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.
Highlights
IntroductionColon cancer is a very lethal malignant tumor with an increased incidence rate in 40–50 y of age, associated with high morbidity and mortality worldwide [1, 2]
Colon cancer is considered much leading cause of deaths in the world
The results showed that stealth liposomes decrease capecitabine uptake in the RES-containing organs when compared with conventional liposomes
Summary
Colon cancer is a very lethal malignant tumor with an increased incidence rate in 40–50 y of age, associated with high morbidity and mortality worldwide [1, 2]. For colon cancer Chemotherapy, Radiotherapy, and surgery are the Clinical therapeutic strategies. Chemotherapeutic approaches often suffer from multidrug resistance, poor bioavailability, and high system toxicity, which may result in poor efficacy and significant adverse effects [5, 6]. To overcome these problems, different approaches have been attempted by giving “selective” delivery to the affected area. Taking the response to chemotherapy of cancer drug delivery into consideration, methods like nanoscale systems (liposomes, micelles and nanoparticles) is growing steadily [7]
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