Budesonide is an anti-inflammatory
drug of choice for treatment of
ulcerative colitis which affects the rectum and a part of or the entire colon. Delivery of
budesonide specifically to the colon would increase the efficacy of the
drug and reduce the side-effects. The aim of this study was to develop an oral matrix system formulation for
budesonide to deliver the major part of the
drug to the colon for treatment of
ulcerative colitis that has not been reported before. Directly compressed matrix
tablets were prepared using different molecular weights of
dextran and three ratios of
drug-to-
polymer. The physical properties of the
tablets including weight variation, hardness, content uniformity, and release profile in HCl 0.1 N,
phosphate buffer pH 7.4 and 6.8 containing 4% rat caecal and colonic contents were studied. The efficacy of the desired formulation was also evaluated against
acetic acid-induced
colitis in rats. Physical properties of the
tablets were in the ranges recommended by official references. More than 10% of the
drug was released in HCl 0.1 N and pH 7.4, while a very drastic increase was observed after exposure to pH 6.8 containing rat caecal contents. The efficacy of the selected formulation against rat-induced
colitis was also increased in comparison to the non-targeted formulation of
budesonide. In conclusion, matrix
tablets with a 1:10
drug-to-
dextran ratio with high molecular weight could deliver the
drug specifically to the colon and are promising for treatment of
ulcerative colitis.