Chitosan coated Ca–alginate microparticles loaded with budesonide for delivery to the inflamed colonic mucosa

Abstract

Using a novel one-step spray-drying process uncoated and Eudragit S 100 coated chitosan-Ca-alginate microparticles efficiently loaded with budesonide (BDS), with bioadhesive and controlled release properties in GIT, were prepared. Microparticles were spherical with mean particle size of 4.05-5.36 microm, narrow unimodal distribution and positive surface charge. A greater extent of calcium chloride limited the swelling ratio of beads, while swelling behaviour of coated beads was mainly determined by properties of enteric coating. Comparing the release profiles of formulations, under different pH conditions, influence of polymer properties and concentration of cross-linker on the rate and extent of drug release was evident. Coating has successfully sustained release of BDS in buffers at pH 2.0 and 6.8, while providing potential for efficient release of BDS at pH 7.4. Release data kinetics indicated influence of erosion and biodegradation of polymer matrix on drug release from microparticles. Prepared formulations were stable for 12 months period at controlled ambient conditions. In conclusion coated microparticles prepared by one-step spray-drying procedure could be suitable candidates for oral delivery of BDS with controlled release properties for local treatment of inflammatory bowel diseases.