Mixed micelles including amphipathic conjugates of rna...

A - Human Necessities – 61 – K

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Details

A61K 47/48 (2006.01) A61K 9/107 (2006.01) A61K 31/713 (2006.01) A61K 47/30 (2006.01) A61K 47/28 (2006.01)

Patent

CA 2692748

Disclosed are improved pharmaceutical formulations for the delivery of RNA interference agents, such as antisense RNA, micro-RNA and siRNA. The formulations employ mixed micelles including amphipathic conjugates of the iRNA agents and amphipathic micelle- forming molecules with extended hydrophilic chains. Also disclosed are methods of using the pharmaceutical formulations to increase delivery of an iRNA agent to an intracellular target, and to decrease extracellular nuclease degradation of an iRNA agent in the formulations.

La présente invention concerne des préparations pharmaceutiques améliorées destinées à administrer des agents d'interférence ARN, tels les ARN antisens, les micro-ARN et les ARNsi. Les préparations utilisent des micelles mixtes, notamment des conjugués amphiphatiques d'agents ARNi, et des molécules formant des micelles amphiphatiques dotées de chaînes hydrophiles allongées. L'invention porte aussi sur des procédés d'utilisation des préparations pharmaceutiques afin d'accroître l'administration d'un agent ARNi à une cible intracellulaire et réduire la dégradation de la nucléase extracellulaire d'un agent ARNi dans les préparations.

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