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Novel glycyrrhetinic acid conjugated pH-sensitive liposomes for the delivery of doxorubicin and its antitumor activities

机译：新型甘草酸缀合的pH敏感的脂质体，用于递送多柔比星及其抗肿瘤活性

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摘要

Over the last few decades pH-sensitive drug delivery systems have been successfully developed for the treatment of cancers by improving the therapeutical effect. In this study, a novel pH-sensitive conjugate glycyrrhetinic acid-polyethylene glycol-Schiff bond-cholesterol (GPSC) has been synthesized successfully and used to construct doxorubicin (DOX)-loaded liposomes (GPSLP/DOX) with both pH-sensitive features and active targeting ability. DOX was incorporated into liposomes using a thin-film hydration method with a relatively high encapsulation efficiency (EE%) and drug loading content (LC%). Physicochemical characteristics, in vitro release behavior, cellular toxicity and cellular uptake, in vivo biodistribution as well as in vivo antitumor activities of GPSLP/DOX were investigated. GPSLP/DOX showed significantly pH-sensitive features in the in vitro release assay. All the blank liposomes were nontoxic in the in vitro cytotoxicity assay. In the MTT assay, GPSLP/DOX showed the highest cell cytotoxicity among all the groups. A cellular uptake study revealed that GPSLP/DOX could be taken up efficiently via receptor-mediated endocytosis and pH-responsive drug release of DOX into cytoplasm, which resulted in a higher cytotoxicity and therapeutical effect. An in vivo NIR fluorescence image study showed that GPSLP/DOX could specifically accumulate in the liver and tumor sites via receptor mediated endocytosis. In vivo antitumor activity results showed that this novel GPSLP/DOX could significantly inhibit tumor growth and prolong survival time due to its pH-responsive behaviour and GA-mediated endocytosis, resulting in a lower systematic toxicity and higher therapeutical effect. All these results confirm that this GA-mediated pH-sensitive GPSLP/DOX is a novel nanocarrier for the delivery of the antitumor agent DOX to reach higher toxicity effects against tumor tissue.
机译：在过去的几十年中，通过改善治疗效果，已经成功开发了pH敏感的药物递送系统以治疗癌症。在该研究中，已成功合成了一种新型pH敏缀合物甘草酸 - 聚乙二醇 - 席克酸胆固醇（GPSC）并用来用pH敏感特征构建多柔比蛋白（DOX）加载的脂质体（GPSLP / DOX）和积极的目标能力。使用具有相对高的封装效率（EE％）和药物负载含量（LC％）的薄膜水合方法将DOX掺入脂质体中。研究了在体内生物分布中的体外释放行为，细胞毒性和细胞摄取的物理化学特征，以及GPSLP / DOX的体内生物分布和体内抗肿瘤活性。 GPSLP / DOX在体外释放测定中显示出显着的pH敏感性。在体外细胞毒性测定中，所有空白脂质体都是无毒的。在MTT测定中，GPSLP / DOX在所有组中显示出最高的细胞细胞毒性。蜂窝摄取研究表明，GPSLP / DOX可以通过受体介导的内吞作用和DOX的pH-响应药物释放有效地吸收到细胞质中，导致细胞毒性和治疗效果更高。体内荧光图像研究表明，GPSLP / DOX可以通过受体介导的内吞作用明确地积聚在肝脏和肿瘤位点。体内抗肿瘤活性结果表明，由于其pH响应性行为和GA介导的内吞作用，这种新的GPSLP / DOX可以显着抑制肿瘤生长和延长存活时间，导致系统毒性较低和较高的治疗效果。所有这些结果证实，该GA介导的pH敏感的GPSLP / DOX是一种新型纳米载体，用于递送抗肿瘤剂DOX，以达到肿瘤组织的更高毒性影响。

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  • 来源
    《RSC Advances》 |2016年第22期|共10页
  • 作者

    Chen Qing; Ding Huaiwei; Zhou Jinxing; Zhao Xiufeng; Zhang Jiulong; Yang Chunrong; Li Kexin; Qiao Mingxi; Hu Haiyang; Ding Pingtian; Zhao Xiuli;

  • 作者单位

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharmaceut Engn Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Mudanjiang Med Univ Hongqi Hosp Mudanjiang 157000 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Jiamusi Univ Coll Pharm 148th Xuefu St Jiamusi 154007 Heilongjiang Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm Shenyang 110016 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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