PMID: 8443332Feb 1, 1993Paper

Local anesthetic-phospholipid interactions. Effects of ionic strength, temperature, and phospholipid mixtures on the binding of dibucaine to phospholipids

Biophysical Chemistry
S BarghouthiM R Eftink

Abstract

The nature of the interaction of amphipathic drugs, such as dibucaine, with phospholipid bilayer membranes was investigated using equilibrium dialysis. Profiles for the binding of cationic dibucaine to unilamellar vesicles were obtained at different temperature and ionic strengths, and for mixtures of neutral phospholipid dimyristylphosphatidylcholine (DMPC) with negatively charged dimyristylphosphatidylglycerol (DMPG). The degree of binding of the cationic drug at pH 5 was found to be higher at temperatures above the Tm of DMPC (24 degrees C) than below Tm. Also enhanced drug binding was found to occur as the concentration of monovalent salt was increased (0.01-0.85 M) and as the percentage of DMPG was increased. Using the Stern and Guoy-Chapman model, which takes into consideration electrostatic effects, we were able to simultaneously fit all our binding data with a minimum of fitting parameters. These parameters (for data at 45 degrees C) are an association constant, K, of 330 M-1, a maximum possible number of drug molecules absorbed per unit surface of vesicle, sigma m+, of 1.70 x 10(-2) A2, and a surface area per bound drug, gamma D, of 48 A2. The data were fitted equally well by an alternate model in which binding of the ...Continue Reading

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Feb 1, 1993·Biophysical Chemistry·S Barghouthi, M R Eftink

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Citations

Mar 9, 2007·European Biophysics Journal : EBJ·G SchwarzM Winterhalter
Mar 15, 2001·Biochimica Et Biophysica Acta·M MondalA Chakrabarti
Aug 2, 2000·International Journal of Biological Macromolecules·C M GómezC Abad
Dec 18, 2002·Journal of Pharmaceutical Sciences·Iolanda PorcarAgustín Campos
May 13, 2008·Langmuir : the ACS Journal of Surfaces and Colloids·Pieter SaveynPaul Van der Meeren
Feb 1, 1993·Biophysical Chemistry·S Barghouthi, M R Eftink
Nov 18, 2005·Journal of Colloid and Interface Science·Clara M GómezConcepción Abad
Jan 19, 1994·Biochimica Et Biophysica Acta·S R LouroO R Nascimento
Jun 3, 2004·Chemistry and Physics of Lipids·Mousumi Mondal, Abhijit Chakrabarti

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