Rationally Engineering Phototherapy Modules of Eosin-Conjugated Responsive Polymeric Nanocarriers via Intracellular Endocytic pH Gradients

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• 作者：Guhuan Liu ; Jinming Hu ; Guoying Zhang ; Shiyong Liu
• 刊名：Bioconjugate Chemistry
• 出版年：2015
• 出版时间：July 15, 2015
• 年：2015
• 卷：26
• 期：7
• 页码：1328-1338
• 全文大小：614K
• ISSN：1520-4812

文摘

Spatiotemporal switching of respective phototherapy modes at the cellular level with minimum side effects and high therapeutic efficacy is a major challenge for cancer phototherapy. Herein we demonstrate how to address this issue by employing photosensitizer-conjugated pH-responsive block copolymers in combination with intracellular endocytic pH gradients. At neutral pH corresponding to extracellular and cytosol milieu, the copolymers self-assemble into micelles with prominently quenched fluorescence emission and low ¹O₂ generation capability, favoring a highly efficient photothermal module. Under mildly acidic pH associated with endolysosomes, protonation-triggered micelle-to-unimer transition results in recovered emission and enhanced photodynamic ¹O₂ efficiency, which synergistically actuates release of encapsulated drugs, endosomal escape, and photochemical internalization processes.