Endothelial envelopment drug carriers
First Claim
1. A composition comprising a multivalent binding agent surface which binds determinants of endothelial or epithelial cells;
- wherein the composition is a microsphere, microaggregate, or macromolecule less than about 250 micrometers in size, and has a matrix capable of containing a drug or diagnostic agent at a content of at least 12% (w/w); and
wherein the multivalent binding agent surface consists of carbohydrate, oligosaccharide, monosaccharide, negatively charged polysaccharide, negatively charged oligosaccharide, dextran sulfate, glycosaminoglycan, heparin, heparin fragment, synthetic heparin analogue, heparan sulfate, dermatan sulfate, chondroitin sulfate, hyaluronic acid; and
which induces rapid partial or total envelopment of said composition by endothelial or epithelial cells and facilitated migration across said cells into proximal tissues.
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Accused Products
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 or normal or focally diseased endothelium, and induces the following in vivo effects: 1) rapid, partial or total endothelial envelopment of the drug (diagnostic) carrier; 2) sequestration of the carrier and protecting 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 or through the vascular endothelium and/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.
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Citations
11 Claims
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1. A composition comprising a multivalent binding agent surface which binds determinants of endothelial or epithelial cells;
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wherein the composition is a microsphere, microaggregate, or macromolecule less than about 250 micrometers in size, and has a matrix capable of containing a drug or diagnostic agent at a content of at least 12% (w/w); and wherein the multivalent binding agent surface consists of carbohydrate, oligosaccharide, monosaccharide, negatively charged polysaccharide, negatively charged oligosaccharide, dextran sulfate, glycosaminoglycan, heparin, heparin fragment, synthetic heparin analogue, heparan sulfate, dermatan sulfate, chondroitin sulfate, hyaluronic acid; and
which induces rapid partial or total envelopment of said composition by endothelial or epithelial cells and facilitated migration across said cells into proximal tissues. - View Dependent Claims (4, 5, 6, 7, 8, 9, 10, 11)
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2. A composition comprising a multivalent binding agent surface which binds determinants of endothelial or epithelial cells;
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wherein the composition is a microsphere, microaggregate, or macromolecule less than about 250 micrometers in size, and has a matrix capable of containing a drug or diagnostic agent at a content of at least 12% (w/w); and wherein the multivalent binding agent is a heparin, a heparin fragment, or synthetic heparin analogue, which induces rapid partial or total envelopment of said composition by endothelial or epithelial cells and facilitated migration across said cells into proximal tissues.
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3. A composition comprising a multivalent binding agent surface which binds determinants of endothelial or epithelial cells;
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wherein the composition is a microsphere, microaggregate, or macromolecule less than about 250 micrometers in size, and has a matrix capable of containing a drug or diagnostic agent at a content of at least 12% (w/w); and wherein the multivalent binding agent consists essentially of heparin, heparin fragment, synthetic heparin analogue, heparan sulfate, dermatan sulfate, chondroitin sulfate, hyaluronic acid or dextran sulfate, which induces rapid partial or total envelopment of said composition by endothelial or epithelial cells and facilitated migration across said cells into proximal tissues.
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Specification