文献类型：期刊文献

英文题名：Well-defined labile diselenide-centered poly(ε-caprolactone)-based micelles for activated intracellular drug release

作者：Wei, Chao[1];Zhang, Yan[1];Xu, Heng[2];Xu, Ying[1];Xu, Yue[1];Lang, Meidong[1,3]

机构：[1]East China Univ Sci & Technol, Sch Mat & Sci & Engn, Key Lab Ultrafine Mat, Minist Educ, Shanghai 200237, Peoples R China;[2]Collaborat Innovat Ctr Petrochem New Mat, Anqing 246011, Anhui, Peoples R China;[3]Shanghai Collaborat Innovat Ctr Biomfg, 130 Meilong Rd, Shanghai 200237, Peoples R China

年份：2016

卷号：4

期号：29

起止页码：5059

外文期刊名：JOURNAL OF MATERIALS CHEMISTRY B

收录：;EI(收录号：20163102658271);WOS:【SCI-EXPANDED(收录号:WOS:000380339100011)】；

基金：Financial support from the National Natural Science Foundation of China (21274039), Shanghai Pujiang Program (14PJD014), 111 Project (B14018), the Specialized Research Fund for the Doctoral Program of Higher Education (20130074110007) and the Basic Research Key Program Project of Commission of Science and Technology of Shanghai (12JC1403000 and 12JC1403100) is gratefully acknowledged. The authors acknowledge Dr Zhong Chen Song's group (Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine) for their support in cell behaviour measurements.

语种：英文

外文关键词：Micelles - Polyols - Chemical bonds - Cancer cells - Ethylene glycol - Ring opening polymerization - Biodegradable polymers - Cytology - Cells - Controlled drug delivery - Reduction - Targeted drug delivery - Tumors - Block copolymers - Selenium compounds

摘要：Well-defined diselenide-centered biodegradable tri-block copolymers methoxyl poly(ethylene glycol)-b-poly(epsilon-caprolactone)-b-methoxyl poly(ethylene glycol) (mPEG-PCL-Se)(2) were precisely synthesized by the combination of ring opening polymerization using di(1-hydroxyethylene) diselenide as a new initiator and a facile coupling reaction. The amphiphilic block copolymers enabled the formation of self-assembled micelles which revealed an excellent reductive response to glutathione (GSH) due to the unique reduction-responsive cleavage of the diselenide bond. Such GSH response ensured an enhanced release of anticancer drugs (DOX) from the micelles in simulative tumor microenvironments; moreover, the drug release could be changed to some extent through fine-tuning the chemical composition of the copolymers. Flow cytometry and confocal laser scanning microscopy (CLSM) measurements confirmed that the DOX-loaded micelles could be efficiently taken up by oral squamous carcinoma (HN30) cells and DOX was released into the nuclei of cancer cells following 4 h of incubation. The cell viability assays showed the diselenide-containing polymers were nontoxic up to a tested concentration (400 mu g mL(-1)), while the DOX-loaded micelles exhibited an evident inhibition toward HN30 cells. Therefore, the reduction-labile biodegradable (mPEG-PCL-Se)(2) may offer an alternative platform for tumor-targeting therapy.