DEVELOPMENT AND CHARACTERIZATION OF PEGYLATED CAPECITABINE LIPOSOMAL FORMULATIONS WITH ANTICANCER ACTIVITY TOWARDS COLON CANCER

Abstract

Objective: Capecitabine is widely used in colorectal cancer treatment and has first-pass metabolism problem. Despite of its promising anticancer potential, capecitabine has not been used due to its poor solubility in water. The purpose of this study was to develop colon targeting capecitabine loaded stealth liposomes, which is a promising technique to avoid first-pass metabolism to achieve the desired bioavailability profile, increased water solubility and sustained release. Methods: Thin film hydration method was used to prepare capecitabine stealth liposomes. Prepared liposomes were characterized for drug release kinetics, stability studies, cell viability studies to determine the cytotoxic effect and in vivo studies in mice bearing colon carcinoma for evaluation of antitumor potential. Results: In vitro releases of liposomes were best fitted in the Higuchi matrix kinetic model with an n value from 0.868-0.964, indicating non-fickian release diffusion. Stability data indicated that liposomes were stable for at least 06 mo at 5±3 ° C. inhibiting activity was increased and with a Significant improvement in AUC, MRT and t1/2 observed as 29.65±5.08, µg h/ml for Stealth liposomes compared with the pure capecitabine and the conventional liposomes. Conclusion: Results suggested that Capecitabine-loaded stealth liposomes can be an effective delivery system for targeting colon cancer.