In situ gelling oral for delivery system of anticancer drug

• Main Authors: Ching-yu Hsu, 徐慶裕
• Other Authors: none
• Format: Others
• Language: zh-TW
• Published: 2011
• Online Access: http://ndltd.ncl.edu.tw/handle/27661687214974152802

碩士 === 國立臺南大學 === 生物科技學系碩士班 === 99 === P is a temperature sensitive polymer, and A is a pH-sensitive polymer. In this study, we combined one anticancer drug, epirubicin with two polymers P and A in different ratios to design an oral in situ gelling formulation for colon cancer therapy. The physicochemical properties, in vitro drug release and in vivo therapeutic efficacy of epirubicin in three P/A formulations were evaluated. Our results demonstrate that the formulation of hydrogel composed of P14%/A 0.75% showed the fastest gelling rate and shortest gelling time among three formulations. Consistently, this formulation also exhibited the highest degree of swelling. The lyophilized preparation of P14%/A 0.75 % hydrogel was found to exhibit wrinkled and sponge-like structure, as shown by scanning electron microscopic images. In addition, the formulation of P14%/A 0.75 % was found to show the sustained release profile and demonstrate the highest percentage of drug release. Epirubicin in this formulation was also found to demonstrate a significant inhibition on CT-26 mouse colon cancer cells in a dose-dependent manner. In in vivo CT-26 bearing Balb/c bearing mice, oral epirubicin formulated in P14%/A 0.75 % hydrogel demonstrated significant improvements in tumor growth inhibition and weight loss. This study highlights the advantages of using temperature and pH-sensitive hydrogel of P/A to deliver epirubicin. These advantages include short gelling time, strong gel strength, high degree of swelling, sustained release effect on epirubicin, and significant in vivo antitumor efficacy. This formulation has a potential to be developed into a long-acting dosage form for oral drugs in the future.