文献类型：期刊文献

英文题名：Light-Cross-linked Enediyne Small-Molecule Micelle-Based Drug-Delivery System

作者：Li, Baojun[1];Wu, Yuequn[2];Wang, Yue[1];Zhang, Mengsi[1];Chen, Huimin[1];Li, Jing[1];Liu, Runhui[2];Ding, Yun[1];Hu, Aiguo[1]

机构：[1]East China Univ Sci & Technol, Sch Mat Sci & Engn, Shanghai Key Lab Adv Polymer Mat, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Mat Sci & Engn, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China

年份：2019

卷号：11

期号：9

起止页码：8896

外文期刊名：ACS APPLIED MATERIALS & INTERFACES

收录：;EI(收录号：20191006594408);WOS:【SCI-EXPANDED(收录号:WOS:000460996900022)】；

基金：The authors gratefully acknowledge the financial support from National Natural Science Foundation of China (21871080, 21503078, and 21474027), the Fundamental Research Funds for the Central Universities (22221818014), and Shanghai Leading Academic Discipline Project (B502). A.H. thanks the "Eastern Scholar Professorship" support from Shanghai local government.

语种：英文

外文关键词：cytotoxicity; drug delivery; enediynes; light-cross-linked; small-molecule micelles

摘要：Light-cross-linked small-molecule micelles with enediyne units are designed for developing efficient drug-delivery systems. Gemcitabine (GEM) is chosen as a model hydrophilic drug and tethered with a maleimide-based enediyne (EDY) as a hydrophobic tail in the preparation of amphiphilic EDY-GEM. The stable micellar particles are obtained by cross-linking the enediyne moieties via photo-induced Bergman cyclization polymerization in aqueous media. The light-cross-linked spherical micelles with a size of 80 rim are characterized with dynamic light scattering and electron microscopy, showing robust micellar stability, bright fluorescent emission due to their intrinsic conjugated structure, and potential passive tumor-targeting ability through the enhanced permeability and retention effect. The drug-loaded micelles, as an example of light-cross-linked small-molecule micelle-based drug-delivery system, exhibit high drug-loading contents (50%) and greatly improved cytotoxicity toward A549 cells (decreasing the IC50 value of Gemcitabine by 10 times), thanks to the greatly increased cellular uptake of the drug-loaded micelles as confirmed by confocal laser scanning microscopy. The light-cross-linked enediyne-based small-molecule micelles system therefore provides a simple yet efficient drug-delivery platform for cancer chemotherapy.