Predicting drug penetration across the blood-brain barrier: comparison of micellar liquid chromatography and immobilized artificial membrane liquid chromatography

Several in vitro methods have been investigated for mimicking drug penetration across the blood-brain barrier (BBB) into the central nervous system (CNS). Both micellar liquid chromatography (MLC) and immobilized artificial membrane (IAM) liquid chromatography were tested in this contribution in order to construct models for BBB transfer prediction. MLC measurements were performed on a C18-column with sodium dodecyl sulfate (SDS), polyoxyethylene (23) lauryl ether (Brij35) or sodium deoxycholate (SDC) as surfactants in the micellar mobile phase. IAM liquid chromatography measurements were performed with a Dulbecco’s phosphate-buffered saline (DPBS) and a certain percentage of methanol as organic modifier in the mobile phase. This study aimed to obtain a high correlation between in vivo and predicted log BB values (= concentration of the drug molecule in the brain to concentration in the blood).