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瘤透性自我递送纳米药物针对线粒体进行增强化疗

Guiping Yuan¹, Yifan Zhang¹, Shiqun Shao²

¹Zhejiang Key Laboratory of Smart Biomaterials and Center for Bionanoengineering, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310058, China; Key Laboratory of Biomass Chemical Engineering of the Ministry of Education, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310058, China.

Journal of controlled release : official journal of the Controlled Release Society

|August 18, 2023

概括

一种新型的ROS响应前药物 (CPT-S-NO) 增强了瘤向和透. 这种药物自我递送系统 (DSDS) 有效地准线粒体,提高了抗瘤功效.

科学领域:

生物材料科学生物材料科学
纳米医学是一种纳米医学.
药物运输药物运输药物运输

背景情况:

药物自我递送系统 (DSDS) 提供优势,但在瘤向,透和控制释放方面面临挑战.
现有的DSDS通常会出现突发释放和非特异分布等问题,限制其治疗潜力.

研究的目的:

为提高DSDS性能开发一种新型ROS响应的两前药物 (CPT-S-NO).
评估CPT-S-NO在增强瘤积累,透和线粒体向优异抗瘤活性方面的疗效.

主要方法:

通过一个 thioether 连接合成一种 zwitterionic 三级氨基氧化物 (TAO) 修饰的坎普托西因 (CPT) 前药物 (CPT-S-NO).
在体外和体外评估CPT-S-NO的药理学特征,瘤向,透和ROS激活释放.
与对照组 (CPT-11和CPT-NO) 相比,线粒体功能障碍和抗瘤疗效的评估.

主要成果:

在水溶液中,CPT-S-NO形成了稳定的纳米粒子,显示出长时间的血液循环.
对于CPT-S-NO.观察到增强的瘤积累,深的瘤透和高效的线粒体向.
由ROS激活的药物释放导致线粒体功能障碍和优异的体内抗瘤疗效.

结论:

在TAO装饰策略有效地创建一个多功率的DSDS与改善的治疗结果.
通过克服传统DSDSs的局限性,CPT-S-NO显示了先进癌症治疗的巨大潜力.
这种方法为为各种治疗剂设计下一代DSDS提供了一个有前途的平台.

关键词:

主动瘤透活动.坎普托塞辛是一种前药物.药物自递送系统是药物自递送系统.线粒体向向的目标三级氨基氧化物三级氨基氧化物

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