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链接剂对通过活跃点击加载制备的脂质体dcetaxel-glutathione的发展的影响

Qing Zhou¹, Hailong Ma², Wei Luo²

¹Department of Respiratory and Critical Care Medicine, West China Hospital, Sichuan University, Chengdu 610041 China; Department of Respiratory and Critical Care Medicine, The Second Affiliated Hospital of Chengdu Medical College, Nuclear Industry 416 Hospital, Chengdu 610051 China.

International journal of pharmaceutics

|January 21, 2025

概括

连接多塞塔塞尔 (DTX) 与马利米德 (MAL) 的链接器显著影响脂质体配方. 在乳腺癌模型中,优化链接器可以增强药物加载,释放和强大的抗瘤活性.

科学领域:

制药科学制药科学
药物运输药物运输药物运输
纳米技术纳米技术

背景情况:

脂质体配方提供了一个可行的策略来封装像多塞塔克塞尔 (DTX) 这样的药物.
使用药物-马利胺 (MAL) 结合物和谷氨 (GSH) 的活跃点击加载是制备脂质体药物配方的一种方法.
将药物连接到maleimide部分的链接器对脂质体系统发育的影响尚未完全理解.

研究的目的:

调查不同链接剂对多塞塔克塞尔载脂质体 (DTX-LIPs) 的特性和疗效的影响.
了解链接器特征如何影响药物加载,释放动力学和体内抗瘤活性.

主要方法:

通过使用各种链接剂合成多塞塔克塞尔-马莱胺 (DTX-MAL) 结合物.
将DTX-MAL合物加载到预装谷氨酸 (GSH) 的脂质体中.
在4T1乳腺癌异种移植模型中评估药物加载效率,体外药物释放概况和体内抗瘤疗效.

主要成果:

链接剂显著影响了DTX-MAL合物的水溶性,影响了脂质体负载效率.
链接器选择通过影响GSH结合原药的激活率来调节脂质体中DTX的释放率.
与快速激活的DTX-GSH一起的脂质体DTX-GSH (DTX-LIPs) 与其他配方和商业DTX相比表现出更好的抗瘤活性.

结论:

链接剂在药物加载,释放动力学和通过活性点击加载制备的脂质体配方的抗瘤疗效方面发挥着关键作用.
合理的链接器设计对于优化脂质体药物的性能和改善治疗结果至关重要.
产药激活被确定为药物释放机制中从这些脂质体释放的速度限制步骤.

关键词:

抗瘤疗效抗瘤疗效点击加载进行加载.多塞塔克塞尔 (Docetaxel) 是一种药物.药物释放药物释放的时间链接器链接器脂质体是一种脂质体.

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