Compositions and methods for enhancing drug delivery across and into ocular tissues
First Claim
1. A method for enhancing delivery of a compound into and across an animal ocular tissue, the method comprising:
- administering to the ocular tissue a conjugate comprising the compound and a delivery-enhancing transporter, wherein;
i. the compound is attached to the delivery-enhancing transporter through a linker, and ii. the delivery-enhancing transporter comprises fewer than 50 subunits and comprises at least 5 guanidino or amidino moieties, thereby increasing delivery of the conjugate into the ocular tissue compared to delivery of the compound in the absence of the delivery-enhancing transporter.
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Abstract
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 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.
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Citations
36 Claims
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1. A method for enhancing delivery of a compound into and across an animal ocular tissue, the method comprising:
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administering to the ocular tissue a conjugate comprising the compound and a delivery-enhancing transporter, wherein;
i. the compound is attached to the delivery-enhancing transporter through a linker, and ii. the delivery-enhancing transporter comprises fewer than 50 subunits and comprises at least 5 guanidino or amidino moieties, thereby increasing delivery of the conjugate into the ocular tissue compared to delivery of the compound in the absence of the delivery-enhancing transporter. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36)
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Specification