pH-responsive release of paclitaxel from hydrazone-containing biodegradable micelles

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• 作者：Peilan Qi ; Yongqiang Bu ; Jing Xu ; Benkai Qin ; Shujuan Luan…
• 关键词：Biodegradable copolymer ; pH ; sensitive ; Polymeric micelle ; Controlled release
• 刊名：Colloid and Polymer Science
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：295
• 期：1
• 页码：1-12
• 全文大小：
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Polymer Sciences; Soft and Granular Matter, Complex Fluids and Microfluidics; Characterization and Evaluation of Materials; Physical Chemistry; Food Science; Nanotechnology and Microengineering;
• 出版者：Springer Berlin Heidelberg
• ISSN：1435-1536
• 卷排序：295

文摘

Many tumor cells have acidic microenvironment that can be exploited for the design of pH-responsive drug delivery systems. In this work, well-defined pH-sensitive and biodegradable polymeric micelles were prepared and evaluate as carrier of paclitaxel (PTX). A diblock copolymer constituting of a poly(ethylene glycol) (PEG) and a polycaprolactone (PCL) segment linked by a pH-sensitive hydrazone bond (Hyd), which was denoted as mPEG-Hyd-PCL, was synthesized. The copolymer was assembled to micelles with mean diameters about 100 nm. The mean diameters and size distribution of the hydrazone-containing micelles increased obviously in mildly acidic environments while kept unchanged in the neutral. No significant change in size was found on polymeric micelles without hydrazone (mPEG-PCL). PTX was loaded into micelles, and the anticancer drug released from mPEG-Hyd-PCL micelles was promoted by the increased acidity. In vitro cytotoxicity study showed that the PTX-loaded mPEG-Hyd-PCL micelles exhibited significantly enhanced cytotoxicity against HepG2 cells compared to the non-sensitive mPEG-PCL micelles. These results suggest that hydrazone-containing copolymer micelles with pH sensitivity and biodegradability show excellent potential as carriers of anticancer drugs.