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Rational design of a “dual lock-and-key” supramolecular photosensitizer based on aromatic nucleophilic substitution for specific and enhanced photodynamic therapy
Chemical Science ( IF 7.6 ) Pub Date : 2020-08-25 , DOI: 10.1039/d0sc01122c Kun-Xu Teng 1 , Li-Ya Niu 1 , Yan-Fei Kang 1 , Qing-Zheng Yang 1
Chemical Science ( IF 7.6 ) Pub Date : 2020-08-25 , DOI: 10.1039/d0sc01122c Kun-Xu Teng 1 , Li-Ya Niu 1 , Yan-Fei Kang 1 , Qing-Zheng Yang 1
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Photosensitizing agents are essential for precise and efficient photodynamic therapy (PDT). However, most of the conventional photosensitizers still suffer from limitations such as aggregation-caused quenching (ACQ) in physiological environments and toxic side-effects on normal tissues during treatment, leading to reduced therapeutic efficacy. Thus, integrating excellent photophysical properties and accurate carcinoma selectivity in a photosensitizer system remains highly desired. Herein, a “dual lock-and-key” supramolecular photosensitizer BIBCl–PAE NPs for specific and enhanced cancer therapy is reported. BIBCl–PAE NPs are constructed by encapsulating a rationally designed glutathione (GSH)-activatable photosensitizer BIBCl in a pH-responsive diblock copolymer. In normal tissues, BIBCl is “locked” in the hydrophobic core of the polymeric micelles due to ACQ. Under the “dual key” activation of low pH and high levels of GSH in a tumor microenvironment, the disassembly of micelles facilitates the reaction of BIBCl with GSH to release water-soluble BIBSG with ideal biocompatibility, enabling the highly efficient PDT. Moreover, benefiting from the Förster resonance energy transfer effect of BIBSG, improved light harvesting ability and 1O2 production are achieved. In vitro and vivo experiments have demonstrated that BIBCl–PAE NPs are effective in targeting and inhibiting carcinoma. BIBCl–PAE NPs show superior anticancer efficiency relative to non-activatable controls.
中文翻译：
基于芳香亲核取代的“双锁匙”超分子光敏剂的合理设计，用于特异性和增强的光动力疗法
光敏剂对于精确有效的光动力疗法（PDT）是必不可少的。然而，大多数常规的光敏剂仍然受到诸如在生理环境中聚集引起的猝灭（ACQ）以及治疗期间对正常组织的毒副作用的限制，导致治疗功效降低。因此，仍然非常需要在光敏剂系统中整合优异的光物理性质和准确的癌选择性。在本文中，报道了用于特异性和增强癌症治疗的“双重锁定和键式”超分子光敏剂BIBC1–PAE NP。BIBCl–PAE NP是通过将合理设计的谷胱甘肽（GSH）激活的光敏剂BIBCl封装在pH响应性双嵌段共聚物中而构建的。在正常组织中 由于ACQ，BIBC1被“锁定”在聚合物胶束的疏水核中。在肿瘤微环境中低pH和高水平GSH的“双重关键”激活下，胶束的分解促进了BIBC1与GSH的反应，以释放具有理想生物相容性的水溶性BIBSG，从而实现了高效PDT。此外，得益于BIBSG的Förster共振能量转移效应，提高了光收集能力和实现了1 O 2的生产。体外和体内实验表明，BIBC1–PAE NP在靶向和抑制癌症方面有效。BIBCl–PAE NPs相对于不可激活的对照显示出优异的抗癌效率。
更新日期：2020-09-16
中文翻译：
基于芳香亲核取代的“双锁匙”超分子光敏剂的合理设计，用于特异性和增强的光动力疗法
光敏剂对于精确有效的光动力疗法（PDT）是必不可少的。然而，大多数常规的光敏剂仍然受到诸如在生理环境中聚集引起的猝灭（ACQ）以及治疗期间对正常组织的毒副作用的限制，导致治疗功效降低。因此，仍然非常需要在光敏剂系统中整合优异的光物理性质和准确的癌选择性。在本文中，报道了用于特异性和增强癌症治疗的“双重锁定和键式”超分子光敏剂BIBC1–PAE NP。BIBCl–PAE NP是通过将合理设计的谷胱甘肽（GSH）激活的光敏剂BIBCl封装在pH响应性双嵌段共聚物中而构建的。在正常组织中 由于ACQ，BIBC1被“锁定”在聚合物胶束的疏水核中。在肿瘤微环境中低pH和高水平GSH的“双重关键”激活下，胶束的分解促进了BIBC1与GSH的反应，以释放具有理想生物相容性的水溶性BIBSG，从而实现了高效PDT。此外，得益于BIBSG的Förster共振能量转移效应，提高了光收集能力和实现了1 O 2的生产。体外和体内实验表明，BIBC1–PAE NP在靶向和抑制癌症方面有效。BIBCl–PAE NPs相对于不可激活的对照显示出优异的抗癌效率。
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