Micellar solubilization of a new antimalarial drug, beta-arteether.
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.
Krishna
A K
AK
College of Pharmacy, University of Iowa, Iowa City 52242.
Flanagan
D R
DR
D000962:Antimalarials / Q000032:analysis*; D037621:Artemisinins; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D008823:Micelles; D012717:Sesquiterpenes / Q000032:analysis*; D012967:Sodium Dodecyl Sulfate; D012995:Solubility; D013501:Surface-Active Agents
D000962:Antimalarials; D037621:Artemisinins; D008823:Micelles; D012717:Sesquiterpenes; D013501:Surface-Active Agents; D012967:Sodium Dodecyl Sulfate; C055141:artemotil