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Spermine modified polymeric micelles with pH-sensitive drug release for targeted and enhanced antitumor therapy

机译：Femermine改性聚合物胶束，具有pH敏感的药物释放，用于靶向和增强的抗肿瘤治疗

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摘要

Tumor targeting delivery of chemotherapeutic drugs by nanocarriers has been demonstrated to be a promising strategy for cancer therapy with improved therapeutic efficacy. In this work, we reported a novel type of active targeting micelle with pH-responsive drug release by using biodegradable poly(lactide)-poly(2-ethyl-2-oxazoline) di-block copolymers functionalized with spermine (SPM). SPM has been considered as a tumor binding ligand through its specific interaction with the polyamine transport system (PTS), a transmembrane protein overexpressed on various types of cancer cell, while its application in nano-drug delivery systems has rarely been explored. The micelles with spherical shape (approximate to 110 nm) could load hydrophobic paclitaxel (PTX) with high capacity, and release the payload much faster at acidic pH (4.5-6.5) than at pH 7.4. This pH-responsive property assisted the rapid escape of drug from the endo/lysosome after internalization as demonstrated by confocal laser scanning microscopy images using coumarin-6 (Cou-6) as a fluorescent probe. With surface SPM modification, the micelles displayed much higher cellular uptake than SPM lacking micelles in various types of cancer cells, demonstrating tumor targeting ability. The uptake mechanism of SPM modified micelles was explored by flow cytometry, which suggested an energy-consuming sag vesicle-mediated endocytosis pathway. As expected, the micelles displayed significantly enhanced anti-cancer activity. This work demonstrates that SPM modified pH-sensitive micelles may be potential drug delivery vehicles for targeting and effective cancer therapy.
机译：已经证明了纳米载体靶向化学治疗药物的肿瘤是具有改善治疗疗效的癌症治疗的有希望的策略。在这项工作中，我们报道了一种新型类型的活性靶向胶束，通过使用可生物降解的聚（丙交酯）-pold（2-乙基-2-恶唑啉）二嵌段共聚物与精霉素（SPM）官能化的官能化的PH-响应药物释放。通过其与多胺输送系统（PTS）的特定相互作用被认为是肿瘤结合配体，其在各种类型的癌细胞上过表达的跨膜蛋白，而其在纳米药物输送系统中的应用很少被探索。具有球形形状的胶束（近似为110nm）可以用高容量加载疏水紫杉醇（PTX），并在酸性pH（4.5-6.5）上释放比pH7.4在pH 7.4中的有效载荷。这种pH-响应性能在内化后辅助药物的快速逃逸，通过共聚焦激光扫描显微镜图像作为荧光探针，通过共聚焦激光扫描显微镜图像证明。对于表面SPM改性，胶束显示比各种类型的癌细胞中缺乏胶束的SPM更高的细胞摄取，证明了肿瘤靶向能力。流式细胞术探索了SPM改性胶束的摄取机理，这提出了消耗能量的凹凸囊泡介导的内吞作用途径。正如预期的那样，胶束显示出显着增强的抗癌活动。这项工作表明SPM改性的pH敏感胶束可以是用于靶向和有效的癌症治疗的潜在药物递送载体。

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  • 来源
    《RSC Advances》 |2019年第20期|共12页
  • 作者

    Chen Yang; Yang Cejun; Mao Juan; Li Haigang; Ding Jinsong; Zhou Wenhu;

  • 作者单位

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Hosp 3 Dept Radiol Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Changsha Med Univ Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

    Cent S Univ Xiangya Sch Pharmaceut Sci Changsha 410013 Hunan Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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