Carrier-free prodrug nanoparticles based on dasatinib and cisplatin for efficient antitumor in vivo  

作　　者：Lu Yang Jiaxi Xu Zheng Xie Faquan Song Xin Wang Rupei Tang 

机构地区：[1]Engineering Research Center for Biomedical Materials,Anhui Key Laboratory of Modern Bio-manufacturing,School of Life Science,Anhui University,Hefei 230601,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2021年第6期762-771,共10页亚洲药物制剂科学（英文）

基　　金：supported by the National Natural Science Foundation of China(No.51803001 and 51503001);the Natural Science Foundation of Anhui Province(No.2008085ME136 and 2008085QE210);the Research Foundation of Education Department of Anhui Province of China(No.KJ2018ZD003,KJ2018A0006 and KJ2019A0015);the Academic and Technology Introduction Project of Anhui University(AU02303203)grant.

摘　　要：Carrier-free drug self-delivery systems consisting of amphiphilic drug-drug conjugate(ADDC)with well-defined structure and nanoscale features have drawn much attention in tumor drug delivery.Herein,we report a simple and effective strategy to prepare ADDC using derivatives of cisplatin(CP)and dasatinib(DAS),which further selfassembled to form reduction-responsive nanoparticles(CP-DDA NPs).DAS was modified with succinic anhydride and then connected with CP derivative by ester bonds.The size,micromorphology and in vitro drug release of CP-DDA NPs were characterized.The biocompatibility and bioactivity of these carrier-free nanoparticles were then investigated by HepG2 cells and H22-tumor bearing mice.In vitro and in vivo experiments proved that CPDDA NPs had excellent anti-tumor activity and significantly reduced toxicities.This study provides a new strategy to design the carrier-free nanomedicine composed of CP and DAS for synergistic tumor treatment.

关 键 词：PRODRUG NANOPARTICLE DASATINIB CISPLATIN 

分 类 号：R943[医药卫生—药剂学]