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Interaction of the macrolide antibiotic azithromycin with lipid bilayers: effect on membrane organization, fluidity,

A Berquand1, N Fa, Y F Dufrêne

  • 1Unité de Chimie des Interfaces, Université Catholique de Louvain, B-1348 Louvain-la-Neuve, Belgium.

Pharmaceutical Research
|April 20, 2005
PubMed
Abstract

Insights

Azithromycin (a macrolide antibiotic) erodes DPPC and DPPE lipid domains but not SM domains in model membranes. It increases membrane fluidity without affecting permeability, highlighting its drug-membrane interaction effects.

Area of Science:

  • Biophysics
  • Pharmacology
  • Materials Science

Background:

  • Lipid bilayers are crucial for cell function.
  • Understanding drug-lipid interactions is vital for drug development.
  • Azithromycin is a widely used macrolide antibiotic.

Purpose of the Study:

  • To investigate azithromycin's effects on model lipid membranes (DPPC:DOPC, DPPE:DOPC, SM:DOPC, SM:Chol:DOPC).
  • To assess azithromycin's impact on membrane molecular organization, fluidity, and permeability.

Main Methods:

  • Atomic Force Microscopy (AFM) for molecular organization.
  • Equilibrium dialysis for azithromycin binding.
  • Fluorescence polarization for membrane fluidity.
  • Calcein-entrapped liposomes for permeability.

Main Results:

  • Azithromycin eroded DPPC and DPPE gel domains but not SM or SM:cholesterol domains.
  • Azithromycin did not alter vesicle permeability.
  • Increased fluidity at the hydrophilic/hydrophobic interface was observed in DPPC:DOPC and DPPE:DOPC models.

Conclusions:

  • Azithromycin's interaction with lipid membranes involves erosion of specific lipid domains.
  • Increased membrane fluidity may explain the observed domain erosion.
  • AFM and biophysical methods are valuable for characterizing drug-membrane interactions.

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