A novel chromatographic solid support with immobilized unilamellar liposomes for model analysis of solute-membrane interaction: comparison with analysis using immobilized artificial membranes and free liposomal membranes

For chromatographic system model analysis of solute-membrane interactions, large unilamellar liposomes can be stably immobilized in the pores of gel beads by avidin-biotin specific binding. Interaction of several beta -blockers, imidazoline derivatives and p-alkylphenols with the immobilized liposomal membranes was shown by their elution profiles. The solutes showed significant retardation on the liposome column compared to the liposome-free column, confirming that the solutes only interact with immobilized liposomes. The membrane partition coefficient (K-LM) of the solutes can be conveniently determined by immobilized liposome chromatography (ILC). Compared with the conventional method for determining the membrane partition coefficient in liposome suspensions, the ILC method is simple and rapid in determining the KLM values of many solutes. Compared with the use of immobilized artificial membranes (IAMs), the immobilized unilamellar liposomes used for ILC runs are more physically similar to fluid lipid bilayers. In addition, the K-LM values of several P-blockers correlated well with drug permeability through Caco-2 cells. (C) 2001 Elsevier Science B.V. All rights reserved.