Chitosan Loaded Mucoadhesive Microspheres of Gliclazide - Journal

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Bushetti S.S et al./ Development and Evaluation of Mucoadhesive Buccal Films of Nebivolol 10. Singh S, Gangwar S, Garg G, Garg V, Sharma PK. Formulation and evaluation of rapidly disintegrating film of Levocetrizine Hydrochloride. Der Pharmacia Letter 2010; 2(2): 434-9. 11. Koland M, Sandeep VP, Charyulu NR. Fast dissolving sublingual films of Ondansetron Hydrochloride: Effect of additives on in vitro drug release and mucosal permeation. J Young Pharm 2010;2(3):216-22. 12. Noha AN, Fatma AI, Nabila AB, Lobna MM. Mucoadhesive buccal patches of miconazole nitrate: in vitro/in vivo performance and effect of ageing. Int J Pharm 2003; 264:1–14. 13. Vinod R, Ashok KP, Rao SB, Kulkarni SV, Shankar MS. Design and evaluation of miconazole nitrate buccal mucoadhesive patches. J Pharm Res 2010;3(6):1338-41. 162 14. Mishra P, Shah K, Gupta A. Spectrophotometric methods for simultaneous estimation of nebivolol hydrochloride and amlodipine besylate in tablets. Int J Pharm and Pharmaceutical Sci 2009;1(2):55- 61. 15. Giradkar KP, Channawar MA, Kajale AD, Sridhar E, Kamble RS, Bakde BV et al. Design, development and in vitro evaluation of bioadhesive dosage form for buccal route. Int J Pharm Res Dev 2010; 2(6):1-20. Address for Correspondence Bushetti S.S, HKES's College of Pharmacy, M R Medical College Campus, Sedam Road, Gulbarga- 585105 E-mail: sharansb69@rediffmail.com RJPS, Jul - Sep, 2011/ Vol 1/ Issue 2
A B S T R A C T RGUHS Journal of Pharmaceutical Sciences Chitosan Loaded Mucoadhesive Microspheres of Gliclazide: In vitro and In vivo Evaluation Senthil A*, Thakkar Hardik R, Ravikumar and Narayanaswamy V.B Department of pharmaceutics, Karavali College of Pharmacy, Mangalore, Karnataka. The objective of the present investigation was to design chitosan loaded mucoadhesive microspheres of gliclazide: in vitro and in vivo evaluation. Type 2 diabetes mellitus is a heterogeneous disease of polygenic origin and involves both defective insulin secretion and peripheral insulin resistance. Despite the availability of new agents for treatment of type 2 diabetes mellitus, oral sulfonylureas remain a cornerstone of therapy, because they are relatively inexpensive and are well tolerated. Since, the site of absorption of gliclazide is from stomach thus dosage forms that are retained in stomach by mucoadhesion; would increase absorption, improve drug efficiency and decrease dose requirements. Microspheres were prepared by simple emulsification phase separation technique. On the basis of the 2 preliminary trials 3 full factorial designs were employed, to study the effect of independent variable X polymer-to-drug and the stirring 1 speed X on dependent variables percentage mucoadhesion, drug entrapment efficiency and particle size. The optimized formulation 2 exhibited a high drug entrapment efficiency of 60%, swelling index 0.42, Percentage of mucoadhesive after 1 hour 62% and the drug release was also sustained for more than 10 hours. In vivo testing of the mucoadhesive microspheres to albino Wistar rats demonstrated significant hypoglycemic effect of gliclazide. Keywords: Mucoadhesive, Gliclazide, Chitosan, Glutaraldehyde. INTRODUCTION A primary object of using mucoadhesive formulations orally would be to achieve a substantial increase in length of stay of the drug in the GI tract. Stability problem in the intestinal fluid can be overcome. Therapeutic effect of drugs insoluble in the intestinal fluids can be improved. Recently, dosage forms that can precisely control the release rates and target drugs to a specific body site have made an enormous impact in the formulation and development of novel drug delivery 1-3 systems . Microspheres form an important part of such novel drug delivery systems. They have carried applications and are 1 prepared using assorted polymers . However, the success of these microspheres is limited owing to their short residence 5 time at the site of absorption . It would therefore be advantageous to have means for providing an intimate contact 6-9 of the drug delivery system with the absorbing membranes . Bioadhesive microspheres have advantages such as efficient absorption and enhanced bioavailability of drugs owing to a high surface-to-volume ratio a much more intimate contact with the mucus layer and specific targeting of drugs to the 10-13 absorption site . Gliclazide, a second generation sulphonylurea derivative and is preferred in therapy because of its selective inhibitory activity towards pancreatic K+ ATP RGUHS Journal of Pharmaceutical Sciences Received: 15/7/2011, Modified: 1/8/2011, Accepted: 12/8/2011 163 Original Research Article channels, antioxidant property, low incidence of producing severe hypoglycemia and other haemobiological effects. The daily dose, which is given in two fractions, is generally between 40 and 80 mg at the beginning of treatment, but the dose can be increased also at severe conditions. Gliclazide is well absorbed from GIT, approximately 80% is absorbed. One dose of gliclazide has a half-life less than 10 hours with the peak absorbance occurring at about 4-6 hours. Like most sulphonylureas, gliclazide binds primarily to plasma albumin (85-99%), allowing it to be distributed uniformly throughout 18-21 the body . Thus, an attempt was made in this investigation to use chitosan as a natural mucoadhesive polymer and prepare microspheres. The microspheres were characterized by in vitro and in vivo tests, and factorial design was used to optimize the variables. MATERIALS AND METHOD Gliclazide was obtained as gift sample from Aurobindo pharmaceuticals, Hyderabad, India. Chitosan (Purified, Viscosity grade 50) was obtained from Fourt's India Limited, Chennai. Dioctyl sodium sulfosuccinate, Heavy and Light liquid paraffin, Glutaraldehyde and Petroleum ether (80:20) was procured from Will son Lab, Mumbai. Preparation of Microspheres Microspheres were prepared by simple emulsification phase separation technique. The different volume of cross-linking agent glutaraldehyde was used as per method described in RJPS, Jul - Sep, 2011/ Vol 1/ Issue 2
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