Bioadhesion drug carriers for endothelial and epithelial...

A - Human Necessities – 61 – K

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A61K 9/16 (2006.01) A61K 9/50 (2006.01) A61K 9/51 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01)

Patent

CA 1324080

ABSTRACT This application describes the preparation and in vivo testing of surface coatings and matrix materials, which when applied to or caused to comprise the carriers for drugs and diagnostic agents, and administered in a fashion that allows efficient vascular access, causes the carriers to recognize determinants present on normal or focally diseased endothelium, and induces the following in vivo effects: 1) rapid, partial or total endothelial envelopment or the drug (diagnostic) carrier; 2) sequestration of the carrier and protection of the entrapped agent from blood vascular clearance at an early time (2 minutes) when the endothelial pocket which envelops the carrier still invaginates into the vascular compartment; 3) acceleration of the carrier's transport across and/or through the vascular endothelium or subendothelial structures into the tissue compartment (interstitium); and 4) improvement of the efficiency with which the drug (or diagnostic) carrier migrates across the endothelium, or epi-endothelial or subendothelial barriers, such that a lower total drug dose is required to obtain the desired effect relative to that required for standard agents. Analogous tissue uptake is described for transepithelial migration into the lungs, bladder and bowel.

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