Formulation and Evaluation of Capecitabine Microspheres for Colorectal Cancer

Abstract

The present study aimed to formulate and evaluate Capecitabine microspheres for colorectal cancer, reduce dosing frequency, and improve patient compliance. Microspheres were prepared by emulsion solvent evaporation using polymers like ethyl cellulose (E.C.) and HPMC K-I00 in different ratios. The prepared microspheres were evaluated for flaw properties, percentage yield, drug entrapment efficiency, and in vitro dissolution studies. Results showed that as the concentration of polymer ratio increases, it affects the particle size, percentage yield, and drug release from the microspheres. The percentage yield of F6 microspheres was up to 95.13%. The release study was done with simulated intestinal fluid (SIF - pH 7.4) for 24 hours. It showed that the drug was protected from being released in the physiological environment of the intestine and efficiently released in the colon (95.85%). The optimized formulation F6 exhibited the drug release in a sustained manner arid following zero order, non-Fickian diffusion mechanism. An accelerated stability study was carried out for the optimized formulation. The results showed no significant changes in percentage drug entrapment efficiency, particle size, and in vitro controlled release of Capecitabine. The surface morphology analysis formulation F6 showed a spherical structure with smooth surface morphology. The prepared microspheres are promising drug delivery for sustained oral administration to target the colon and provide a better kinetic profile with improved bioavailability.