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合理设计和高药载荷的相对生物性能grazoprevir无形纳米粒子配方

Joseph Della Rocca^1,2, Cory Bottone³, Majid Mahjour²

¹Discovery Pharmaceutical Sciences, Merck & Co., Inc, Rahway, NJ, USA.

Pharmaceutical development and technology

|August 7, 2025

概括

理性设计的Grazoprevir (GZP) 纳米颗粒显示出希望,其中一种配方与无形分散生物性能相匹配. 这项研究探讨了纳米粒子对药物输送和更高负载的益处.

科学领域:

制药科学制药科学
材料科学材料科学材料科学
药物运输药物运输药物运输

背景情况:

无形固体分散是像Grazoprevir (GZP) 这样的溶解不良药物常见的.
纳米粒子配方提供了改善生物性能和更高药物负载的潜力.
以前用于GZP的纳米粒子设计并没有充分利用其潜力.

研究的目的:

为了评估合理设计的无形格拉索普雷维尔 (GZP) 纳米粒子配方.
为了比较纳米粒子生物性能与无形分散配方.
使用纳米粒子探索增强的药物加载和释放配置文件.

主要方法:

使用高压均质化和共同降水,然后喷雾干燥来制造GZP纳米颗粒.
配方包括GZP-乙基纤维素和GZP-HPMCAS-L与SLS.
鉴定包括超离心,FIB-SEM,溶解研究和狗药理动力学 (PK) 研究.

主要成果:

GZP-乙基纤维素纳米颗粒显示出快速释放,但范围有限,无法匹配无形分散性能.
GZP-HPMCAS-L/SLS纳米粒子 (45/45/10) 由由辅助剂稳定的纯无形药物组成.
45/45/10 GZP-HPMCAS-L/SLS配方与无形分散药物释放率和程度相匹配,在体内达到相当的PK.

结论:

与传统的无形分散相比,直接设计的纳米粒子配方可以实现更高的生物性能.
45/45/10 GZP/HPMCAS-L/SLS纳米颗粒配方证明了Grazoprevir药物传递改善的潜力.
纳米粒子技术为更高的药物负载和潜在的较小剂量形式提供了可行的策略.

关键词:

无形固体分散的分散.增强生物可用性增强生物可用性药物输送是药物输送的过程.这种药物是grazoprevir.纳米颗粒是一种纳米粒子.

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