Hypoxia-activatable nano-prodrug for fluorescently tracking drug release in mice  

作　　者：Haidong Li Qichao Yao Zhongji Pu Jeewon Chung Haoying Ge Chao Shi Ning Xu Feng Xu Wen Sun Jianjun Du Jiangli Fan Jingyun Wang Juyoung Yoon Xiaojun Peng 

机构地区：[1]State Key Laboratory of Fine Chemicals,Dalian University of Technology,Dalian 116024,China [2]Department of Chemistry and Nanoscience,Ewha Womans University,Seoul 03760,Korea [3]Ningbo Institute of Dalian University of Technology,Ningbo 315016,China [4]School of Bioengineering,Dalian University of Technology,Dalian 116024,China

出　　处：《Science China Chemistry》2021年第3期499-508,共10页中国科学（化学英文版）

基　　金：supported by the National Creative Research Initiative programs of the National Research Foundation of Korea(NRF),the Korean Government(MSIP)(2012R1A3A2048814);the National Natural Science Foundation of China(21421005,21808028);the Natural Science Foundation of Liaoning United Fund(U1608222,U1908202)。

摘　　要：Chemotherapy is one of the commonly used methods to treat various types of cancers in clinic by virtue of its high efficiency and universality. However, strong side effects and low concentration of conventional drugs at the tumor site have always been important factors that plague the chemotherapy effects of patients, further precluding their practical applications. Thereof, to solve the above dilemma, by integration of anticancer drug(nitrogen mustard, NM) into an NIR fluorophore(a dicyanoisophorone derivative), an intelligent prodrug NIR-NM was developed via molecular engineering strategy. Prodrug NIR-NM stimulated in hypoxia condition exhibits significantly higher toxicity to cancer cells than normal cells, essentially reducing the collateral damage to healthy cells and tissues of nitrogen mustard. More importantly, the nanoparticle prodrug FA-lip@NIR-NM showed the advantages of the high accumulation of drug at tumor site and long-circulation capacity in vivo, which endowed it the ability to track the release of the active chemotherapeutic drug and further treat solid tumors.

关 键 词：NIR fluorescent probe activatable HYPOXIA PRODRUG imaging 

分 类 号：TQ460.1[化学工程—制药化工]