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Passive Lipoidal Diffusion and Carrier-Mediated Cell Uptake Are Both Important Mechanisms of Membrane Permeation in Drug Disposition
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
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2014 (English)In: Molecular Pharmaceutics, ISSN 1543-8384, Vol. 11, no 6, 1727-1738 p.Article, review/survey (Refereed) Published
Abstract [en]

Recently, it has been proposed that drug permeation is essentially carrier-mediated only and that passive lipoidal diffusion is negligible. This opposes the prevailing hypothesis of drug permeation through biological membranes, which integrates the contribution of multiple permeation mechanisms, including both carrier-mediated and passive lipoidal diffusion, depending on the compound's properties, membrane properties, and solution properties. The prevailing hypothesis of drug permeation continues to be successful for application and prediction in drug development. Proponents of the carrier-mediated only concept argue against passive lipoidal diffusion. However, the arguments are not supported by broad pharmaceutics literature. The carrier-mediated only concept lacks substantial supporting evidence and successful applications in drug development.

Place, publisher, year, edition, pages
2014. Vol. 11, no 6, 1727-1738 p.
Keyword [en]
permeation, passive lipoidal diffusion, "carrier-mediated only" concept
National Category
Pharmacology and Toxicology
URN: urn:nbn:se:uu:diva-228525DOI: 10.1021/mp400713vISI: 000336941900001OAI: oai:DiVA.org:uu-228525DiVA: diva2:734318
Available from: 2014-07-16 Created: 2014-07-16 Last updated: 2014-07-16Bibliographically approved

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Artursson, PerLennernäs, Hans
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