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Therapeutic Nanosystem Consisting of Singlet-Oxygen-Responsive Prodrug and Photosensitizer Excited by Two-Photon Light
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2017-12-28 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00394
Yi Lin 1 , Xiao-fang Jiang 1 , Xiangyan Duan 1 , Fang Zeng 1 , Bo Wu 1 , Shuizhu Wu 1
Affiliation  

Using light as the sole stimulus and employing the generated singlet oxygen as a therapeutic agent and the trigger to activate chemo-drug release could serve as an elegant way to bring into full play the advantageous features of light and enhance therapeutic efficacy through a combination of chemotherapy and photodynamic therapy. Herein a liposomal drug system has been developed by embedding a fluorescent photosensitizer and a prodrug into phospholipid vesicles. Upon one- or two-photon light irradiation, the photosensitizer generates singlet oxygen, which removes the protecting group of the prodrug and subsequently causes the release of the active drug chlorambucil. With the combined action of O21 and chlorambucil, highly controllable cytotoxicity toward cancer cells was achieved. In addition, the fluorescent photosensitizer gives out fluorescent signal acting as the drug monitoring agent. This strategy may provide an efficient approach for cancer treatment and some useful insights for designing light-stimulated on-demand therapeutic systems.

中文翻译:

由双光子光激发的单线态氧响应性前药和光敏剂组成的治疗性纳米系统

使用光作为唯一刺激物,并使用产生的单线态氧作为治疗剂,并激活化学药物释放的触发器,可以作为一种优雅的方式来充分发挥光的优势,并通过化学疗法相结合来提高治疗功效和光动力疗法。在本文中,已经通过将荧光光敏剂和前药嵌入磷脂囊泡中来开发脂质体药物系统。在单光子或双光子光照射下,光敏剂产生单线态氧,该单线态氧除去前药的保护基,并随后释放活性药物苯丁酸氮芥。在O 2 1的共同作用下苯丁酸氮芥和苯丁酸氮芥对​​癌细胞具有高度可控的细胞毒性。另外,荧光光敏剂发出用作药物监测剂的荧光信号。该策略可以为癌症治疗提供有效的方法,并为设计光刺激的按需治疗系统提供一些有用的见识。
更新日期:2017-12-28
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