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Biophys Chem. 1981 Jun;13(3):253-64. doi: 10.1016/0301-4622(81)80007-5.

Interaction of some charged amphiphilic drugs with phosphatidylcholine vesicles. A spin label study of surface potential effects.

Biophysical chemistry

L E Eriksson, J Westman

Affiliations

  1. Department of Biophysics, University of Stockholm, Arrhenhis Laboratory, S-106 91 Stockholm, Sweden.

PMID: 17000169 DOI: 10.1016/0301-4622(81)80007-5

Abstract

Adsorptions of amphiphilic drugs (propranolol, alprenolol, metoprolol and tetracaine) to phosphalidylcholine vesicles in media of different pH and NaCl concentrations have been studied. A positively charged spin label amphiphile, N,N-di-methyl-N-nonyl-N-tempoylammoniumbromide, was used to follow the variation in the surface potential by ESR. Competition experiments between the probe molecule and the drugs were carried out. A spin-labeled analogue of propranolol was also employed. We have analysed the results in terms of the theory for the diffuse double layer (Gouy-Chapman) and treated various equilibrium models. A weak, specific adsorption of chloride ions was introduced. For the charged forms of the drugs simulations of the experiments by numerical solution of the system of equations in a satisfactory way furnished intrinsic binding constants, independent of surface potential effects. The common electrostatic surface potential is mainly ruling the competition, and not the number of surface vacancies.

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