FORMULATION AND EVALUATION OF COLON-TARGETED TEGAFUR MICROSPHERES

Document Type : Original Article

Authors

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt

Abstract

Tegafur (TGF) is an antineoplastic drug which used for treatment of neoplasm of gastro-intestinal tract including colon cancer. Cellulose acetate butyrate microspheres containing the drug were prepared by using the emulsion-solvent evaporation technique. The microspheres were spherical and free flowing. The yield was greater than 97% and more than 95% of the drug was encapsulated. The effect of microsphere size and pH of the dissolution medium on the drug release was investigated. Sustained release profiles of TGF from TGF-CAB microspheres were observed. In all cases the drug release followed Higuchi diffusion model. Microspheres of smaller size gave a relatively higher dissolution rate of the drug. The drug release was slower in acidic medium (pH 1.2) suggesting that using CAB microspheres would be of value for controlling the drug release and potential colonic-targeting of the drug.