Compositions and methods for the delivery of...

A - Human Necessities – 61 – K

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Details

A61K 31/7088 (2006.01) A61K 9/127 (2006.01) A61K 47/12 (2006.01) A61K 47/28 (2006.01) A61K 48/00 (2006.01) C07H 21/00 (2006.01) C07H 21/04 (2006.01) C12Q 1/68 (2006.01)

Patent

CA 2294988

The present invention relates to compositions and methods which enhance the transport of nucleic acids, especially oligonucleotides at various sites in the alimentary canal of an animal. The methods and compositions enhance the transport of oligonucleotides across the mucosa of the alimentary canal via the use of one or more penetration enhancers. The invention features the use of various fatty acids, bile salts, chelating agents and other penetration enhancers, as well as carrier compounds, to enhance the stability of nucleic acids and/or their transport across and/or into cells of the alimentary canal. In one preferred embodiment, the compositions and methods of the invention are utilized to effect the oral delivery of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic or prophylactic purposes.

Cette invention concerne des compositions et des procédés qui améliorent le transport d'acides nucléiques et plus particulièrement d'oligonucléotides au niveau de divers sites dans le tube digestif d'un animal. Les procédés et les compositions améliorent le transport des oligonucléotides au niveau des muqueuses du tube digestif via l'utilisation d'au moins un activateur de pénétration. L'invention implique l'utilisation de divers acides gras, sels biliaire, agent chelateur et autres activateurs de pénétration ainsi que de composés vecteurs pour améliorer la stabilité des acides nucléiques et/ou leur transport au niveau de cellules et/ou dans des cellules du tube digestif. Dans une forme de réalisation préférée, les compositions et les procédés de cette invention sont utilisés pour effectuer l'apport par voie orale d'un oligonucléotide non codant chez un animal afin de moduler l'expression d'un gène chez ce dernier pour des raisons d'investigation, de thérapie ou de prévention.

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