Microspheres For Colonic Delivery Of Betamethasone In Inflammatory Bowel Disease

Abstract

For treating colonic diseases, conventional oral drug delivery systems are not effective, as they fail to reach the appropriate site of action. Thus, there is a need to develop effective and safe therapy for the treatment of colonic disorders. The aim of the present study was to design a colon-specific delivery system for an anti-inflammatory synthetic glucorticoid, Betamethasone, with minimal degradation and optimum delivery of the drug with relatively higher local concentration, which may provide more effective therapy for inflammatory bowel disease including Crohn disease and ulcerative colitis. A multiparticulate system having pH sensitive property and specific enzyme biodegradability for colon targeted delivery of Betamethasone was developed. Tamarind gum microspheres were prepared by emulsion dehydration technique using different ratio of polymer. These microspheres were coated with Eudragit S-100 by oil in oil solvent evaporation method using core : coat ration (5:1) . Tamarind gum microspheres and Eudragit coated tamarind gum microspheres were evaluated for surface morphology, particle size and size distribution, percentage drug entrapment, surface accumulation studies, in vitro drug release in simulated gastrointestinal fluids. The prepared microspheres were spherical in shape in the size range of 53 μm to 190 μm, the encapsulation efficiency was in range of 64-80 % depending upon the concentration of gum. The drug release was about 10-12% in first four hours of study gradually rises in 5th hour and 80% drug release occurs in 8-10 hr thus showing desirable drug release in the colonic simulated environment.