Synthesis and characterization of multi-functional linear-dendritic block copolymer for intracellular delivery of antitumor drugs

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• 作者：Hongzhi Qiao ; Juan Li ; Yang Wang ; Qineng Ping ; Guangji Wang ; Xiaochen Gu
• 关键词：Linear-dendritic block copolymers ; pH-sensitive ; Specific drug targeting ; Cellular uptake ; Pharmacokinetics
• 刊名：International Journal of Pharmaceutics
• 出版年：2013
• 出版时间：16 August, 2013
• 年：2013
• 卷：452
• 期：1-2
• 页码：363-373
• 全文大小：2756 K

文摘

A novel amphiphilic linear-dendritic block copolymer, semi-polyamidoamine-b-poly(d,l-lactic acid) (PALA) was synthesized and evaluated for its potential as a drug delivery system in this study. PALA was self-assembled in aqueous solution to form nanomicelles with low critical micelle concentration; antitumor drug docetaxel (DTX) was successfully encapsulated into micelles. The prepared micelles demonstrated pH-induced charge conversion and dimension changes. In vitro drug release suggested susceptibility of DTX-loaded micelles to acidic microenvironment. Hemolysis and cytotoxicity testing also indicated in vitro biocompatibility of PALA. Pharmacokinetic study in rats proved that DTX-loaded PALA micelles enhanced the AUC of DTX and prolonged drug clearance in comparison to conventional DTX injection (Taxotere^?). It was concluded that self-assembled micelles from linear-dendritic block copolymer PALA demonstrated potential for intracellular delivery of anticancer molecules, and that its safety and efficacy in chemotherapy should be further studied.