Drug Partitioning in lipid bilayers

The interaction of therapeutic agents with lipid membranes determines their pharmacokinetic characteristics as well as their distribution within organs and cells, respectively, i.e. between membrane domains of particular lipid composition and aqueous compartments of particular pH values. The affinity of low molecular compounds to lipid bilayers of defined lipid composition is studied in a liposome/buffer system in combination with bilayer permeation and/or with the interaction of the compound with the efflux protein P-glycoprotein. With this approach, the known phospholipidosis-reversing effect of alpha-tocopherol could be assigned to its striking effect on the lipid bilayer affinity of the neutral forms of basic lipophilic drugs.

ETH Research Database: id 8911
Contacts: Prof. Dr. Heidi Wunderli-Allenspach, Dr. Stefanie Krämer