自组装绿茶多酚基纳米制剂的载体增强型光动力癌症治疗。,ACS Sustainable Chemistry & Engineering

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自组装绿茶多酚基纳米制剂的载体增强型光动力癌症治疗。
ACS Sustainable Chemistry & Engineering ( IF 8.4 ) Pub Date : 2020-10-20 , DOI: 10.1021/acssuschemeng.0c06645
Xiangyu Chen _{1,

2} , Zeng Yi _{1,

2} , Guangcan Chen _{1,

2} , Xiaomin Ma _{1,

2} , Wen Su _{1,

2} , Zhiwen Deng _{1,

2} , Lei Ma _{1,

2} , Qiulan Tong _{1,

2} , Yaqin Ran _{1,

2} , Xudong Li _{1,

2}

Affiliation

近来，已经开发了各种纳米技术来改善当前的光动力癌症疗法，其通常与光敏剂的缺陷有关，包括不良的溶解性，不足的光动力活性和高的暗毒性。天然来源的绿茶多酚，尤其是（-）-epigallocatechin-3-gallate（EGCG），具有固有的抗肿瘤活性。在这项工作中，进行了EGCG共轭聚乙二醇（PEG）（EGP）和二氢卟酚e6（Ce6）的自组装，以制备多酚纳米颗粒（EGP–Ce6 NPs），以实现载体增强的光动力癌症治疗。在EGCG与Ce6的比率从0.5、1.0到2.0的EGP–Ce6 NP的不同组中，EGP–Ce6 / 0.5 NPs的最大载药量（44％）和包封率（89％）。自组装的EGP–Ce6 NP具有良好的溶解性和最小的暗毒性。与游离药物相比，EGP–Ce6 NPs在细胞内摄取，活性氧（ROS）生成以及对多细胞肿瘤球的渗透性方面显示出增强的作用，表明它们作为光动力剂的可行性。此外，验证了EGP–Ce6 NP将光敏剂Ce6的光动力作用与EGP的抗肿瘤作用相结合，从而实现了载体增强型光动力癌症治疗。这项研究提出了一种简单的策略，即利用基于绿茶多酚的纳米技术来解决光敏剂的缺点以及增强的抗肿瘤效率，率先将天然产物应用于光动力疗法，不仅用于癌症，而且还用于皮肤病，传染病和心血管疾病。

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Carrier-Enhanced Photodynamic Cancer Therapy of Self-Assembled Green Tea Polyphenol-Based Nanoformulations

Recently, various nanotechnologies have been developed to improve the current photodynamic cancer therapy, which is generally associated with the deficiencies of photosensitizers including poor solubility, inadequate photodynamic activity, and high dark toxicity. Naturally resourced green tea polyphenols, especially (−)-epigallocatechin-3-gallate (EGCG), are well documented to have intrinsic antitumor activity. In this work, the self-assembly of EGCG-conjugated poly(ethylene glycol) (PEG) (EGP) and chlorin e6 (Ce6) was conducted to fabricate polyphenol nanoparticles (EGP–Ce6 NPs) for achieving carrier-enhanced photodynamic cancer therapy. Among different groups of EGP–Ce6 NPs with the ratio of EGCG to Ce6 varying from 0.5, 1.0 to 2.0, EGP–Ce6/0.5 NPs had the maximum drug loading (44%) and encapsulation rate (89%). The self-assembled EGP–Ce6 NPs had good solubility and minimal dark toxicity. Compared with free drugs, EGP–Ce6 NPs showed enhanced effects in intracellular uptake, reactive oxygen species (ROS) generation, and penetrability into multicellular tumor spheres, indicative of their feasibility as photodynamic agents. Furthermore, EGP–Ce6 NPs were verified to integrate the photodynamic effect of the photosensitizer Ce6 with the antitumor effect of EGP, realizing the carrier-enhanced photodynamic cancer therapy. This study proposed a simple strategy by utilizing green tea polyphenol-based nanotechnology to resolve the shortcomings of photosensitizers along with enhanced antitumor efficiency, spearheading the application of natural products in photodynamic therapies for not only carcinoma but also dermatologic, infectious, and cardiovascular diseases.

更新日期：2020-11-02

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