Hydroxypropylcyclodextrins in parenteral use. I: Lipid dissolution and effects on lipid transfers in vitro.
Hydroxypropyl ethers of cyclodextrins form water-soluble inclusion complexes with lipids. Of the three hydroxypropylcyclodextrins examined, hydroxypropyl-alpha-cyclodextrin had limited specificity for phospholipids, and hydroxypropyl-beta-cyclodextrin had limited specificity for cholesterol, and hydroxypropyl-gamma-cyclodextrin was nonspecific. The formation of inclusion complexes was found to be a fast and reversible process in which complexation of cholesterol did not inhibit its oxidation by cholesterol oxidase, and cholesterol of the erythrocyte membrane could be exchanged within a minute for cholesteryl methyl ether which was in the inclusion complex. Thus, hydroxypropylcyclodextrin in the circulation may catalyze the transport of lipids in the direction of equilibrium distribution.
Irie
T
T
Gerontology Research Center, National Institute on Aging, National Institutes of Health, Baltimore, MD 21224.
Fukunaga
K
K
Pitha
J
J
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002784:Cholesterol / Q000737:chemistry; D003505:Cyclodextrins / Q000737:chemistry*; D004910:Erythrocyte Membrane / Q000737:chemistry; D006801:Humans; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry*; D012995:Solubility; D047391:alpha-Cyclodextrins; D047392:beta-Cyclodextrins; D047408:gamma-Cyclodextrins
D003505:Cyclodextrins; D008055:Lipids; D047391:alpha-Cyclodextrins; D047392:beta-Cyclodextrins; D047408:gamma-Cyclodextrins; C479658:hydroxypropyl-alpha-cyclodextrin; C479659:hydroxypropyl-gamma-cyclodextrin; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D002784:Cholesterol