Cytosol-Specific Fluorogenic Reactions for Visualizing Intracellular Disintegration of Responsive Polymeric Nanocarriers and Triggered Drug Release

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• 作者：Yanyan Jiang ; Guhuan Liu ; Xiaorui Wang ; Jinming Hu ; Guoying Zhang ; Shiyong Liu
• 刊名：Macromolecules
• 出版年：2015
• 出版时间：February 10, 2015
• 年：2015
• 卷：48
• 期：3
• 页码：764-774
• 全文大小：667K
• ISSN：1520-5835

文摘

Supramolecular aggregates of stimuli-responsive block copolymers are increasingly utilized as drug nanocarriers. Although in situ tracking their triggered disintegration and drug release processes at the cellular level is highly desirable, it remains a considerable challenge. We report the fabrication of double hydrophilic block copolymers covalently conjugated with 伪,尾-unsaturated ketone-caged coumarin functionalities in the thermoresponsive block. Upon thermo-induced micellization and cellular uptake, Michael addition reaction of unsaturated ketone moieties with thiol compounds (GSH and Cys) in the reductive subcellular compartments leads to micelle-to-unimer transition. This is accompanied by concomitant fluorescence emission turn-on and triggered drug release, allowing for the process visualization.