A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 9/127 (2006.01)
Patent
CA 2378438
Fully lipid-encapsulated therapeutic agent particles of a charged therapeutic agent are prepared by combining a lipid composition containing preformed lipid vesicles, a charged therapeutic agent, and a destabilizing agent to form a mixture of preformed vesicles and therapeutic agent in a destabilizing solvent. The destabilizing solvent is effective to destabilize the membrane of the preformed lipid vesicles without disrupting the vesicles. The resulting mixture is incubated for a period of time sufficient to allow the encapsulation of the therapeutic agent within the preformed lipid vesicles. The destabilizing agent is then removed to yield fully lipid-encapsulated therapeutic agent particles. The preformed lipid vesicles comprise a charged lipid which has a charge which is opposite to the charge of the charged therapeutic agent and a modified lipid having a steric barrier moiety for control of aggregation.
Pour la préparation de particules à encapsulation lipidique intégrale d'un agent thérapeutique chargé, on combine une composition lipidique renfermant des vésicules lipidiques préformées, un agent thérapeutique chargé et un agent déstabilisant pour former un mélange de vésicules préformées et d'agent thérapeutique dans un solvant déstabilisant. Ce solvant déstabilisant est capable de déstabiliser la membrane des vésicules lipidiques préformées sans porter atteinte aux vésicules. On fait incuber le mélange ainsi obtenu pendant un laps de temps suffisant pour encapsuler l'agent thérapeutique dans les vésicules lipidiques préformées. Après retrait de l'agent déstabilisant, on obtient des particules d'agent thérapeutique à encapsulation lipidique complète. Les vésicules lipidiques préformées comprennent un lipide chargé dont la charge est opposée à celle de l'agent thérapeutique chargé et un lipide modifié comportant une fraction barrière stérique destinée à réguler l'agrégation.
Cullis Pieter R.
Maurer Norbert
Wong Kim F.
Inex Pharmaceuticals Corp.
Smart & Biggar
The University Of British Columbia
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