基于聚己内酯和聚乙二醇的基于环糊精为中心的药物偶联两亲性 A(14)B(7) 嵌段星形共聚物的合成、自组装和载药能力。

Synthesis, self-assembly, and drug-loading capacity of well-defined cyclodextrin-centered drug-conjugated amphiphilic A(14)B(7) Miktoarm star copolymers based on poly(epsilon-caprolactone) and poly(ethylene glycol).

机构信息

MOE Key Laboratory of Macromolecule Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China.

出版信息

Biomacromolecules. 2010 Apr 12;11(4):934-43. doi: 10.1021/bm901371p.

DOI:10.1021/bm901371p

PMID:20225892

Abstract

Novel drug-conjugated amphiphilic A(14)B(7) miktoarm star copolymers composed of 14 poly(epsilon-caprolactone) (PCL) arms and 7 poly(ethylene glycol) (PEG) arms with beta-cyclodextrin (beta-CD) as core moiety were synthesized by the combination of controlled ring-opening polymerization (CROP) and "click" chemistry. (1)H NMR, FT-IR, and SEC-MALLS analyses confirmed the well-defined A(14)B(7) miktoarm star architecture. These amphiphilic miktoarm star copolymers could self-assemble into multimorphological aggregates in aqueous solution, which were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). Moreover, the drug-loading efficiency and drug-encapsulation efficiency of the drug-conjugated miktoarm star copolymers were higher than those of the corresponding non-drug-conjugated miktoarm star copolymers.

摘要

新型药物偶联两亲性 A(14)B(7) 星型嵌段共聚物由 14 个聚己内酯（PCL）臂和 7 个聚乙二醇（PEG）臂组成，以β-环糊精（β-CD）为核部分，通过控制开环聚合（CROP）和“点击”化学合成。（1）H NMR、FT-IR 和 SEC-MALLS 分析证实了具有明确结构的 A(14)B(7) 星型嵌段共聚物。这些两亲性星型嵌段共聚物在水溶液中可以自组装成多种形态的聚集体，这通过动态光散射（DLS）和透射电子显微镜（TEM）进行了表征。此外，药物偶联的星型嵌段共聚物的药物载药效率和药物包封效率均高于相应的非药物偶联的星型嵌段共聚物。