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Targeted dextran-b-poly(epsilon-caprolactone) micelles for cancer treatments

机译：靶向葡聚糖-B-聚（Epsilon-Caprolacterone）胶束用于癌症处理

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摘要

In this study, targeted drug deliveries with excellent biocompatibility have been investigated to improve the efficacy and reduce the systemic toxicity of drugs. First, amphiphilic dextran-b-poly(epsilon-caprolactone) (Dex-PCL) copolymers were synthesized by a "click" reaction between alpha-alkyne terminated dextran and azido-terminated poly(epsilon-caprolactone). Then, the targeted molecules, such as folic acid and galactose, were conjugated to Dex-PCL. To verify their feasibility as drug delivery vehicles, DOX was loaded into Dex-PCL micelles with or without a targeted molecule. The in vitro release of DOX from DOX-loaded micelles demonstrated that there was a continuous release after burst release in the first 6 h. The cell viability assay of DOX-loaded micelles conjugated with targeting molecules against HeLa and HepG2 cells was investigated. Targeted DOX-loaded micelles showed significant bindings with tumor cells and efficient inhibition to corresponding targeted cells. Therefore, targeted DOX-loaded micelles provided an efficient drug delivery platform for the inhibition of cancer cells.
机译：在这项研究中，已经研究了具有优异生物相容性的靶向药物递送，以提高药物的疗效和降低全身毒性。首先，通过α-炔烃封端的葡聚糖和偶氮封端的聚（epsilon-己内酯）之间的“点击”反应合成两亲性葡聚糖-B-聚（epsilon-己内酯）（DEX-PCL）共聚物。然后，靶向分子，例如叶酸和半乳糖，与DEX-PCL缀合。为了验证其作为药物递送车辆的可行性，DOX随身携带或没有靶向分子的DEX-PCL胶束。从Dox加载的胶束的DOX的体外释放表明，在前6小时爆裂后爆裂后存在连续释放。研究了与靶向分子与HeLa和HepG2细胞缀合的DOX负载胶束的细胞活力测定。靶向的DOX加载的胶束显示出与肿瘤细胞的显着结合，并有效抑制对应的靶细胞。因此，靶向DOX加载的胶束为抑制癌细胞提供了有效的药物递送平台。

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  • 来源
    《RSC Advances》 |2015年第24期|共8页
  • 作者

    Zhang Zhe; Chen Xiaofei; Gao Xiaoye; Yao Xuemei; Chen Li; He Chaoliang; Chen Xuesi;

  • 作者单位

    NE Normal Univ Dept Chem Changchun 130024 Peoples R China;

    NE Normal Univ Dept Chem Changchun 130024 Peoples R China;

    Chinese Acad Sci Changchun Inst Appl Chem Changchun 130022 Peoples R China;

    NE Normal Univ Dept Chem Changchun 130024 Peoples R China;

    NE Normal Univ Dept Chem Changchun 130024 Peoples R China;

    Chinese Acad Sci Changchun Inst Appl Chem Changchun 130022 Peoples R China;

    Chinese Acad Sci Changchun Inst Appl Chem Changchun 130022 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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