ANTI-TUMOR DRUG DELIVERY OF A pH-SENSITIVE POLY(ASPARTIC ACID)-CONTAINING BLOCK COPOLYMER

YU Shufang; WANG Zheng; WU Guolin; WANG Yinong; GAO Hui; MA Jianbiao

doi:10.3724/SP.J.1105.2012.11222

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ANTI-TUMOR DRUG DELIVERY OF A pH-SENSITIVE POLY(ASPARTIC ACID)-CONTAINING BLOCK COPOLYMER

Research Article | 更新时间：2021-03-19

- ANTI-TUMOR DRUG DELIVERY OF A pH-SENSITIVE POLY(ASPARTIC ACID)-CONTAINING BLOCK COPOLYMER
- Acta Polymerica Sinica Issue 4, Pages: 427-432(2012)
- 作者机构：
  
  1. 功能高分子材料教育部重点实验室南开大学高分子化学研究所,天津,300071
  2. 天津理工大学化学化工学院天津 300191>
- 作者简介：
- 基金信息：
- DOI：10.3724/SP.J.1105.2012.11222
  CLC：
- Published：20 April 2012，
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YU Shufang, WANG Zheng, WU Guolin, WANG Yinong, GAO Hui, MA Jianbiao. ANTI-TUMOR DRUG DELIVERY OF A pH-SENSITIVE POLY(ASPARTIC ACID)-CONTAINING BLOCK COPOLYMER. [J]. Acta Polymerica Sinica (4):427-432(2012)
DOI：

YU Shufang, WANG Zheng, WU Guolin, WANG Yinong, GAO Hui, MA Jianbiao. ANTI-TUMOR DRUG DELIVERY OF A pH-SENSITIVE POLY(ASPARTIC ACID)-CONTAINING BLOCK COPOLYMER. [J]. Acta Polymerica Sinica (4):427-432(2012) DOI： 10.3724/SP.J.1105.2012.11222.

摘要

通过大分子引发剂-氨基--甲氧基聚乙二醇引发N-羧基--氨基环内酸酐开环聚合和水合肼侧基改性

制备了一系列聚乙二醇-聚氨基酸类三嵌段共聚物.其中聚氨基酸链段包括具有酰肼基的聚天冬氨酸衍生物(PAHy)

以及疏水性的聚丙氨酸链段.引入具有pH响应性的腙键键合阿霉素

利用键合阿霉素与游离阿霉素之间的-叠合作用

在聚合物自组装形成胶束过程中通过化学键合+物理包埋的方式充分负载药物.该胶束以聚丙氨酸链段为核心

以PEG链段为冠层

以PAHy链段为包裹药物的壳层.载药胶束的粒径在170 nm左右.研究不同pH值条件下载药胶束的药物释放能力

随环境pH值的降低药物的释放速率显著增加.

Abstract

A novel biodegradable ABC type triblock copolymer was synthesized by N-carboxyl anhydride ring-opening polymerization.Triblock copolymer mPEG-poly(asparthyl hydrazide)-PLAla (mPEG-PAHy-PLAla) was synthesized by hydrazine aminolysis.DOX was conjugated to the polymer through a pH-sensitive hydrazone bond.High drug-loaded polymeric micelles were obtained via the - interaction between conjugated and free DOX molecules.FTIR

dynamic light scattering

UV and TEM were used in the characterization and measurements.It was found that this polymer/drug complex could form nano-scaled core-shell-corona trilayer particles in aqueous solution.PLAla

PAHy(DOX) and PEG blocks served as the hydrophobic core

pH-sensitive shell and hydrophilic corona

respectively.The drug release experiments displayed a pH-dependent behavior that DOX release rate increased significantly as the environmental pH value dropped from physiologically 7.4 to acidic values resulted from the cleavage of hydrazone bonds and the increasing of hydrophilicity of PAHy segements at lower pH values.This new platform represents a promising candidate in the formulation of targeted drug delivery systems to the low pH tumor tissues.

关键词

聚天冬氨酸腙键阿霉素pH-响应性

Keywords

Poly(aspartic acid)Hydrazone bondDOXpH-responsive

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Related Institution

Key Laboratory of Functional Polymer Materials (Ministry of Education), Institute of Polymer Chemistry, Nankai University

Beijing Institute of Pharmacology and Toxicology

Department of Polymer Science and Engneering, Zhejiang University

MOE Key Laboratory of Macromolecular Synthesis and Functionalization

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