Encapsulation of antineoplastic agents in liposomes

Details Encapsulation of antineoplastic agents in liposomes Encapsulation of antineoplastic agents in liposomes

A - Human Necessities

61

K

167/163

A61K 9/127 (2006.01) A61K 47/48 (2006.01) B01J 13/02 (2006.01)

Patent

CA 1305054

ABSTRACT A process for preparing a multilamellar vesicle in the absence of organic solvent or detergents comprises the steps of: a) dispersing a lipid in an aqueous solvent to form a multila- mellar vesicle; b) rapidly freezing the multilamellar vesicle to obtain a frozen lipid-aqueous medium mixture; and c) warming the mixture to melt the aqueous medium. Methods for encapsulating ionizable antineoplastic agents in liposomes using transmembrane potentials are provided. Trapping efficiencies approaching 100% and rapid loading are readily achieved. Dehydration protocols which allow liposomes to be conveniently used in the adminis- tration of antineoplastic agents in a clinical setting are also pro- vided. In accordance with other aspects of the invention, transmem- brane potentials are used to reduce the rate of release of ionizable drugs from liposomes.

615733

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