High drug:lipid formulations of liposomal- antineoplastic...

Details High drug:lipid formulations of liposomal- antineoplastic... High drug:lipid formulations of liposomal- antineoplastic...

A - Human Necessities

61

K

167/163

A61K 9/127 (2006.01)

Patent

CA 1338702

A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problems related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.

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