文献类型：期刊文献

英文题名：Near-Infrared Fluorescent Theranostic Cisplatin Prodrug with Transcatheter Intra-Arterial Therapy: Application to Rabbit Hepatocellular Carcinoma

作者：Li, Qiang[1,2];Wang, Qi[1,2];Wang, Saibo[3];Zhu, Shiqin[1,2];Yuan, Tianwen[3];Guo, Zhiqian[1,2];Cao, Jun[3];Tian, He[1,2];Zhu, Wei-Hong[1,2]

机构：[1]East China Univ Sci & Technol, Sch Chem & Mol Engn, Shanghai Key Lab Funct Mat Chem, Key Lab Adv Mat, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Joint Int Res Lab Precis Chem & Mol Engn, Sch 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：2018

卷号：1

期号：8

外文期刊名：ADVANCED THERAPEUTICS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000506348700008)】；

基金：Q.L. and Q.W. contributed equally to this work. This work was supported by grants from NSFC/China (21788102, 21421004, 21636002, and 81602718), National key Research and Development Program (2016YFA0200300), Fundamental Research Funds for the Central Universities (222201814013), and Shanghai Health and Family Planning Commission Research Foundation (201540158). All animal studies were performed in accordance with the relevant ethical guidelines.

语种：英文

外文关键词：controllable release; near-infrared fluorescence; prodrugs; rabbit hepatocellular carcinoma; transcatheter intra-arterial therapy; tumor targeting

摘要：Transcatheter intra-arterial therapy (TIT) has become valuable in the battle against primary and secondary hepatic malignancies. However, the lack of a mechanism to visualize real-time drug release and avoid fast metabolic clearance of chemotherapeutic agents is the primary barrier to TIT for hepatocellular carcinoma. Here, a specific near-infrared (NIR) fluorescent prodrug platform, that is, DSPE-mPEG/DCM-S-Pt micelles (DCM-S-Pt@PEG), to assist TIT in direct administration to large mammals like rabbits, is presented. DCM-S-Pt@PEG consists of a NIR fluorophore for tracing drug release, a nonspecific antitumor drug cisplatin for hepatocellular carcinoma treatment, a glutathione-activatable disulfide linker, and a DSPE-mPEG nano-micelle carrier for controllable drug release. DCM-S-Pt@PEG can make the drug accumulation in tumor tissues enhance the therapeutic effect by: i) specific delivery of prodrug to hepatic tumor tissues through the femoral artery by TIT, ii) sustained drug-release from the biodegradable lipid DSPE-mPEG micelle to minimize metabolic clearance, and iii) cancer biomarker-activated drug release. It provides a promising strategy to assist TIT in treating unresectable devastating hepatocellular carcinoma administration in the rabbit model, rather than common mouse model.