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首页> 外文期刊>Nanotechnology >Preparation of multilocation reduction-sensitive core crosslinked folate-PEG-coated micelles for rapid release of doxorubicin and tariquidar to overcome drug resistance
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Preparation of multilocation reduction-sensitive core crosslinked folate-PEG-coated micelles for rapid release of doxorubicin and tariquidar to overcome drug resistance

机译：用于快速释放多柔比蛋白和Tariquidar的多算子还原敏感核交联叶酸胶束的制备克服耐药性

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摘要

Herein, we prepared folate-targeting core crosslinked polymeric micelles (CCL/FA) containing multiple disulfide bonds located at the interface and core of the micelles to co-deliver doxorubicin (DOX) and the P-glycoprotein (P-gp) inhibitor tariquidar (TQR) for reversing drug resistance. The stability and redox-responsive behavior of the CCL/FA micelles was evaluated through the changes in morphology, molecular weight and hydrodynamic size. On the one hand, the micelles possessed good stability, which led to the suppression of drug release from the CCL micelles in the physiological environment. On the other hand, under reductive conditions, the CCL micelles collapsed rapidly and accelerated drug release markedly. In vitro cytotoxicity measurements, combined with confocal laser scanning microscopy (CLSM) and flow cytometry, confirmed that the dual-drug-loaded micelles exhibited obviously higher cytotoxicity to MCF-7/ ADR-resistant cells than free DOX center dot HCl, single-drug loaded CCL micelles and nontargeted CCL micelles. The results imply that co-delivering DOX and TQR by CCL/FA micelles may be a promising way of overcoming multidrug resistance in tumor treatments.
机译：在此，我们制备含有位于胶束界面和芯的多硫化键的叶酸靶向核交联的聚合物胶束（CCL / FA），以共传送多柔比蛋白（DOX）和P-糖蛋白（P-GP）抑制剂Tariquidar（ TQR）用于逆转耐药性。通过形态学，分子量和流体动力学尺寸的变化评价CCL / FA胶束的稳定性和氧化还原响应行为。一方面，胶束具有良好的稳定性，这导致了从生理环境中的CCL胶束中抑制药物释放。另一方面，在还原条件下，CCL胶束迅速塌陷并显着加速药物释放。体外细胞毒性测量，与共聚焦激光扫描显微镜（CLSM）和流式细胞术结合，证实了双药物负载胶束对MCF-7 / ADR抗性细胞显示出明显高于免费的DOX中心点HCL，单药的细胞毒性装载的CCL胶束和非靶案中的CCL胶束。结果暗示CCL / FA胶束共传送DOX和TQR可能是克服肿瘤治疗中多药耐药的有希望的方法。

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  • 来源
    《Nanotechnology》 |2017年第8期|共14页
  • 作者

    Yi Xiaoqing; Zhao Dan; Zhang Quan; Xu Jiaqi; Yuan Gongdao; Zhuo Renxi; Li Feng;

  • 作者单位

    Wuhan Univ Coll Chem &

    Mol Sci Minist Educ Key Lab Biomed Polymers Wuhan 430072 Peoples R China;

    Wuhan Univ Coll Chem &

    Mol Sci Minist Educ Key Lab Biomed Polymers Wuhan 430072 Peoples R China;

    Wuhan Univ Coll Chem &

    Mol Sci Minist Educ Key Lab Biomed Polymers Wuhan 430072 Peoples R China;

    Wuhan Univ Coll Chem &

    Mol Sci Minist Educ Key Lab Biomed Polymers Wuhan 430072 Peoples R China;

    Wuhan Univ Coll Chem &

    Mol Sci Minist Educ Key Lab Biomed Polymers Wuhan 430072 Peoples R China;

    Wuhan Univ Coll Chem &

    Mol Sci Minist Educ Key Lab Biomed Polymers Wuhan 430072 Peoples R China;

    Wuhan Univ Coll Chem &

    Mol Sci Minist Educ Key Lab Biomed Polymers Wuhan 430072 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 特种结构材料;
  • 关键词

    micelles; multiple disulfide bonds; co-delivery; reverse multidrug resistance;

    机译：胶束;多种二硫键;共同递送;反向多药抗性;

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