Lipid-itraconazole interaction in lipid model membranes

Itraconazole, a lipophilic, fungal sterol-biosynthesis inhibitor, does not disturb membrane organization parameters measured by differential scanning calorimetry and infrared spectroscopy. Conformational analysis studies suggest that the molecular volume and the position of itraconazole in the lipid...

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Bibliographic Details
Published in:	Journal of pharmacy and pharmacology Vol. 43; no. 3; p. 167
Main Authors:	Brasseur, R, Goormaghtigh, E, Ruysschaert, J M, Duquenoy, P H, Marichal, P, Vanden Bossche, H
Format:	Journal Article
Language:	English
Published:	England 01-03-1991
Subjects:	1,2-Dipalmitoylphosphatidylcholine - chemistry Calorimetry, Differential Scanning Itraconazole Ketoconazole - analogs & derivatives Ketoconazole - chemistry Lipids - chemistry Membranes, Artificial Molecular Conformation Phospholipids - chemistry Spectrophotometry, Infrared
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Summary:	Itraconazole, a lipophilic, fungal sterol-biosynthesis inhibitor, does not disturb membrane organization parameters measured by differential scanning calorimetry and infrared spectroscopy. Conformational analysis studies suggest that the molecular volume and the position of itraconazole in the lipid membrane is similar to that of dipalmitoyl phosphatidylcholine. The mean energy of interaction between itraconazole and the phospholipid is -60.6 kJ mol-1 whereas this energy in the pure lipid matrix is -54.3 kJ mol-1. The mean molecular area of itraconazole calculated by projecting the molecule on the lipid-water interface is equal to that occupied by the pure lipid (60 A2/molecule).
ISSN:	0022-3573
DOI:	10.1111/j.2042-7158.1991.tb06659.x