BIODEGRADABLE POLYMER: A NOVEL PHARMACEUTICAL CARRIER FOR SUSTAINED RELEASE OF METRONIDAZOLE
Keywords:Metronidazole, Chitosan microspheres, Scanning electron microscopy, Cross-linking
Objective: To optimize and evaluate the formulation of metronidazole (MT)-loaded chitosan microspheres and to investigate the efficiency of biodegradable polymer in developing sustained release formulation of MT to prolong the action of drug.
Methods: MT microspheres were prepared using emulsion cross-linking method. Polymer-drug compatibility study was done using Fourier transform infrared. Physical characteristics were evaluated by particle size,SEM, flow properties etc. In vitro studies for evaluating drug release for MT-loaded chitosan microspheres were done by dissolution study.
Results: Particle size of the formulated microspheres was found to be within the range of 110-130 Î¼m. Flow properties of F1-F7 such as angle of repose, bulk density, and tapped density were found to be within limits. Drug entrapment efficiency was found to be better for all the formulations within the range of 74.82-84.32% w/w. Drug loading capacity was found to be in the range of 56-83.2% w/v. In vitro drug release was found to be in the range of 81.32-96.23% w/v.
Conclusion: In spite of all the above results, we conclude that F5 formulation was optimized depending on the data obtained from the drug loading capacity and percentage drug release studies. F5 formulation is formulated with drug-polymer ratio 1:2 with 1% of di octyl sodium sulfo succinate and 8 ml of glutaraldehyde as a cross-linking agent.
Dixit N, Bhanu DM, Sagar PS. Sustained release drug delivery system. Indian J Res Pharm Biotechnol 2013;1(3):305-10.
Chugh I, Seth N, Rana AC, Gupta S. Oral sustained release drug delivery system: An overview. Int J Res Pharm 2012;3(5):57-62.
Vinothkumar G, Babu KA. Formulation and evaluation of cross linked chitosan microspheres containing mitomycin-c. Int J Pharm Bio Sci 2011;2(4):1-6.
Patel KS, Patel MB. Preparation and evaluation of chitosan microspheres containing nicorandil. Int J Pharm Investig 2014;4:32-7.
European pharmacopoeia. 5.0 01/2005:0934 pg: 2038.
Available from: http://www.drugbank.com.
Chaurasia M, Chourasia MK, Jain NK, Jain A, Soni V, Gupta Y, et al. Cross-linked guar gum microspheres: A viable approach for improved delivery of anticancer drugs for the treatment of colorectal cancer. AAPS PharmSciTech 2006;7:74.
Sannan Y, Kurita K, Iwakura Y. Studies on chitin. 2. Effect of deacetylation on solubility. Makromol Chem 1976;177(3):589-600.
Sannan T, Kurita K, Iwakura Y. Studies on chitin Vol. 1. Makromol Chem 1975;176:1191-5.
Atyabi F, Vahabzadeh R, Dinarvand R. Preparation of ethylcellulose coated gelatine microspheres as a multiparticulate colonic delivery system for 5â€“Aminosalicylic acid. Iran J Pharm Res 2004;2:81-6.
Nykanen P. Development of Multiple-unit oral formulations for colon specific drug delivery using enteric polymers and organic acids as excipients. Division of biopharmaceutics and pharmacokinetics. Ind J Pharm Edu Res 2003;5(4):1-44.
Knaul JZ, Hudson SM, Creber KA. Improved mechanical properties of chitosan fibers. J Appl Polym Sci 1999;72(3):1721-32.
Miyazaki S, Ishii K, Nadai T. The use of chitin and chitosan as drug carriers. Chem Pharm Bull (Tokyo) 1981;29:3067-9.
United States pharmacopoeia. 29â€“NF24 Page 1425.
Cina SJ, Russell RA, Conradi SE. Sudden death due to metronidazole/ethanol interaction. Am J Forensic Med Pathol 1996;17:343-6.
Williams CS, Woodcock KR. Do ethanol and metronidazole interact to produce a disulfiram-like reaction? Ann Pharmacother 2000;34:255-7.
Gupta NK, Woodley CL, Fried R. Effect of metronidazole on liver alcohol dehydrogenase. Biochem Pharmacol 1970;19:2805-8.
VisapÃ¤Ã¤ JP, Tillonen JS, Kaihovaara PS, Salaspuro MP. Lack of disulfiram-like reaction with metronidazole and ethanol. Ann Pharmacother 2002;36:971-4.
Zheng H, Du YM, Yu JH, Huang RH, Zhang LN. Preparation and characterization of chitosan/poly(vinyl alcohol) blend fibers. J Appl Polym Sci 2001:80(3):2558-65.
Umadevi SK, Thiruganesh R, Suresh S, Reddy KB. Formulation and evaluation of chitosan microspheres of aceclofenac for colon-targeted drug delivery. Biopharm Drug Dispos 2010;31:407-27.
Sriram P, Kamlekar D, Hazari S. Preparation and in vitro evaluation of chitosan microspheres of eplerenone. Int J Pharm Pharm Sci 2013;5(3):226-9.
Asha K, Vikash D. Formulation and evaluation of Zidovudine loaded chitosan microspheres for controlled release. Int J Drug Dev Res 2012;4(1):975-89.
Kumar SS, Saha AK, Kavitha K, Basu SK. Evaluation of clobazam loaded ionically cross-linked microspheres by using chitosan S. Pelagia research library. Der Pharm Sin 2012;3(6):616-23.
Dini E, Alexandridou S, Kiparissides C. Synthesis and characterization of cross-linked chitosan microspheres for drug delivery applications. J Microencapsul 2003;20:375-85.
Mzumder R, Nath LK, Haque A, Maity T, Prasanta KC, Shrestha B, et al. Formulation and in vitro evaluation of natural polymers based microspheres for colonic drug delivery. Int J Pharm Pharm Sci 2010;2(1):211-9.
Ganesh S, Kumar DS, Kumar BS, Abhilash R, Bharadwaj PS, Prudhvi Raj KV, et al. Controlled release formulation and evaluation of Idarubicin microsphere using biodegradable hydrophilic and hydrophobic polymer mixture. Asian J Pharm Clin Res 2010;3(3):179-82.
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