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Linear and high-molecular-weight poly-porphyrins for efficient photodynamic therapy dagger

机译：用于高效光动力疗法匕首的线性和高分子量多卟啉

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摘要

Photodynamic therapy (PDT) holds great potential in cancer treatment due to the advantages of non-invasiveness, negligible side-effect, and high spatiotemporal selectivity. Porphyrin is the most widely used photosensitizer in clinical treatment. However, its PDT efficacy is always limited by the undesired aggregation caused quenching (ACQ) effect originating from the planar and rigid structure. In this work, a linear polymeric porphyrin with "structure defects" was developed to overcome the ACQ effect for most of the photosensitizers with conjugated macrocycles. Compared to porphyrin monomers, poly-porphyrins could improve singlet oxygen generation ability, and the singlet oxygen quantum yield enhanced with increasing molecular weight of poly-porphyrins. To achieve efficient in vivo PDT, PEG and acetazolamide were conjugated to the optimized poly-porphyrins to afford pP-PEG-AZ nanoparticles (pP-PEG-AZ NPs) with excellent stability, efficient in vitro intracellular internalization, negligible dark-toxicity, notable photo-toxicity, and in vivo anti-cancer efficacy based on combined PDT and anti-angiogenesis therapy.
机译：光动力疗法（PDT）由于非侵袭性，缺点和高时的选择性高的优点，具有巨大的癌症治疗潜力。卟啉是临床治疗中最广泛使用的光敏剂。然而，其PDT功效总是受到来自平面和刚性结构的不期望的聚集导致淬火（ACQ）效应的限制。在这项工作中，开发了具有“结构缺陷”的线性聚合物卟啉，以克服具有共轭大键的大多数光敏剂的ACQ效应。与卟啉单体相比，聚卟啉可以改善单脉冲氧气产生能力，随着多卟啉的分子量增加，单向氧量子产率增强。为了在体内PDT中实现高效，PEG和乙酰唑胺与优化的聚卟啉缀合，得到PP-PEG-AZ纳米颗粒（PP-PEG-AZ NPS），具有优异的稳定性，高效的体外细胞内内化，忽略不计的毒性，显着光学毒性，基于组合PDT和抗血管生成治疗的体内抗癌疗效。

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  • 来源
    《Biomaterials Science》 |2021年第13期|共10页
  • 作者

    Zheng Nan; Li Xiahui; Huangfu Shangwei; Xia Kangkai; Yue Ruofei; Wu Huijian; Song Wangze;

  • 作者单位

    Dalian Univ Technol Sch Chem Engn State Key Lab Fine Chem Dalian 116024 Peoples R China;

    Dalian Univ Technol Sch Bioengn Dalian 116024 Peoples R China;

    Dalian Univ Technol Sch Chem Engn State Key Lab Fine Chem Dalian 116024 Peoples R China;

    Dalian Univ Technol Sch Bioengn Dalian 116024 Peoples R China;

    Dalian Univ Technol Sch Chem Engn State Key Lab Fine Chem Dalian 116024 Peoples R China;

    Dalian Univ Technol Sch Bioengn Dalian 116024 Peoples R China;

    Dalian Univ Technol Sch Chem Engn State Key Lab Fine Chem Dalian 116024 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 分子生物学;
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