Preparation of 5-florouracil microspheres for colonic drug delivery

5-Fluorouracil is widely used anticancer drug,which are effective during the S-phase of cellcycle. Since It has poor bioavailability so targeting of 5-Fluorouracil at site of action is of great beneficial. Attempt has been made to develop a stable microparticulate formulation of 5-Fluorouracil to be administered orally to target colon. Here, chitosan was chosen as polymer. Chitosan microspheres were coated with eudragit s-100.The Cross linked chitosan microspheres containing 5-Fluorouracil were prepared by emulsification method using glutaraldehyde as crosslinking agent and characterized for %Yield, ParticleSize, Surface properties and Morphology, Entrapment Efficiency and DSC. InVitro release studies of coated and uncoated chitosan microspheres was performed in pH progression medium at 37 ± 0.5 0C ,in simulated gastric fluid, simulated intestinal fluid. As compared to chitosan microspheres, coated microspheres(1: 5 ) showed about 7.88% drug release after 6 hours and rest of drug releases upto 24 hours. When the core:coat ratio is 1: 10 , release does not occur. Hence, we can conclude that eudragit coated chitosan microspheres prevents drug release in stomach, small intestine, targets colon only; thus avoiding systemic side-effects associated with 5-Fluorouracil.