Abstract

OPTIMIZED DEVELOPMENT AND EVALUATION OF MICROBIALLY TRIGGERED BASED ORNIDAZOLE MICROSPHERES FOR COLON TARGETING

Verma Surender*, Bhalla Gaurav and Goyal Gourav

Abstract

The objective of the present study is to formulate and evaluate microbially triggered based colon targeted microspheres using two carriers tragacanth gum and inulin individually which would protect the release of the drug in the physiological environment of the stomach and small intestine and release the drug in the colon providing local action for the treatment of the amoebiasis. Ornidazole is a 5- nitroimidazole derivative and is used in the treatment of susceptible protozoal infections and also in anaerobic bacterial infections mainly for amoebiasis, giardiasis, vaginitis and duodenal ulcers. It is more effective against amoebiasis than metronidazole. The research involves the formulation, optimization and evaluation of colon targeting microspheres. The colon targeting microspheres were successfully developed by Ionotropic gelation technique, using tragacanth gum and inulin polymers in various proportions. Further, the prepared microspheres were characterized for particle size, morphology, entrapment efficiency, in vitro drug release, release kinetics, compatibility studies (DSC) and stability studies, Best formulations were selected from both type of microspheres as ORT4 and ORI4 based on amount of tragacanth gum or inulin, sodium alginate and glutaraldehyde affecting % CDR and % EE. Drug release kinetics of ORT4 as well as ORI4 system best corresponds to koresmeyer peppas kinetics in absence of rat caecal content while in presence of rat caecal contents, ORT4 followed zero order kinetics and ORI4 still followed koresmeyer peppas kinetics and the mechanism of drug release of all batches obtained from koresmeyer peppas kinetics corresponding to non Fickian diffusion showing Super Case II Transport mechanism.

Keywords: Amoebiasis, Colon targeted microspheres, Ornidazole, Koresmeyer peppas kinetics.