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Title: Halofantrine-phospholipid interactions: Monolayer studies
Authors: Go, M.-L. 
Feng, S.-S. 
Keywords: Critical surface pressure
Dipalmitolylphosphatidylcholine monolayer
Issue Date: 2001
Citation: Go, M.-L., Feng, S.-S. (2001). Halofantrine-phospholipid interactions: Monolayer studies. Chemical and Pharmaceutical Bulletin 49 (7) : 871-876. ScholarBank@NUS Repository.
Abstract: The antimalarial agent halofantrine penetrates dipalmitolylphosphatidylcholine (DPPC) monolayers resulting in an increase in surface pressure and an expansion in area occupied by the lipid components of the monolayer. This phenomenon is observed at concentrations (0.05-0.2 μM) of halofantrine that have no surface activity. Penetration increases with drug concentration and is greatest at low initial surface pressures of the monolayer. A critical surface pressure of the DPPC monolayer has been determined from constant area and constant pressure conditions. The magnitude of these values support the hypothesis that halofantrine readily penetrates the DPPC monolayers. The presence of cholesterol in the DPPC monolayer hampers penetration and a lower critical surface pressure is obtained under such conditions. Even then, a slower rate of penetration is observed only in monolayers maintained at high initial surface pressures (10, 15 mN/m), corresponding to the liquid condensed phase of the monolayer, and not at low surface pressures (2.5, 5.0 mN/m). These results help to give a better understanding of the dynamics of the halofantrine-phospholipid interaction as well as the pharmacodynamic character of the drug.
Source Title: Chemical and Pharmaceutical Bulletin
ISSN: 00092363
DOI: 10.1248/cpb.49.871
Appears in Collections:Staff Publications

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