Self-assembled micelles of novel amphiphilic copolymer cholesterol-coupled F68 containing cabazitaxel as a drug delivery system

• DOI: 10.2147/ijn.s61220
• Publication Date: 2014-05-13T02:43:46Z
• Authors: Yihui Deng; Yanzhi Song; Qingjing Tian; Zhenjun Huang; Di Fan; Zhennan She; Xinrong Liu; Xiaobo Cheng; Bin Yu
• Keywords: Cabazitaxel; Nanocarriers

Abstract: Despite being one of the most promising amphiphilic block copolymers, use Pluronic F68 in drug delivery is limited due to its high critical micelle concentration (CMC). In this study, we developed a novel derivative, cholesterol-coupled (F68-CHMC). This new derivative has CMC 10 µg/mL, which 400-fold lower than that F68. The drug-loading capacity F68-CHMC was investigated by encapsulating cabazitaxel, antitumor drug. Drug-loaded micelles were fabricated self-assembly method with simple dilution. optimum particle size 17.5±2.1 nm, an entrapment efficiency 98.1% and loading 3.16%. vitro release studies demonstrated cabazitaxel-loaded had delayed sustained-release properties. A cytotoxicity assay S180 cells showed blank noncytotoxic cell viability nearly 100%, even at 1,000 µg/mL. IC 50 revealed more cytotoxic Tween 80-based cabazitaxel solution free cabazitaxel. vivo activity against also indicated better tumor inhibition (79.2%) 80 (56.2%, P <0.05). Based on these results, conclude copolymer may be potential nanocarrier improve solubility biological other hydrophobic drugs. Keywords: F68, cholesterol, synthesis, micelles, cancer therapy