Real-Time Monitoring of Anticancer Drug Release with Highly Fluorescent Star-Conjugated Copolymer as a Drug Carrier

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• 作者：Feng Qiu ; Dali Wang ; Qi Zhu ; Lijuan Zhu ; Gangsheng Tong ; Yunfeng Lu ; Deyue Yan ; Xinyuan Zhu
• 刊名：Biomacromolecules
• 出版年：2014
• 出版时间：April 14, 2014
• 年：2014
• 卷：15
• 期：4
• 页码：1355-1364
• 全文大小：648K
• 年卷期：v.15,no.4(April 14, 2014)
• ISSN：1526-4602

文摘

Chemotherapy is one of the major systemic treatments for cancer, in which the drug release kinetics is a key factor for drug delivery. In the present work, a versatile fluorescence-based real-time monitoring system for intracellular drug release has been developed. First, two kinds of star-conjugated copolymers with different connections (e.g., pH-responsive acylhydrazone and stable ether) between a hyperbranched conjugated polymer (HCP) core and many linear poly(ethylene glycol) (PEG) arms were synthesized. Owing to the amphiphilic three-dimensional architecture, the star-conjugated copolymers could self-assemble into multimicelle aggregates from unimolecular micelles with excellent emission performance in the aqueous medium. When doxorubicin (DOX) as a model drug was encapsulated into copolymer micelles, the emission of star-conjugated copolymer and DOX was quenched. In vitro biological studies revealed that fluorescent intensities of both star-conjugated copolymer and DOX were activated when the drug was released from copolymeric micelles, resulting in the enhanced cellular proliferation inhibition against cancer cells. Importantly, pH-responsive feature of the star-conjugated copolymer with acylhydrazone linkage exhibited accelerated DOX release at a mildly acidic environment, because of the fast breakage of acylhydrazone in endosome or lysosome of tumor cells. Such fluorescent star-conjugated copolymers may open up new perspectives to real-time study of drug release kinetics of polymeric drug delivery systems for cancer therapy.