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混合干逆:通过SEDDS提供口服蛋白质的潜在载体

Fabrizio Ricci¹, Sera Lindner¹, Simona Summonte¹

¹Thiomatrix Forschungs-und Beratungs GmbH, Trientlgasse 65, Innsbruck, 6020, Austria.

Drug delivery and translational research

|February 18, 2025

概括

混合干逆 (dRMs) 增强了自我乳化药物递送系统 (SEDDS) 的治疗性蛋白质脂性. 这种方法显著增加了蛋白质的负载和稳定性,为口服蛋白质的输送铺平了道路.

科学领域:

制药科学制药科学
生物技术是生物技术.
药物输送系统药物输送系统

背景情况:

治疗性蛋白质通常需要增强的传递系统进行口服,因为脂友性差和酶降解.
自乳化药物输送系统 (SEDDS) 提供了口服输送的潜力,但在结合水友蛋白质方面面临着挑战.
干逆 (dRMs) 提供了一种新的方法来修改蛋白质特性以改善配方.

研究的目的:

评估混合干逆 (dRMs) 在提高治疗蛋白质的脂友性方面的有效性.
评估将含蛋白质的dRM纳入自我乳化药物递送系统 (SEDDS) 的情况.
调查dRMs装载的SEDDS对酶降解的稳定性和保护能力.

主要方法:

马过氧化酶 (HRP) 被封装在混合的dRM中,使用大豆酸丁胆 (SPC) 和酸 (SD).
在模拟生理流体中,HRP-dRMs的分布系数和稳定性得到了特征.
将HRP-dRMs装入SEDDS,然后对有效载荷,稳定性,分布系数和酶保护进行表征.

主要成果:

表面活性剂在dRMs中的协同效应使得在没有有机辅溶剂的SEDDS中实现了高蛋白有效载荷 (3%w/v).
加入HRP-dRMs显著增加了HRP的脂友性 (LogD),从-3.36增加到3.10.
超过95%的内置蛋白质在暴露于青素和化学青素后保持完整,显示出增强的稳定性.

结论:

混合dRM有效地增加治疗性蛋白质脂友性,并促进它们纳入SEDDS.
这种dRM-SEDDS方法允许前所未有的高分子量蛋白质加载,比以前的方法增加了15倍.
这些发现表明dRMs是口服治疗蛋白质输送的有希望的工具.

关键词:

疏水离子离子配对口服药物输送是通过口服药物进行的.自体乳化药物输送系统自体乳化药物输送系统治疗性蛋白质是一种治疗性蛋白质.

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