Method of inhibiting leakage of drug encapsulated in liposomes

Details Method of inhibiting leakage of drug encapsulated in liposomes Method of inhibiting leakage of drug encapsulated in liposomes

A - Human Necessities

61

K

A61K 31/553 (2006.01) A61K 9/127 (2006.01) A61K 47/24 (2006.01)

Patent

CA 2376849

The present invention provides a method of inhibiting the leakage of a drug encapsulated in liposomes, which comprises satisfying at least two requirements selected from the group consisting of the following three requirements: using at least two lipid bilayers of the liposomes, controlling the average particle size of the liposomes to 120 nm or more, and using lipid having a phase transition temperature higher than in vivo temperature as lipid constituting the liposomes. Also, the present invention provides a liposome preparation which is stable in vivo and satisfies at least two requirements selected from the group consisting of the following three requirements: the number of lipid bilayers of the liposomes is at least two, the liposomes have an average particle size of 120 nm or more, and lipid constituting the liposomes has a phase transition temperature higher than in vivo temperature.

L'invention concerne une méthode de régulation de la fuite d'un médicament encapsulé dans des liposomes consistant à satisfaire au moins deux des trois conditions suivantes, c'est-à-dire, utiliser des membranes lipidiques des liposomes à deux bicouches ou plus, réguler le diamètre particulaire moyen des liposomes à 120 nm ou davantage et utiliser, en tant que lipide constituant les liposomes, un lipide ayant une température de transition de phase supérieure à la température du corps; ainsi qu'une préparation de liposomes stable <i>in vivo</i> satisfaisant au moins deux des trois conditions suivantes, c'est-à-dire, utiliser des membranes lipidiques des liposomes à deux bicouches ou davantage, ajuster le diamètre particulaire moyen des liposomes à 120 nm ou davantage et utiliser, en tant que lipide constituant les liposomes, un lipide ayant une température de transition de phase supérieure à la température corporelle.

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