Self-microemulsifying drug delivery system containing calebin-A enhanced treatment of colorectal cancer

• Main Authors: Lynn Perera, 林貝拉
• Other Authors: Min-Hsiung Pan
• Format: Others
• Language: en_US
• Published: 2017
• Online Access: http://ndltd.ncl.edu.tw/handle/yuf87f

碩士 === 國立臺灣大學 === 食品科技研究所 === 105 === Colorectal cancer is the third most commonly diagnosed cancer and the third leading cause of cancer death worldwide. Recent studies have shown that calebin-A, a phytochemical from the rhizomes of turmeric (Curcuma longa), has anti-cancer, anti-inflammation, and anti-oxidation potential. However due to its hydrophobic property, the therapeutic potentials of calebin-A is greatly limited in the in vivo models by its poor solubility. There are various drug delivery systems that have been reported to be successful in delivering hydrophobic agents into an aqueous environment. The aim of this study is to use self-microemulsifying drug delivery system (SMEDDS) to ameliorate the low bioavailability of calebin-A for further investigation of its anti-tumor potential in human colon carcinoma cell line (HCT 116) xenografts nude mice. In this study, SMEDDS containing polyoxyethylene (20) sorbitan monooleate (Tween 80), polyethylene glycol 400 (PEG 400), and medium-chain triglyceride (MCT) was fabricated for oral administration of calebin-A. The results showed that SMEDDS containing calebin-A had droplets size of 28.7 nm and zeta potential of -9.7 mV. Based on in vitro lipid digestion study, SMEDDS containing calebin-A produced 7.5-fold more solubilized calebin-A than calebin-A MCT suspension. The results from HCT 116 xenografts nude mice suggested that 50 mg/kg calebin-A SMEDDS could decrease tumor growth rate through upregulation of phosphorylated check point kinase, p53, p21 protein expressions; decreased cdc25A, cyclin B1, cdc2, cyclin A protein levels; resulting in S phase and G2/M phase arrest. According to the results from this study, SMEDDS could improve the efficacy of calebin-A for the treatment of colorectal cancer.