Nanoparticles for delivery of nucleic acids and stable...

C - Chemistry – Metallurgy – 12 – N

Patent

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C12N 15/87 (2006.01) C07D 251/54 (2006.01) C07D 251/70 (2006.01) C07H 21/02 (2006.01) A61K 31/713 (2006.01) A61K 47/22 (2006.01) A61K 47/26 (2006.01) A61K 47/42 (2006.01) A61K 47/48 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2536191

Nanoparticles of double-stranded nucleic acid complexed about a complexing agent such as the melamine derivatives of formulae I and II, preferably forming a trimeric nucleic acid complex. In alternative embodiments, polyarginine or a polymer of Gln and Asn further complexed with the double-stranded nucleic acid complex. In a preferred embodiment, the ds nucleic acid is a double stranded RNA having 15 to 30 base pairs suitable for RNA interference. In another aspect of the invention, a ds RNA is produced in which all of the uridines are changed to 5-methyluridine. Preferably, the resultant ds RNAs have 15 to about 30 base pairs and are suitable for RNA interference.

L'invention concerne des nanoparticules d'acide nucléique double brin formant un complexe autour d'un agent complexant tel que des dérivés de mélamine représentés par les formules I et II, et qui forment de préférence un complexe d'acide nucléique trimère. Dans d'autres formes de réalisation, la polyarginine ou un polymère de Gln et d'Asn forme en outre un complexe avec le complexe d'acide nucléique double brin. Dans une forme de réalisation préférée, l'acide nucléique double brin est un ARN double brin qui comporte 15 à 30 paires de bases et convient pour l'interférence ARN. Dans un autre aspect de l'invention, on produit un ARN double brin dans lequel toutes les uridines sont transformées en 5-méthyluridine. De préférence, les ARN double brin obtenus comportent de 15 à environ 30 paires de bases et conviennent pour l'interférence ARN.

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