A Smart Drug Delivery System from Charge-Conversion Polymer-Drug Conjugate for Enhancing Tumor Therapy and Tunable Drug Release

被引：22

作者：

Huang, Hailong ^{[1
]}

Li, Yapeng ^{[1
]}

Sa, Zongpeng ^{[1
]}

Sun, Yuan ^{[1
]}

Wang, Yuzhen ^{[1
]}

Wang, Jingyuan ^{[1
]}

机构：

[1] Jilin Univ, Alan G MacDiarmid Inst, Changchun 130012, Peoples R China

来源：

MACROMOLECULAR BIOSCIENCE | 2014年 / 14卷 / 04期

关键词：

amphiphiles; biomaterials; charge transfer; conjugated polymers; drug delivery systems; INTRACELLULAR RELEASE; PH; MICELLES; NANOPARTICLES;

D O I：

10.1002/mabi.201300337

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A smart drug delivery system is prepared by citraconylated polyaspartic acid (PASP) derivate-drug conjugate. The conjugate contains two pH-sensitive groups: citraconic amide and hydrazone linker. Citraconic amide group can enhance tumor therapy efficiency by the extracellular pH-sensitive charge-conversion property. Hydrazone linker between polymer and drug can cleave efficiently in the intracellular pH environment. The resulting conjugate shows dual-pH sensitive properties: extracellular pH-triggered enhanced tumor targeting and intracellular pH-triggered drug release. The results of physicochemical properties, intracellular location, and cytotoxicity of conjugate micelles demonstrate that this novel smart drug delivery system can enhance intracellular delivery of drug at a low pH and then release drug rapidly.

引用

页码：485 / 490

页数：6

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