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Micellar solubilization of a new antimalarial drug, beta-arteether
1College of Pharmacy, University of Iowa, Iowa City 52242.
Abstract:
beta-Arteether (1) is a new antimalarial drug derived from artemisinin (2, quinghaosu). Compound 1 is quite water insoluble, but very soluble in a variety of organic solvents. Solubilization in a variety of surfactants was investigated to obtain higher concentrations of 1 in aqueous solutions. Anionic and cationic surfactants exhibited dramatic solubilizing ability for 1, while nonionic surfactants showed significantly lower solubilizing ability. The solubilization data are analyzed on the basis of a pseudo-phase model with 1 exhibiting a high partition coefficient into the micellar phase. An empirical model is presented to identify the possible sites of solubilization of 1 in the micelle.
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