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首页> 外文期刊>RSC Advances >Paclitaxel prodrug based mixed micelles for tumor-targeted chemotherapy
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Paclitaxel prodrug based mixed micelles for tumor-targeted chemotherapy

机译：紫杉醇前药基混合胶束用于肿瘤靶向化疗

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摘要

An effective chemotherapy is usually subject to an insufficient loading of hydrophobic drugs as well as severe side effects. In order to address these dilemmas in one formulation, we herein construct paclitaxel prodrug based mixed micelles (MMs) for tumor-targeted chemotherapy. The paclitaxel prodrug containing a hydrophobic PTX and a hydrophilic PEG chain can self-assemble into uniform MMs with distearoyl phosphoethanolamine-polyethylene glycol-folate (DSPE-PEG-FA). The resultant MMs with preferable stability and hemolysis compatibility could improve the cellular uptake of nanoparticles via FA receptor-mediated endocytosis as compared to the single micelles (SMs). This tumor targetability was also confirmed in vivo by fluorescent imaging. MMs with a stable drug loading as well as tumor targetability displayed elevated in vitro cytotoxicity and in vivo antitumor efficacy compared with Taxol, which could be a potential formulation for cancer therapy.
机译：有效的化疗通常受到疏水药物的不足以及严重的副作用。 为了在一种配方中解决这些困境，在此方面，我们在本文中构建基于紫杉醇前药的混合胶束（MMS）用于肿瘤靶向化疗。 含有疏水性PTX和亲水性PEG链的紫杉醇前药可以自组装成均匀的MMS，用Distearoyl磷乙醇胺 - 聚乙二醇乙二醇酯（DSPE-PEG-FA）。 具有优选稳定性和溶血相容性的所得MMS可以通过FA受体介导的内吞作用，与单胶束（SMS）相比，通过FA受体介导的内吞作用来改善纳米颗粒的细胞摄取。 这种肿瘤靶向也通过荧光显像在体内确认。 MMS具有稳定的药物载荷以及肿瘤靶向在体外细胞毒性和体内抗肿瘤效力升高，与紫杉醇相比，这可能是癌症治疗的潜在配方。

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  • 来源
    《RSC Advances》 |2018年第1期|共10页
  • 作者

    Tang Dongyang; Zhao Xin; Yang Tie; Wang Cheng;

  • 作者单位

    Henan Inst Sci &

    Technol Dept Expt Ctr Xinxiang 453003 Henan Peoples R China;

    Xinxiang Cent Hosp Dept Pharm Xinxiang 453000 Henan Peoples R China;

    Jiangsu Chiatai Tianqing Pharmaceut Co Ltd Nanjing Res Ctr Nanjing 210042 Jiangsu Peoples R China;

    Zhejiang Univ Coll Pharmaceut Sci 866 Yuhangtang Rd Hangzhou 310058 Zhejiang Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
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