文献类型：期刊文献

英文题名：Nanomized tumor-microenvironment-active NIR fluorescent prodrug for ensuring synchronous occurrences of drug release and fluorescence tracing

作者：Li, Qiang[1,2];Cao, Jun[3];Wang, Qi[1,2];Zhang, Jie[1,2];Zhu, Shiqin[1,2];Guo, Zhiqian[1,2];Zhu, Wei-Hong[1,2]

机构：[1]East China Univ Sci & Technol, Sch Chem & Mol Engn, Key Lab Adv Mat, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Chem & Mol Engn, Joint Int Res Lab Precis Chem & Mol Engn, Inst Fine Chem,Feringa Nobel Prize Scientist Join, Shanghai 200237, Peoples R China;[3]Dahua Hosp, Dept Intervent Oncol, Shanghai 200237, Peoples R China

年份：2019

卷号：7

期号：9

起止页码：1503

外文期刊名：JOURNAL OF MATERIALS CHEMISTRY B

收录：;EI(收录号：20191006585546);WOS:【SCI-EXPANDED(收录号:WOS:000459905100014)】；

基金：The authors acknowledge financial support from NSFC/China (21788102, 21421004, 21636002 and 81602718), National key Research and Development Program (2016YFA0200300), Fundamental Research Funds for the Central Universities (222201814013), Shanghai Health and Family Planning Commission Research Foundation (201540158), and Program of Introducing Talents of Discipline to Universities (B16017).

语种：英文

外文关键词：Biological organs - Infrared devices - Tumors - Targeted drug delivery - Biochemistry - Chromophores - Controlled drug delivery - Sulfur compounds - Drug interactions - Conjugated polymers - Diagnosis - Fluorescence

摘要：Improving the bioavailability and tumor-targeting ability of a prodrug, as well as monitoring its active ingredient release in vivo, is still a challenge in cancer diagnosis and therapy. Herein, a specific nanomized tumor-microenvironment-active near-infrared (NIR) fluorescent DCM-S-GEM/ PEG prodrug was developed as a potent monitoring platform, wherein we conjugated antitumor drug gemcitabine (GEM) and NIR fluorescent chromophore dicyanomethylene-4H-pyran (DCM) via glutathione (GSH)-activatable disulfide linker and encapsulated DCM-S-GEM into an amphiphilic polymer DSPE-mPEG by self-assembly. The nanomized DCM-S-GEM/ PEG prodrug exhibits excellent photostability and high biocompatibility, significantly improving the therapeutic efficacy toward lung tumor cells with fewer side-effects toward normal cells. Furthermore, when compared with the standalone DCM-S-GEM prodrug, the micellization with diblock DSPE-mPEG avoids fast metabolism, facilitates the accumulation of drugs in lung tumor tissues, displays longer tumor retention, and realizes precise drug release in lung tumors. The nanomized DCM-S-GEM/ PEG prodrug can be developed as a promising tool to monitor prodrug delivery and activation processes in vivo.