Light-Cross-linked Enediyne Small-Molecule Micelle-Based Drug-Delivery System

被引：22

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

来源：

ACS APPLIED MATERIALS & INTERFACES | 2019年 / 11卷 / 09期

基金：

中国国家自然科学基金;

关键词：

cytotoxicity; drug delivery; enediynes; light-cross-linked; small-molecule micelles; POROUS ORGANIC POLYMERS; CELL LUNG-CANCER; BERGMAN CYCLIZATION; COPOLYMER MICELLES; NANOPARTICLES; VESICLES; EFFICACY; POLYPHENYLENES; CAMPTOTHECIN; GEMCITABINE;

D O I：

10.1021/acsami.8b22516

中图分类号：

TB3 [工程材料学];

学科分类号：

0805 ; 080502 ;

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.

引用

页码：8896 / 8903

页数：8

共 22 条

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[J]. INTERNATIONAL JOURNAL OF POLYMER SCIENCE, 2020, 2020
[22] Ultraviolet Light-Assisted Electrospinning of Core-Shell Fully Cross-Linked P(NIPAAm-co-NIPMAAm) Hydrogel-Based Nanofibers for Thermally Induced Drug Delivery Self-Regulation
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[J]. ADVANCED MATERIALS INTERFACES, 2020, 7 (12):

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