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首页> 外文期刊>RSC Advances >iRGD-mediated reduction-responsive DSPE-PEG/LA-PLGA-TPGS mixed micelles used in the targeted delivery and triggered release of docetaxel in cancer
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iRGD-mediated reduction-responsive DSPE-PEG/LA-PLGA-TPGS mixed micelles used in the targeted delivery and triggered release of docetaxel in cancer

机译：IRGD介导的减少响应性DSPE-PEG / LA-PLGA-TPGS用于靶向递送的混合胶束和癌症中的多西紫杉醇释放

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摘要

Reduction-sensitive micelles with crosslinked cores were developed to load the lipophilic chemotherapeutic drug docetaxel (DTX) in order to overcome the issues of toxicity, water insolubility, and rapid metabolism of DTX. These DTX-loaded micelles (MM(DTX/Crosslink)) provide efficient incorporation and sustained release of DTX. Using independently synthesized LA-PLGA-TPGS and DSPE-PEG polymers as vehicles, MM(DTX/Crosslink) was found to be reduction-responsive, and possessed desirable drug entrapment efficiency (84.17 +/- 1.15%) and drug loading efficiency (6.21 +/- 0.07%). The MM(DTX/Crosslink) quickly dissociated under reduction conditions that mimicked the reductive intracellular environment, suggesting that it can rapidly release the encapsulated DTX in vitro. Furthermore, to target MM(DTX/Crosslink) to tumors for cancer therapy, iRGD was conjugated to the surface of MM(DTX/Crosslink). The iRGD-MM(DTX/Crosslink) micelles significantly increased the cellular uptake of DTX and inhibited cell proliferation, compared to the micelles without iRGD modification. Moreover, the iRGD-MM(DTX/Crosslink) micelles presented enhanced antitumor effects based on the analyses of apoptosis and cell cycle arrest. The micelles developed in this work may constitute a stable, efficient, and powerful system to deliver DTX into cancer cells.
机译：开发了具有交联芯的减敏胶束以加载亲脂化学治疗药物多紫杉醇（DTX），以克服DTX的毒性，水不溶性和快速代谢的问题。这些DTX加载的胶束（MM（DTX / Crosslink））提供了DTX的有效掺入和持续释放。使用独立合成的La-PLGA-TPGS和DSPE-PEG聚合物作为车辆，发现MM（DTX /交联剂）被发现还原响应性，并且具有所需的药物夹带效率（84.17 +/- 1.15％）和药物负载效率（6.21 +/- 0.07％）。 MM（DTX / Crosslink）在减少造型的细胞内环境模仿条件下快速解离，表明它可以在体外快速释放包封的DTX。此外，对癌症治疗的肿瘤靶向mM（dtx / crosslink），IRGD与MM（DTX /交联链接）的表面缀合。与没有IRGD改性的胶束相比，IRGD-MM（DTX / Crosslink）胶束显着增加了DTX的细胞摄取和抑制细胞增殖。此外，IRGD-MM（DTX / Crosslink）胶束基于细胞凋亡和细胞周期骤停的分析呈现增强的抗肿瘤效应。本作作品中开发的胶束可以构成稳定，有效和强大的系统，以将DTX递送到癌细胞中。

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  • 来源
    《RSC Advances》 |2016年第34期|共12页
  • 作者

    Wang Lu; Xie Xi; Liu Di; Fang Xiao-Bin; Li Peng; Wan Jian-Bo; He Cheng-Wei; Chen Mei-Wan;

  • 作者单位

    Univ Macau Inst Chinese Med Sci State Key Lab Qual Res Chinese Med Ave Padre Tomas Pereira SJ Taipa 999078 Macao Peoples R China;

    Sun Yat Sen Univ Sch Chem &

    Chem Engn Guangzhou 510275 Guangdong Peoples R China;

    Univ Minnesota Sch Math Minneapolis MN 55455 USA;

    Univ Macau Inst Chinese Med Sci State Key Lab Qual Res Chinese Med Ave Padre Tomas Pereira SJ Taipa 999078 Macao Peoples R China;

    Univ Macau Inst Chinese Med Sci State Key Lab Qual Res Chinese Med Ave Padre Tomas Pereira SJ Taipa 999078 Macao Peoples R China;

    Univ Macau Inst Chinese Med Sci State Key Lab Qual Res Chinese Med Ave Padre Tomas Pereira SJ Taipa 999078 Macao Peoples R China;

    Univ Macau Inst Chinese Med Sci State Key Lab Qual Res Chinese Med Ave Padre Tomas Pereira SJ Taipa 999078 Macao Peoples R China;

    Univ Macau Inst Chinese Med Sci State Key Lab Qual Res Chinese Med Ave Padre Tomas Pereira SJ Taipa 999078 Macao Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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