Method of dehydrating liposomes using protective sugars

Details Method of dehydrating liposomes using protective sugars Method of dehydrating liposomes using protective sugars

1993-02-24

1996-11-26

Azpuru, Carlos

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Liposomes

264 41, 264 43, 264 46, A61K 9127, B01J 1302, B01J 1304

Patent

active

055783201

ABSTRACT:
Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration. Concentration gradients capable of generating transmembrane potentials can be created across the liposome membranes either before or after dehydration, and the transmembrane potentials resulting from these gradients can be used to load charged materials, e.g., drugs, into the liposomes.

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