Lipid particles having asymmetric lipid coating and method...

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 47/48 (2006.01) C12N 15/88 (2006.01)

Patent

CA 2520864

A method of preparing lipid particles having an asymmetric lipid coating is described. The lipid composition of the outer lipid coating of the particles varies from the inner to outer surfaces. The asymmetric lipid particles are formed by preparing a lipid composition containing a charged lipid and a therapeutic agent, where the particles each have an outer lipid coating with an external lipid leaflet and an internal lipid structure. The particles are then incubated under conditions effective to remove the charged lipid from the external lipid leaflet, thus rendering the lipid coating asymmetric. The particles have the ability to their regain surface charge via translocation of the lipids.

L'invention concerne un procédé pour préparer des particules lipidiques présentant un revêtement lipidique asymétrique. La composition lipidique du revêtement lipidique extérieur des particules se modifie des surfaces intérieures aux surfaces extérieures. La formation des particules lipidiques asymétriques comprend la préparation d'une composition lipidique contenant un agent thérapeutique et un lipide chargé, chaque particule présentant un revêtement lipidique extérieur comprenant un feuillet lipidique externe et une structure lipidique interne. Les particules sont ensuite incubées dans des conditions efficaces, pour éliminer le lipide chargé du feuillet lipidique externe, ce qui permet de rendre le revêtement lipidique asymétrique. Les particules présentent la capacité de regagner la surface par l'intermédiaire d'une translocation des lipides.

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