NDLI: Interaction of the Macrolide Antibiotic Azithromycin with Lipid Bilayers: Effect on Membrane Organization, Fluidity, and Permeability

Content Provider	Springer Nature Link
Author	Berquand, A. Fa, N. Dufrêne, Y. F. Mingeot Leclercq, M. P.
Copyright Year	2005
Abstract	To investigate the effect of a macrolide antibiotic, azithromycin, on the molecular organization of DPPC:DOPC, DPPE:DOPC, SM:DOPC, and SM:Chol:DOPC lipid vesicles as well as the effect of azithromycin on membrane fluidity and permeability.The molecular organization of model membranes was characterized by atomic force microscopy (AFM), and the amount of azithromycin bound to lipid membranes was determined by equilibrium dialysis. The membrane fluidity and permeability were analyzed using fluorescence polarization studies and release of calcein-entrapped liposomes, respectively.In situ AFM images revealed that azithromycin leads to the erosion and disappearance of DPPC and DPPE gel domains, whereas no effect was noted on SM and SM:cholesterol domains. Although azithromycin did not alter the permeability of DPPC:DOPC, DPPE:DOPC, SM:DOPC, and SM:Chol:DOPC lipid vesicles, it increased the fluidity at the hydrophilic/hydrophobic interface in DPPC:DOPC and DPPE:DOPC models. This effect may be responsible for the ability of azithromycin to erode the DPPC and DPPE gel domains, as observed by AFM.This study shows the interest of both AFM and biophysical methods to characterize the drug-membrane interactions.
Starting Page	465
Ending Page	475
Page Count	11
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	22
Issue Number	3
e-ISSN	1573904X
Language	English
Publisher	Kluwer Academic Publishers-Plenum Publishers
Publisher Date	2005-03-21
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	AFM azithromycin fluidity lateral domains lipids permeability Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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