N-Boc-Histidine-Capped PLGA-PEG-PLGA as a Smart Polymer for Drug Delivery Sensitive to Tumor Extracellular pH

被引：73

作者：

Chang, Guangtao ^{[1
]}

Li, Chong ^{[2
]}

Lu, Weiyue ^{[2
]}

Ding, Jiandong ^{[1
]}

机构：

[1] Fudan Univ, Key Lab Mol Engn Polymers Minist Educ, Dept Macromol Sci, Adv Mat Lab, Shanghai 200433, Peoples R China

[2] Fudan Univ, Dept Pharmaceut, Sch Pharm, Shanghai 201203, Peoples R China

来源：

MACROMOLECULAR BIOSCIENCE | 2010年 / 10卷 / 10期

关键词：

block copolymers; drug delivery systems; micelles; POROUS POLY(D; L-LACTIDE-CO-GLYCOLIDE); SCAFFOLDS; SCORPION-LIKE MACROMOLECULES; BLOCK-COPOLYMER MICELLES; IN-VITRO DEGRADATION; TRIBLOCK COPOLYMERS; DOXORUBICIN; RELEASE; NANOPARTICLES; HYDROGELS; SOL;

D O I：

10.1002/mabi.201000117

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 pH-sensitive polymer was synthesized by introducing the N-Boc-histidine to the ends of a PLGA-PEG-PLGA block copolymer. The synthesized polymer was confirmed to be biodegradable and biocompatible, well dissolved in water and forming micelles above the CMC. DOX was employed as a model anticancer drug. In vitro drug release from micelles of N-Boc-histidine-capped PLGA-PEG-PLGA exhibited significant difference between pH = 6.2 and pH = 7.4, whereas DOX release from micelles composed of un-capped virgin polymers was not significantly sensitive to medium pH. Uptake of DOX from micelles of the new polymer into MDA-MB-435 solid tumor cells was also observed, and pH sensitivity was confirmed. Hence, the N-Boc-histidine capped PLGA-PEG-PLGA might be a promising material for tumor targeting.

引用

页码：1248 / 1256

页数：9

共 49 条

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