Biopharmaceutics and Biologic Drugs

Biography

Biography: Kala D

Abstract

A number of colonic diseases could be treated more efficiently by delivering the drug locally in the colon. For the management of active, mild to moderate ulcerative colitis, an oral preparation of topical corticosteroid with reduced systemic exposure is preferred. Budesonide, a synthetic non-halogenated potent corticosteroid with high topical anti-inflammatory effect was selected as model drug.The polymer selected; chitosan is biocompatible, non-toxic and can be biodegraded by the microflora present in the human colon. Budesonide microspheres were prepared by ionotropic gelation process and were coated with eudragit S-100 polymer to prevent drug release in the stomach. The effect of concentration of polymer chitosan and cross linking agent TPP on drug entrapment efficiency, particle size and release profile were investigated. To assess the biodegradability of chitosan by the colonic microorganism, in vitro release studies in presence of rat caecal content were also performed. In vivo therapeutic experiment was done using TNBS induced colitis in rats. The therapeutic effect was assessed by determining the damage score, clinical activity score, C/B weight ratio and MPO activity measurement. The study showed that oral administration of budesonide microspheres exerted an affirmative impact on the colonic ulcer healing by decreasing the area of ulceration, reducing the mass of colon by improving the symptoms of colitis. The designed system was highly promising for potential targeting of budesonide to the colonic region with inconsiderable drug release under simulated gastric condition.