Immobilized biomembrane chromatography of highly lipophilic drugs

Drug interaction with lipid bilayers was quantified by immobilized biomembr ane chromatography on a series of columns containing different small amount s of human red cell membrane vesicles to extend and characterize this techn ique, which shows a potential for drug screening and prediction of drug abs orption in humans. The chromatographic retention volume for each drug was e ssentially proportional to the amount of immobilized lipid, and the slope e qualled the capacity factor (K-s) previously determined on single columns. Gel beds containing 0.5-2 pmol of membrane phospholipid allowed analysis of drugs with log K-s values of 2.5-4.3 in time periods of 1 min to 1 h. High ly lipophilic drugs could thus be analyzed conveniently in aqueous buffer. (C) 1999 Elsevier Science B.V. All rights reserved.