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Research Article
Development and Evaluation of Biodegradable Chitosan Microspheres Loaded with Ranitidine and Cross Linked with Glutaraldehyde

S. Ramachandran, G. Thirumurugan and M.D. Dhanaraju

American Journal of Drug Discovery and Development, 2011, 1(2), 105-120.

Abstract

The present study aimed at the formulation of biodegradable chitosan microspheres loaded with ranitidine to overcome the poor bioavailability and frequent dose administration. Chitosan microsphere was prepared by simple emulsification technique by glutaraldehyde crosslinking. Various process variable and formulation variable such as speed of emulsification, cross linking time, drug/polymer ratio, volume of cross linking agent and volume of surfactant were optimized. Formulated microspheres were characterized for its entrapment efficiency, drug loading, in vitro drug release, Kinetics of drug release, surface morphology, particle size analysis, Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) thermal analysis. The characterized ranitidine microsphere formulations were investigated for in vivo gastric and duodenal antiulcer activity. The characterization of the fabricated microspheres showed smooth surface with narrow particle size distribution and entrapment efficiency upto 84%. The prepared microspheres exhibited a controlled drug release of 74% over a period of 24 h with initial burst release of 35% in the first 2 h. The FTIR and DSC reports showed that there was no potential drug interaction between the drug and polymer. In vivo studies shows that gastric volume, pH, total acidity and ulcer index of formulated ranitidine microspheres were significantly reduced as 2.67 mL, 5.59, 110 mEq L-1 and 1.74, respectively and also there is no evidence of extra tissue damage as seen in the biopsy report. From the data obtained it can be concluded that the chitosan microspheres could be considered as a potential biodegradable carrier for controlled drug delivery of ranitidine.

ASCI-ID: 2817-8

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