Transport of the neutral form of amphiphilic drugs through a planar bilayer lipid membrane: The role of the pH gradient |
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| Institution: | 1. Department of Chemical Engineering, The University of Melbourne, Parkville, Melbourne 3010, Australia;2. Department of Chemical Engineering, The University of Texas at Austin, Austin, TX 78712, United States;1. Particle and Interfacial Technology Group, Ghent University, Belgium;2. Facultad del Mar y Medio Ambiente, Universidad del Pacifico, Ecuador;3. Masdar Institute, Khalifa University of Science and Technology, United Arab Emirates;1. Technische Universität Dresden, Institute of Construction Materials, DE-01062 Dresden, Germany;2. Paul Scherrer Institut, Department of Spallation Neutron Source (ASQ), CH-5232 Villigen/AG, Switzerland;1. Department of Atmospheric Sciences, National Central University, Chung–Li, Taiwan;2. Institute of Space Science, National Central University, Chung–Li, Taiwan |
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| Abstract: | The inner field compensation (IFC) method was used to measure the dependence of the boundary potential (BP) difference of a bilayer lipid membrane (BLM) on remantadin concentration. It was found that the BP difference depended on the pH gradient and the buffer capacity of the solution. The addition of remantadin at one side of the membrane caused changes in the pH values in the unstirred layers near both surfaces of the membrane. These changes were detected by means of measurement of the transmembrane open circuit potential in the presence of the protonophore pentachlorphenol. The sign of the transmembrane potential corresponded to a pH decrease on the membrane cis-side (where REM was added) and a rise on the irons-side. There was no increase in the membrane conductance due to the remantadin addition.A model of remantadin penetration through the lipid membrane is proposed. According to this model, the neutral form of the drug passes through the membrane. The formation and decomposition reactions of the neutral form, taking place at the membrane boundaries, are accompanied by the ejection and sorption of protons, respectively. The pH changes in lyzosomes or receptosomes due to remantadin penetration are discussed within the framework of the resulting model. |
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