Drug-induced hierarchical self-assembly of poly(amino acid)for efficient intracellular drug delivery  

作　　者：Zifen Li Yanxue Yang Chuan Peng Hang Liu Rui Yang Yi Zheng Lulu Cai Hong Tan Qiang Fu Mingming Ding 

机构地区：[1]College of Polymer Science and Engineering,State Key Laboratory of Polymer Materials Engineering,Sichuan University,Chengdu 610065,China [2]Personalized Drug Therapy Key Laboratory of Sichuan Province,Department of Pharmacy,Sichuan Provincial People's Hospital,School of Medicine,University of Electronic Science and Technology of China,Chengdu 610072,China

出　　处：《Chinese Chemical Letters》2021年第4期1563-1566,共4页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(Nos.51873118,21474064,52022062);the KeyResearch and Development Program of Science and Technology Department of Sichuan Province(No.2019YFS0514);Science and Technology Project of Chengdu(No.2019-YF05-00784-SN);the Project of State Key Laboratory of Polymer Materials Engineering(No.sklpme2020-2-03);the Fundamental Research Funds for Central Universities。

摘　　要：As a potent anticancer drug,gambogic acid(GA)suffers from its poor water solubility and low chemical stability and shows a limited clinical outcome.To address this problem,we report here a simple and effective strategy to immobilize and deliver GA using a reducible diblock poly(amino acid)as a model.The electrostatic interaction between GA and polymer enables a high drug loading content up to 53.6%.Moreover,the drug complexation induces a micelle-to-vesicle transformation,combined with a conformation tra nsition from random coil to a-helix.The hierarchically assembled drug nanocomplexes can serve as a smart carrier for efficient cell internalization and triggered release of multiple drugs under intracellular acidic and reductive conditions,resulting in a synergistic antitumor efficacy in vitro.This work provides a new insight into the drug-carrier interaction and a facile nanoplatform for drug delivery applications.

关 键 词：Poly(amino acid)s Electrostatic complexation Gambogic acid Hierarchical self-assembly Secondary conformation 

分 类 号：TB383.1[一般工业技术—材料科学与工程] TQ460.4[化学工程—制药化工]