Liposome with increased retention volume

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/127 (2006.01) A61K 31/16 (2006.01) A61K 31/535 (2006.01) A61K 31/60 (2006.01) A61K 31/70 (2006.01) A61K 47/24 (2006.01) A61K 49/04 (2006.01) B01J 13/02 (2006.01)

Patent

CA 2186745

- 24 - The present invention provides preparations capable of efficiently holding water soluble substance particularly non-electrolytic water soluble substances. Liposomes and suspensions thereof comprising multilamellar liposomes characterized in that the liposome membrane is formed from a neutral phospholipid comprising a substantially saturated fatty acid residue a charged phospholipid comprising a substantially saturated fatty acid residue, ratio of said neutral phospholipid and charged phospholipid is 200:1 to 3:1, weighted average particle size of the liposome is 50 nm to 3,000 nm, and an encapsulation capacity of the liposome (internal aqueous phase (volume)/lipids (weight)) is at least 5 ml/g. The present liposome preparation can encapsulate an aqueous so1ution of a non-electrolytic water soluble substances with an encapsulation capacity (internal aqueous phase/lipids) of at least 5 ml/g.

La présente invention concerne un liposome capable de retenir efficacement même une substance hydrosoluble non-électrolyte, la membrane liposomique étant constituée d'un phospolipide neutre contenant essentiellement des restes d'acides gras saturés, et d'un phospholipide chargé contenant essentiellement des restes d'acides gras saturés. Le rapport pondéral phospholipide neutre/phospholipide chargé est de 200 pour 1 à 3 pour 1. Ce liposome est caractérisé par un diamètre particulaire moyen de 50 à 3000 nm et par une capacité de rétention (rapport phase liquide interne/lipide) d'au moins 5 ml/g. Sa capacité de rétention d'une substance hydrosoluble non-électrolyte en solution aqueuse est d'au moins 5ml/g.

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