在自我乳化药物输送系统中辅助剂毒性和耐受性:基于细胞的测试的见解
Marlene Ramona Schmidt1, Magdalena Ender1, Melanie Lena Ebert1
1Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.
International journal of pharmaceutics
|February 7, 2026
概括
选择合适的辅助剂对于开发安全的自我乳化药物输送系统 (SEDDS) 是至关重要的. 这项研究表明,辅助剂的化学结构显著影响细胞耐受性,指导生物相容配方的设计,并最大限度地减少药物不良反应.
科学领域:
- 制药科学 制药科学
- 毒理学 毒理学 毒理学
- 生物相容性研究 生物相容性研究
背景情况:
- 辅助剂毒理评估对于自乳化药物输送系统 (SEDDS) 的开发至关重要.
- 了解辅助剂对细胞耐受性的影响,是设计生物相容SEDDS的关键.
- 这项研究调查了SEDDS助剂的物理化学特性,氧化稳定性和生物兼容性.
研究的目的:
- 在SEDDS配方中确定影响细胞耐受性的关键因素.
- 评估各种油,辅溶剂和表面活性剂的生物兼容性.
- 为了确定SEDDS中辅助剂毒性的结构-活性关系.
主要方法:
- 使用动态光散射进行物理化学表征.
- 通过氧化物量化的氧化稳定性评估.
- 在CaCo-2和HEK-293细胞中进行生物兼容性测试,包括血液溶解试验和细胞活力 (MTT).
主要成果:
- 和甘油三醇显示出比自由脂肪酸更高的细胞活力.
- 配溶剂毒性与脂性有所不同;异醇导致早期的膜应激,甘油诱导延迟的血液溶解.
- 基于PEG的表面活性剂表现出比脂肪酒精和基于糖的配方更好的生物相容性,与较低的过氧化物水平相关.
结论:
- 辅助剂的选择显著影响细胞应激和潜在的不良药物反应在基于脂质的口服输送.
- 诸如和甘油三和基于PEG的表面活性剂之类的特定辅助剂提供了更好的生物相容性.
- 了解辅助剂结构-活性关系对于优化SEDDS安全性和有效性至关重要.
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