Passive lipoidal diffusion and carrier-mediated cell uptake are both important mechanisms of membrane permeation in drug disposition

Research output: Contribution to journalArticle

  • External authors:
  • Dennis Smith
  • Per Artursson
  • Alex Avdeef
  • Li Di
  • Gerhard F. Ecker
  • Bernard Faller
  • Manfred Kansy
  • Edward H. Kerns
  • Stefanie D. Krämer
  • Hans Lennernäs
  • Han Van De Waterbeemd
  • Kiyohiko Sugano
  • Bernard Testa

Abstract

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. © 2014 American Chemical Society.

Bibliographical metadata

Original languageEnglish
Pages (from-to)1727-1738
Number of pages11
JournalMolecular Pharmaceutics
Volume11
Issue number6
DOIs
Publication statusPublished - 2 Jun 2014

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