...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>ACS applied materials & interfaces >Design of pH-Sensitive Nanovesicles via Cholesterol Analogue Incorporation for Improving in Vivo Delivery of Chemotherapeutics
【24h】

Design of pH-Sensitive Nanovesicles via Cholesterol Analogue Incorporation for Improving in Vivo Delivery of Chemotherapeutics

机译：通过胆固醇类似物掺入改善化学治疗剂的pH敏感纳米粒子

获取原文
获取原文并翻译 | 示例
   

获取外文期刊封面封底 >>

       
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

pH-responsive polymersomes have emerged as promising nanocarriers for antitumor drugs to realize their fast release and action in a weakly acidic microenvironment of tumor cells. Herein, however, we designed a remarkably pH-responsive polymersome self-assembled from amphiphilic benzimidazole-based polyphosphazenes via the incorporation of cholesteryl hemisuccinate (CholHS), a type of cholesteric molecule, into the polymersome bilayers to inhibit the drug release during blood circulation. Actually, unwanted premature drug leakage before arriving at the acidic tumor site has become a serious problem for polymersomes encapsulating water-soluble drugs, especially when the drug loading is at a high level, thus limiting the therapeutic efficacy. In this study, polymersomes displayed high loading capability of doxorubicin hydrochloride as 12.83%. More importantly, CholHS incorporation decreased the membrane permeability of the polymersome and effectively retarded the cargo release under physiological conditions but induced the fast drug-release rate at pH 5.5, demonstrating a more remarkably acid-responsive release behavior when compared to that of the CholHS-free polymersomes. Further in vivo investigations including pharmacokinetic and antitumor activity studies verified the extended circulation time and enhanced antitumor efficacy of the drug-loaded CholHS-incorporated polymersomes.
机译：pH-响应聚合物已经出现为抗肿瘤药物的有前途的纳米载体，以实现它们在肿瘤细胞的弱酸性微环境中的快速释放和作用。然而，在本文中，我们设计了一种显着的pH-响应性聚合物，通过掺入胆气甾醇的半眼（Cholhs），一种胆甾型分子，进入聚合物组双层，以抑制血液循环期间的药物释放的显着pH-响应性聚合物组合物。实际上，在到达酸性肿瘤部位之前的不需要的过早药物泄漏已成为包封水溶性药物的聚合物的严重问题，特别是当药物载荷处于高水平时，因此限制了治疗效果。在该研究中，聚合物显示盐酸辛酸多柔比星的高负载能力为12.83％。更重要的是，Cholhs掺入降低了聚合物的膜渗透性，并有效地将货物释放在生理条件下抑制，但与胆管的含量诱导在pH5.5时的快速药物释放速率，显示出更显着的酸性响应释放行为 - 游离聚合物。此外，在体内研究包括药代动力学和抗肿瘤活性研究，验证了延长的循环时间和增强药物胆量掺入聚合物的抗肿瘤效果。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号