Immobilized biomembrane chromatography of highly lipophilic drugs

Drug interaction with lipid bilayers was quantified by immobilized biomembrane chromatography on a series of columns containing different small amounts of human red cell membrane vesicles to extend and characterize this technique, which shows a potential for drug screening and prediction of drug absorption in humans. The chromatographic retention volume for each drug was essentially proportional to the amount of immobilized lipid, and the slope equalled 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. Highly lipophilic drugs could thus be analyzed conveniently in aqueous buffer. (C) 1999 Elsevier Science B.V. All rights reserved.