Low rigidity liposomal antibacterial composition

A - Human Necessities – 61 – K

Patent

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A61K 9/127 (2006.01)

Patent

CA 2206296

The invention relates to a liposomal formulation containing at least one therapeutic agent such as an antibiotic and to a method of treatment of bacterial infections through the administration of such a formulation. There is provided a low rigidity multilamellar liposomal formulation, free of cholesterol, comprising a neutral lipid, an anionic lipid and at least one therapeutic agent, wherein the liposomal formulation enhances the penetration of the therapeutic agent inside a bacterial cell. A preferred lipid combination is dipalmitoylphosphatidylcholine (DPPC): dimirystoylphosphatidylglycerol (DMPG) at a ratio of 10:1 to 15:1, with total lipid concentration ranging from 5 to 85 mM.

L'invention concerne une formulation de liposomes contenant au moins un agent thérapeutique tel qu'un antibiotique, et un procédé permettant de traiter des infections bactériennes par l'administration d'une telle formulation. On présente une formulation de liposomes multilamellaire à faible rigidité, ne contenant pas de cholestérol mais un lipide neutre, un lipide anionique et au moins un agent thérapeutique, formulation destinée à favoriser la pénétration de l'agent thérapeutique dans une cellule bactérienne. Une combinaison préférée de lipides est la dipalmitoylphosphatidylcholine (DPPC): dimirystoylphosphatidylglycerol (DMPG), selon un rapport allant de 10:1 à 15:1, la concentration lipidique totale variant entre 5 et 85 mM.

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