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Passive Lipoidal Diffusion and Carrier-Mediated Cell Uptake Are Both Important Mechanisms of Membrane Permeation in Drug Disposition

Faller, Bernard and Artursson, Per and Avdeef, Alex and Li, Di and Ecker, Gerhard and Houston, Brian and Kansy, Manfred and Kerns, Ed and Kraemer, Stefanie and Lennernaes, Hans and van de Waterbeemd, Han and Sugano, Kiyohiko and Testa, Bernard (2014) Passive Lipoidal Diffusion and Carrier-Mediated Cell Uptake Are Both Important Mechanisms of Membrane Permeation in Drug Disposition. Molecular Pharmacology, 11 (-). pp. 1727-1738. ISSN -

Abstract

This commentary discusses the prevailing permeation hypothesis, which we conclude is consistent with the experimental data. Importantly, this commentary also addresses uncertainties among drug researchers that result from recent articles (Dobson, 2008, 2009; Kell, 2011, 2013) from a group that assert the carrier-mediated only concept (CMOC) of drug permeation and attempt to invalidate passive lipoidal diffusion across biological membranes into cells and across cell layer membranes. We conclude CMOC lacks sufficient evidence. CMOC is not a sound scientific principle and lacks experimental evidence. Carrier-mediated transport and passive lipoidal diffusion permeation mechanisms are complementary, their relative contribution depending on many physicochemical and biochemical factors (e.g., concentration gradient, lipophilicity and hydrogen bonding of the diffusing compound, transporter affinity and Km).

Item Type: Article
Date Deposited: 12 Oct 2016 00:45
Last Modified: 12 Oct 2016 00:45
URI: https://oak.novartis.com/id/eprint/20214

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