Compositions and methods for enhancing drug delivery across...

A - Human Necessities – 61 – K

Patent

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A61K 47/48 (2006.01)

Patent

CA 2438784

This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent (Fig. 4) across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

L'invention porte sur des compositions et procédés renforçant la livraison de médicaments ou d'autres agents dans et à travers les tissus épithéliaux dont les tissus oculaires et les tissus endothéliaux dont la barrière sang-cerveau. Ces compositions et procédés utilisent un transporteur accélérateur de livraison présentant un nombre suffisant de fragments de chaînes latérales guanidino ou amidino pour renforcer la livraison d'un composé conjugué au réactif (fig 4) à travers une ou plusieurs couches de tissus, par rapport à un composé non conjugué. Les polymères renforçateurs de livraison comprennent par exemple des molécules de polyarginine de préférence d'une longueur comprise entre environ 6 et 25 résidus.

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