Transport of the neutral form of amphiphilic drugs through a planar bilayer lipid membrane. The role of the pH gradient

V. V. Cherny, M. V. Simonova, V. S. Sokolov, V. S. Markin

Research output: Contribution to journalArticle

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 trans-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.

Original languageEnglish (US)
Pages (from-to)17-25
Number of pages9
JournalJournal of Electroanalytical Chemistry
Volume298
Issue number1
DOIs
StatePublished - 1990

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Lipid bilayers
Membrane Lipids
Membranes
Pharmaceutical Preparations
Protons
Sorption
Buffers
Decomposition
Networks (circuits)

ASJC Scopus subject areas

  • Chemical Engineering(all)
  • Analytical Chemistry
  • Electrochemistry

Cite this

Transport of the neutral form of amphiphilic drugs through a planar bilayer lipid membrane. The role of the pH gradient. / Cherny, V. V.; Simonova, M. V.; Sokolov, V. S.; Markin, V. S.

In: Journal of Electroanalytical Chemistry, Vol. 298, No. 1, 1990, p. 17-25.

Research output: Contribution to journalArticle

Cherny, V. V. ; Simonova, M. V. ; Sokolov, V. S. ; Markin, V. S. / Transport of the neutral form of amphiphilic drugs through a planar bilayer lipid membrane. The role of the pH gradient. In: Journal of Electroanalytical Chemistry. 1990 ; Vol. 298, No. 1. pp. 17-25.
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