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

Smith, D, Artursson, P, Avdeef, A, Di, L, Ecker, GF, Faller, B, Houston, JB, Kansy, M, Kerns, EH, Kramer, SD, Lennernas, H, Van De Waterbeemd, H, Sugano, K and Testa, B (2014) Passive lipoidal diffusion and carrier-mediated cell uptake are both important mechanisms of membrane permeation in drug disposition. Molecular Pharmaceutics. pp. 1727-1738.


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

Item Type: Article
Additional Information: NIBR author: Faller, B institute: NIBR contributor address: (Smith) 4 The Maltings, Walmer-Kent-CT14-7AR, United Kingdom (Artursson, Lennernas) Department of Pharmacy, Biomedical Centre, Uppsala University, S-752 63 Uppsala, Sweden (Avdeef) 1732 First Avenue, #102, New York, NY 10128, United States (Di) Pharmacokinetics, Dynamics and Metabolism, Pfizer Inc., Groton, CT 06340, United States (Ecker) Department of Medicinal Chemistry, University of Vienna, Althanstrasse, 141090 Wien, Austria (Faller) Novartis Institutes for Biomedical Research, WSJ-350.3.04, CH-4002 Basel, Switzerland (Houston) School of Pharmacy and Pharmaceutical Sciences, University of Manchester, Oxford Road, Manchester, M13 9PT, United Kingdom (Kansy) Non-Clinical Safety Department, F. Hoffmann-La Roche, CH-4070 Basel, Switzerland (Kerns) National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, MD 20850, United States (Kramer) Institute of Pharmaceutical Sciences, ETH, Zurich, Switzerland (Van De Waterbeemd) 14 Rue de la Rasclose, 66690 Saint Andre, France (Sugano) Research Formulation, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom (Testa) Department of Pharmacy, University Hospital Lausanne, CH-1011 Lausanne, Switzerland (Kerns) 21705 Mobley Farm Drive, Laytonsville, MD 20882, United States
Date Deposited: 13 Oct 2015 13:12
Last Modified: 13 Oct 2015 13:12


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