Immobilized-liposome chromatographic analysis of drug partitioning into lipid bilayers.

The chromatographic retardation of drugs on a gel bed with immobilized liposomes was shown to correlate with the absorption of the drugs through epithelial cell layers, which is related to drug partitioning into the lipid bilayers of cell membranes. The capacity factors were divided by the lipid concentration (mM) in the gel bed to obtain specific capacity factors, Ks. The logarithm of the octanol-water distribution ratios showed a linear correlation with log Ks, whereas the logarithm of the apparent permeability coefficients in epithelial cell monolayers and the absorption of drugs orally administered in humans (data from other laboratories) increased over the interval 0 < log Ks < 1 and attained a saturation level in the interval 1 < log Ks < 3. Immobilized-liposome chromatography may be applicable for prediction of drug uptake through epithelial cell membranes.