Albumin enhances the diffusion of lipophilic drugs into the membrane bilayer.
In earlier work, we reported on the manner with which lipophilic drug molecules interact with the cell membrane in order to (a) enter the bilayer and laterally diffuse to their respective protein sites of action, or (b) penetrate this biological barrier to reach the cell interior. A remaining uncertainty is how lipophilic molecules reach the hydrophobic membrane core after traversing the aqueous medium and membrane polar surface. Here we present preliminary data using deuterium NMR, demonstrating the role of bovine serum albumin in facilitating this process. Our observation allows us to postulate a mechanism by which the passive transport of lipophilic ligands across the membrane can be greatly enhanced through the assistance of carrier proteins.
Makriyannis
Alexandros
A
Center for Drug Discovery and Department of Pharmaceutical Sciences and Chemistry, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, United States. a.makriyannis@neu.edu
Guo
Jianxin
J
Tian
Xiaoyu
X
D000418:Albumins / Q000494:pharmacology*; D001692:Biological Transport / Q000187:drug effects / Q000502:physiology; D002462:Cell Membrane / Q000378:metabolism*; D003903:Deuterium; D004058:Diffusion; D013759:Dronabinol / Q000737:chemistry / Q000378:metabolism*; D008051:Lipid Bilayers / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy
D000418:Albumins; D008051:Lipid Bilayers; D013759:Dronabinol; D003903:Deuterium