Evaluation of sphingomyelin, cholester, and phosphatidylcholine-based immobilized artificial membrane liquid chromatography to predict drug penetration across the blood-brain barrier
Evaluation of sphingomyelin, cholester, and phosphatidylcholine-based immobilized artificial membrane liquid chromatography to predict drug penetration across the blood-brain barrier
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DOI：
10.1007/s00216-014-8054-7
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发表时间：
2014-10-01
影响因子：
4.3
通讯作者：
Lynen, Frederic
中科院分区：
文献类型：
--
作者：
De Vrieze, Mike;Verzele, Dieter;Lynen, Frederic
在过去的几十年中，已经测试了几种体外方法预测药物穿过血脑屏障的能力。迄今为止，在高效液相色谱中，最受关注的是胶束液相色谱和固定化人工膜液相色谱。IAMLC已被描述为一种可行的方法，因为固定相模拟细胞膜的脂质环境。然而，IAMLC的研究几乎完全限于基于磷脂酰胆碱（PC）的固定相，即使PC只是存在于细胞膜中的脂质之一。在这篇文章中，鞘磷脂和胆固醇固定相已被测试的第一次对他们的能力，以预测药物渗透通过血脑屏障。在与PC固定相比较后，鞘磷脂和胆固醇为基础的列描绘了类似的预测性能。将来自不同固定相的数据结合并没有导致模型的改进。
Over the past decades, several in vitro methods have been tested for their ability to predict drug penetration across the blood-brain barrier. So far, in high-performance liquid chromatography, most attention has been paid to micellar liquid chromatography and immobilized artificial membrane (IAM) LC. IAMLC has been described as a viable approach, since the stationary phase emulates the lipid environment of a cell membrane. However, research in IAMLC has almost exclusively been limited to phosphatidylcholine (PC)-based stationary phases, even though PC is only one of the lipids present in cell membranes. In this article, sphingomyelin and cholester stationary phases have been tested for the first time towards their ability to predict drug penetration across the blood-brain barrier. Upon comparison with the PC stationary phase, the sphingomyelin- and cholester-based columns depict similar predictive performance. Combining data from the different stationary phases did not lead to improvements of the models.