microsponges for colon targeted drug delivery system: an overview. Asain J Pharm Tech. 2011;1(4):87-93.
Amrutiya N, Bajaj A, Madan M. Development of microsponges for topical delivery of mupirocin. AAPS PharmSciTech. 2009;10(2):402-9. doi: 10.1208/s12249-009-9220-7, PMID 19381834.
EI-Houssieny BM, Hamouda HM. Formulation and evaluation of clotrimazole from pluronic for gels. J Drug Dis Ther. 2010;4:33-43.
Yadav V, Jadhav P, Dombe S, Bodhe A, Salunkhe P. Formulation and evaluation of microsponge gel for topical delivery of antifungal drug. Int J App Pharm. 2017;9(4):30-7. doi: 10.22159/ijap.2017v9i4.17760.
Gusai T, Dhavalkumar M, Soniwala M, Dudhat K, Vasoya J, Chavda J. Formulation and optimization of microsponge-loaded emulgel to improve the transdermal application of acyclovir-a DOE based approach. Drug Deliv Transl Res. 2021;11(5):2009-29. doi: 10.1007/s13346-020-00862-w, PMID 33159290.
Jelvehgari M, Siahi Shadbad MR, Azarmi S, Martin GP, Nokhodchi A. The microsponge delivery system of benzoyl peroxide: preparation, characterization and release studies. Int J Pharm. 2006;308(1-2):124-32. doi: 10.1016/j.ijpharm.2005.11.001, PMID 16359833.
Maiti S, Kaity S, Ray S, Sa B. Development and evaluation of xanthan gum-facilitated ethyl cellulose microsponges for controlled percutaneous delivery of diclofenac sodium. Acta Pharm. 2011;61(3):257-70. doi: 10.2478/v10007-011-0022-6, PMID 21945905.
Sodiyal N. Formulation and evaluation of ketoconazole loaded microsponge gel for topical drug delivery. World J Pharm Res. 2020;9(9):1060-9.
Lakshmi PK, Marka KK, Aishwarya S, Shyamala B. Formulation and evaluation of ibuprofen topical gel: a novel approach for penetration enhancement. Int J Appl Pharm. 2011;3(3):25-30.
Shahzad Y, Afreen U, Nisar Hussain Shah S, Hussain T. Applying response surface methodology to optimize nimesulide permeation from topical formulation. Pharm Dev Technol. 2013;18(6):1391-8. doi: 10.3109/10837450.2012.723721, PMID 22994526.
Pawar AP, Gholap AP, Kuchekar AB, Bothiraja C, Mali AJ. Formulation and evaluation of optimized oxybenzone microsponge gel for topical delivery. J Drug Deliv. 2015;2015(1):261068. doi: 10.1155/2015/261068, PMID 25789176.
Kshirasagar N, Puchchakayala G, KB. Comparative pharmacokinetic studies of marketed and microsponges gel loaded with diclofenac diethylamine in rabbits. Res J Pharm Technol. 2021;14(12):6385-91. doi: 10.52711/0974-360X.2021.01104.
Sareen R, Nath K, Jain N, Dhar KL. Curcumin loaded microsponges for colon targeting in inflammatory bowel disease: fabrication, optimization, and in vitro and pharmacodynamic evaluation. Biomed Res Int. 2014;2014(1):340701. doi: 10.1155/2014/340701, PMID 25093165.
Shuhaib B, Dr. Suja C. Formulation and characterization of topical gel containing microsponge of mefenamic acid. World J Pharm Life Sci. 2018;4(2):109-19.
Syed SM, Gaikwad SS, Wagh S. Formulation and evaluation of gel containing fluconazole microsponges. Asian J Pharm Res Dev. 2020;8(4):231-9.
Jain V, Singh R. Development and characterization of eudragit RS 100 loaded microsponges and its colonic delivery using natural polysaccharides. Acta Pol Pharm. 2010;67(4):407-15. PMID 20635537.
Kiliçarslan M, Baykara T. The effect of the drug/polymer ratio on the properties of the verapamil HCl loaded microspheres. Int J Pharm. 2003;252(1-2):99-109. doi: 10.1016/s0378-5173(02)00630-0, PMID 12550785.
Priyanka NV, Neeraja P, Mangilal T, Kumar MR. Formulation and evaluation of gel loaded with microspheres of apremilast for transdermal delivery system. Asian J Pharm Clin Res. 2019;7:411-7. doi: 10.22159/ajpcr.2019.v12i2.29374.
Thavva VE, Baratam SR. Formulation and evaluation of terbinafine hydrochloride microsponge gel. Int J App Pharm. 2019;11(6):78-85. doi: 10.22159/ijap.2019v11i6.32502.
Zia RA, Nazir AK, Khan MK, Maan AA, Rashid AY. Preparation of ascorbic acid and cholecalciferol microsponges for topical application. Int J Pharm Pharm Sci. 2017;9(10):280-7. doi: 10.22159/ijpps.2017v9i10.17525.
Rajeswari S, Swapna V. Microsponges as a neoteric cornucopia for drug delivery systems. Int J Curr Pharm Sci. 2019;11(3):4-12. doi: 10.22159/ijcpr.2019v11i3.34099.
Published
How to Cite
Issue
Section
Copyright (c) 2024 SONIA GUPTA, JYOTI GUPTA
This work is licensed under a Creative Commons Attribution 4.0 International License.