通过pH驱动的脂质体封装改善了urolithin A的稳定性,生物可访问性和生物可用性:一项比较研究
Yue Hu1, Lu Zhang2, Lin-Feng Wei1
1National R&D Center of Freshwater Fish Processing, College of Life Science, Jiangxi Normal University, Nanchang, Jiangxi 330022, China.
International journal of biological macromolecules
|October 21, 2023
概括
与传统方法相比,使用pH驱动方法制备的urolithin A (UroA) 脂质体显示出更好的稳定性和生物可用性. 这种新的方法提高了UroA的交付,用于潜在的治疗应用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
- 生物化学 生物化学
背景情况:
- 乌罗立A (UroA) 具有多种生物活性.
- 较差的水溶性和较低的生物可用性限制了UroA的治疗潜力.
- 埃拉基坦宁是UroA肠道代谢物的前体.
研究的目的:
- 开发一种pH驱动的方法来将UroA加载到脂质体中.
- 为了提高UroA.的稳定性和口服生物可用性.
- 为了比较新的pH驱动方法脂质体 (PDM-ULs) 与传统的薄膜分散脂质体 (TFM-ULs).
主要方法:
- 利用了UroA.的pH依赖性溶解特性.
- 封装的UroA通过pH驱动的方法进入脂质体.
- 特征性脂肪体属性 (大小,PDI,泽塔潜力,封装效率).
- 评估了脂质体的稳定性 (热,储存,体外消化) 和生物可访问性.
- 通过对大鼠进行的药理动力学研究来评估口服生物可用性.
主要成果:
- 脂质体有效地封装了UroA.
- PDM-ULs具有较小的粒子大小,较低的PDI和zeta潜力,与TFM-ULs相比,封装效率更高.
- PDM-ULs表现出优越的热,储存和体外消化稳定性.
- PDM-ULs显示显著增强生物可访问性和口服生物可用性 (1.91倍TFM-ULs).
结论:
- 这种pH驱动的方法是有效的准备UroA载荷的脂质体.
- PDM-ULs显著提高了UroA的稳定性和口服生物可用性.
- 这种脂质体配方有望增强UroA的治疗应用.
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