Title:
VASCULAR DELIVERY SYSTEMS
Document Type and Number:
WIPO Patent Application WO/2009/133545
Kind Code:
A3
Abstract:
The site-specific expression of selectins on endothelial cells of blood vessels during angiogenesis provides an opportunity to target anti-cancer drugs to the vascular endothelium to extend the range of the therapeutic effect. This invention describes an innovative drug targeting strategy for the selective delivery of the anticancer drugs to endothelial cells by means of polymer-drug conjugates modified with a carbohydrate ligand for the vascular selectins. A model chemotherapeutic drug, doxorubicin, and the E-selectin ligand, sLex, are attached to a biocompatible polymer (HPMA). The selective binding, cellular uptake, intracellular fate, and cell cytotoxicity of the polymer-bound drug are investigated in human endothelial cells.
Inventors:
DAVID AYELET (IL)
ASHKENAZY GONEN (IL)
SHAMAY YOSI (IL)
ASHKENAZY GONEN (IL)
SHAMAY YOSI (IL)
Application Number:
PCT/IL2009/000152
Publication Date:
December 02, 2010
Filing Date:
February 11, 2009
Export Citation:
Assignee:
UNIV BEN GURION (IL)
DAVID AYELET (IL)
ASHKENAZY GONEN (IL)
SHAMAY YOSI (IL)
DAVID AYELET (IL)
ASHKENAZY GONEN (IL)
SHAMAY YOSI (IL)
International Classes:
A61K47/48; A61K49/00; A61P35/00
Domestic Patent References:
| WO2000066091A1 | 2000-11-09 | |||
| WO1993013804A1 | 1993-07-22 |
Foreign References:
| US20060241022A1 | 2006-10-26 | |||
| US5648458A | 1997-07-15 |
Other References:
SEYMOUR L W: "SOLUBLE POLYMERS FOR LECTIN-MEDIATED DRUG TARGETING", ADVANCED DRUG DELIVERY REVIEWS, ELSEVIER BV, AMSTERDAM, NL LNKD- DOI:10.1016/0169-409X(94)90007-8, vol. 14, no. 1, 1 April 1994 (1994-04-01), pages 89 - 111, XP001032660, ISSN: 0169-409X
GIRARD C ET AL: "Sialyl Lewis analogs based on a quinic acid scaffold as the fucose mimic", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB LNKD- DOI:10.1016/J.BMCL.2005.05.004, vol. 15, no. 13, 1 July 2005 (2005-07-01), pages 3224 - 3228, XP025313732, ISSN: 0960-894X, [retrieved on 20050701]
GIRARD C ET AL: "Sialyl Lewis
Attorney, Agent or Firm:
TEITELBAUM, Rachel (P.O. Box 1352, Jerusalem, IL)
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