Photodynamic therapy (PDT) takes advantage of photosensitizers (PSs) to generate reactive oxygen species (ROS) for cell killing when excited by light. It has been widely used in clinic for therapy of multiple cancers. Currently, all the FDA-approved PSs, including porphyrin, are all small organic molecules, suffering from aggregation-caused quenching (ACQ) issues in biological environment and lacking tumor targeting capability. Nanoparticles (NPs) with size between 20nm and 200nm possess tumor targeting capability due to the enhanced permeability and retention (EPR) effect. It is urgent to develop a new strategy to form clinical-approved-PSs-based NPs with improved ROS generation capability. In this study, we report a strategy to overwhelm the ACQ of porphyrin by doping it with a type of aggregation-induced emission (AIE) luminogen to produce a binary NPs with high biocompatibility, and enhanced fluorescence and ROS generation capability. Such NPs can be readily synthesized by mixing a porphyrin derivative, Ce6 with a typical AIE luminogen, TPE-Br. Here, our experimental results have demonstrated the feasibility and effectiveness of this strategy, endowing it a great potential in clinical applications.

中文翻译：

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具有增强的活性氧生成能力的二元有机纳米粒子用于光动力治疗

光动力疗法 (PDT) 利用光敏剂 (PS) 在光激发时产生活性氧 (ROS) 杀死细胞。它已广泛用于临床治疗多种癌症。目前，包括卟啉在内的所有FDA批准的PS都是有机小分子，在生物环境中存在聚集引起的猝灭（ACQ）问题，缺乏肿瘤靶向能力。尺寸在 20 之间的纳米粒子 (NPs)纳米和 200由于增强的渗透性和保留（EPR）效应，nm具有肿瘤靶向能力。迫切需要制定一种新的策略来形成具有改进的 ROS 生成能力的临床批准的基于 PSs 的 NPs。在这项研究中，我们报告了一种策略，通过掺杂一种聚集诱导发射 (AIE) 发光剂来压倒卟啉的 ACQ，以产生具有高生物相容性、增强荧光和 ROS 生成能力的二元纳米粒子。通过将卟啉衍生物 Ce6 与典型的 AIE 发光剂 TPE-Br 混合，可以很容易地合成此类 NP。在这里，我们的实验结果证明了该策略的可行性和有效性，使其在临床应用中具有巨大的潜力。