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Chlorhexidine Effects on Membrane Lipid Domains of Human Buccal Epithelial Cells

Department of Pharmaceutical Chemistry, School of Pharmacy, The University of Kansas, Lawrence, Kansas 66045

M.R. Tavakoli-Saberi

Department of Pharmaceutical Chemistry, School of Pharmacy, The University of Kansas, Lawrence, Kansas 66045

H. Zheng

Department of Pharmaceutical Chemistry, School of Pharmacy, The University of Kansas, Lawrence, Kansas 66045

E.N. Boyce

Department of Pharmaceutical Chemistry, School of Pharmacy, The University of Kansas, Lawrence, Kansas 66045

The effect of chlorhexidine gluconate on the adherence of Candida albicans to human buccal epithelial cells (BEC) and drug-induced alterations in BEC membrane-lipid packing order were examined. Treatment of BEC with attached yeasts with 0.1 and 0.2% chlorhexidine resulted in significant yeast detachment after 90 and 60 min, respectively. Following pre-treatment of BEC with > 0.1% chlorhexidine, yeast adherence was inhibited by > 80%. In parallel experiments, the fluorescence anisotropy of BEC labeled with fluorescent membrane probes-diphenylhexatriene (DPH) and trimethylammonium DPH-was assessed following exposure to chlorhexidine. The fluorescence anisotropy decreased with increasing concentrations of chlorhexidine, which indicated that the drug decreased epithelial-cell membrane-lipid packing order. Chlorhexidine concentrations that altered epithelial-cell membrane-lipid packing order, particularly in superficial regions, were similar to those drug concentrations required for detachment of adherent yeasts. Similar results were obtained with a second antifungal, nystatin A. While the effects of chlorhexidine on the buccal-cell membrane-lipid packing order were not reversed by multiple washings, the opposite situation occurred with nystatin A. The results suggest that chlorhexidine-induced alterations ofBEC membrane-lipid order may be involved in the antifungal actions of the drug.

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Journal of Dental Research, Vol. 71, No. 6, 1298-1303 (1992)
DOI: 10.1177/00220345920710060601


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