Preparation of large liposomes by infusion into peg

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 39/00 (2006.01) A61K 9/00 (2006.01)

Patent

CA 2436348

This invention provides a method of preparing large liposomes with high entrapment capacity for pharmaceutical substances. The method generally entails infusing a lipid/alcohol solution directly into an aqueous polymer solution. The resulting liposome, which may be incorporated with a pharmaceutical substance, typically consists of multilamellar vesicles that have an average size of about 1 to 8 microns. The ratio of lipid to polymer, average molecular weight of the polymer, polymer concentration, ionic strength, and temperature of incubation are variables disclosed herein to control liposome size and incorporation of components and pharmaceutical substances.

L'invention concerne un procédé de préparation de liposomes de grande taille avec une grande capacité de piégeage des substances pharmaceutiques. Ce procédé consiste généralement à perfuser une solution lipidique/alcool directement dans une solution de polymère aqueuse. Le liposome ainsi obtenu auquel on peut incorporer une substance pharmaceutique, se compose généralement de vésicules multilamellaires dont la taille moyenne se situe entre 1 et 8 microns environ. Le rapport lipides/polymères, le poids moléculaire moyen du polymère, la concentration de polymères, la force ionique et la température d'incubation sont des variables décrites ici pour commander la taille des liposomes et l'incorporation des composants et des substances pharmaceutiques.

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