Preparation of multivesicular liposomes for controlled...

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 31/7036 (2006.01) A61K 31/7068 (2006.01)

Patent

CA 2199004

Disclosed are multivesicular liposomes (MVL's) containing biologically active substances, the multivesicular liposomes having defined size distribution, adjustable average size, adjustable internal chamber size and number, and a controlled and variable release rate of the biologically active substance. The process involves encapsulating at least one biologically active substance and optionally an osmotic spacer in a first aqueous component encapsulated within the liposomes. The rate of release of the active substance into the surrounding environment in which the liposomes are introduced can be decreased by increasing the osmolarity of the first aqueous component or increased by decreasing the osmolarity.

L'invention concerne des liposomes multivésiculaires (MVL) contenant des substances biologiquement actives et présentant une distribution granulométrique définie, une granulométrie moyenne modulable, un nombre et une taille de cavités internes modulables, ainsi qu'une vitesse de libération variable de la substance biologiquement active. Le procédé consiste à encapsuler au moins une substance biologiquement active et, éventuellement, un élément d'espacement osmotique, dans un premier constituant aqueux encapsulé dans les liposomes. La vitesse de libération de la substance active dans l'environnement dans lequel les liposomes sont introduits peut être réduite par augmentation de l'osmolarité du premier constituant aqueux ou augmentée par réduction de ladite osmolarité.

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