文献类型：期刊文献

英文题名：Folate-conjugated pH-controllable fluorescent nanomicelles acting as tumor targetable drug carriers

作者：Hao, Weiju[1,2];Wang, Tong[1,2];Liu, Danyang[1,2];Shang, Yazhuo[1,2];Zhang, Junqi[3,4];Xu, Shouhong[1,2];Liu, Honglai[1,2]

机构：[1]East China Univ Sci & Technol, Key Lab Adv Mat, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Dept Chem, Shanghai 200237, Peoples R China;[3]Fudan Univ, Key Lab Med Mol Virol, Minist Hlth, Sch Basic Med Sci, 138 Yixueyuan Rd, Shanghai 200032, Peoples R China;[4]Fudan Univ, Key Lab Med Mol Virol, Minist Educ, Sch Basic Med Sci, 138 Yixueyuan Rd, Shanghai 200032, Peoples R China

年份：2017

卷号：184

期号：8

起止页码：2881

外文期刊名：MICROCHIMICA ACTA

收录：;EI(收录号：20242616437631);WOS:【SCI-EXPANDED(收录号:WOS:000406066500044)】；

基金：Financial support for this work was provided by the National Natural Science Foundation of China (No. 21276074), National Natural Science Foundation of China for Innovative Research Groups (No. 51621002).

语种：英文

外文关键词：Nanomicelles; Fluorescence tracking; pH-sensitivity; Tumor targeting; Transfection; Intracellular drug delivery; Apoptosis

摘要：The authors describe biocompatible nanomicelle based drug carriers that can be used for simultaneous (a) fluorescence tracking, (b) pH-controlled release of the cancer drug doxorubicin (DOX), and (c) targeting the folate receptor. The pH-sensitive triblock copolymer is composed of poly2-(diisopropylamino) ethyl methacrylate and methoxypoly (ethylene glycol) which were prepared by radical polymerization and 'click' chemistry. The copolymers undergo selfassembly to form spherical micelles with diameters between 100 and 200 nm and a pH-trigger capability at pH values from 5.8 to 6.2. The micelles enabled DOX to be released at pH 5.0 at a much higher rate than at pH 7.4. Studies on cellular uptake revealed selective internalization of the DOX-loaded nanomicelles into HeLa cells where they can be imaged fluorometrically. Quantitative analysis of the green fluorescence indicated that the FITC-labeled micelles possess a transfection efficiency of about 79% while that of the nanomicellles with folate is only similar to 40% under the same conditions. Confocal laser scanning microscopy indicates that the micelles invade the lysosome of HeLa cells and that the DOX released by micelles causes strong cell lethality. In our preception, this work provides useful insights in terms of designing multifunctional drug carriers and of improving the applicability of copolymer micelles for drug delivery systems.