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Activatable paclitaxel prodrug in enhanced hypoxic microenvironment upon irradiation.
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2020-08-27 , DOI: 10.1002/anie.202008732
Shiyu Zhou 1 , Xiuli Hu 2 , Rui Xia 2 , Shi Liu 2 , Qing Pei 2 , Guang Chen 1 , Zhigang Xie 2 , Xiabin Jing 2
Affiliation  

The innate hypoxic microenvironment of most solid tumors has a major influence on tumor growth, invasiveness, and distant metastasis. Here, a hypoxia‐activated self‐immolative prodrug of paclitaxel (PTX2‐Azo) was synthesized and encapsulated by a peptide copolymer decorated with the photosensitizer chlorin e6 (Ce6) to prepare light‐boosted PTX nanoparticle (Ce6/PTX2‐Azo NP). In this nanoparticle, PTX2‐Azo prevents premature drug leakage and realizes specific release in hypoxic tumor microenvironment and the photosensitizer Ce6 not only efficiently generates singlet oxygen under light irradiation but also acts as a positive amplifier to promote the release of PTX. The combination of photodynamic therapy (PDT) and chemotherapy results in excellent antitumor efficacy, demonstrating the great potential for synergistic cancer therapy.

中文翻译:

辐照后可增强缺氧微环境的可活化紫杉醇前药。

大多数实体瘤的先天性缺氧微环境对肿瘤的生长,侵袭性和远处转移有重大影响。在此合成了紫杉醇的低氧激活自消灭性前药(PTX 2-偶氮),并用装饰有光敏剂二氢卟吩e6(Ce6)的肽共聚物封装,制备了光增强的PTX纳米粒子(Ce6 / PTX 2-偶氮NP)。 )。在这种纳米粒子中,PTX 2‐偶氮可防止过早的药物泄漏并在缺氧的肿瘤微环境中实现特定释放,并且光敏剂Ce6不仅在光照射下有效产生单线态氧,而且还充当促进PTX释放的正向放大器。光动力疗法(PDT)和化学疗法的结合产生了优异的抗肿瘤功效,证明了协同癌症疗法的巨大潜力。
更新日期:2020-08-27
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