• DEVELOPMENT AND CHARACTERIZATION OF EUDRAGIT-S100 COATED STARCH MICROSPHERES OF 5-FLUOROURACIL FOR COLON TARGETING

Abstract

An objective of the present investigation was to prepare and evaluate Eudragit-S100 coated starch microspheres for colon specific delivery of 5-fluorouracil (FU). Starch microspheres were prepared by emulsion dehydration method using different ratios of FU and starch (0.5 to 2.0 w/v), stirring speeds (300-1200 rpm) and emulsifier concentrations (0.5%-2% v/v). The yield of preparation and encapsulation efficiency was high for all starch microspheres. Microspheres prepared by using drug: polymer ratio 40:100 w/w, stirring speed 600 rpm, and 1.5 % w/v concentration of emulsifying agent (span 80) were selected as an optimized formulation. Eudragit-S100 coating of starch microspheres was performed dip coating method using core : coat ratio (1:10). Starch microspheres and Eudragit-S100 coated starch microspheres were evaluated for surface morphology, particle size and size distribution, swellability, percentage drug entrapment, and in vitro drug release in simulated gastrointestinal fluids (SGF). The in vitro drug release study of optimized formulation was also performed in simulated colonic fluid in the presence of 4 % rat cecal content. Organ distribution study in albino rats was performed to establish the targeting potential of optimized formulation in the colon. The release profile of 5-FU from eudragit-S100 coated starch microspheres was pH dependent. In acidic medium, the release rate was much slower however the drug was released quickly at pH 7.4. It is concluded from the present investigation that Eudragit-S100 coated starch microspheres are promising controlled release carriers for colon-targeted delivery of 5-FU.