In vivo agents comprising cationic drugs, peptides and metal chelators with acidic saccharides and glycosaminoglycans, giving improved site-selective localization, uptake mechanism, sensitivity and kinetic-spatial profiles, including tumor sites
US6106866A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Jul 31, 1995 |
| Grant date | Aug 22, 2000 |
| Priority date | — |
| Expiry date | Jul 31, 2015 |
Classification
- Technology area (CPC B)Performing Operations; Transporting
- CPC primaryB82Y5/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A drug carrier composition comprising a drug complexed with dermatan sulfate is disclosed. The drug is preferably an anti tumor drug and may be taxol, a peptide onco-agent or vincristine. The most preferred antitumor drug is doxorubicin. The dermatan sulfate is essentially purified dermatan sulfate with a sulfur content of up to 9% (w/w) and with selective oligosaccharide oversulfation. The compositions are administered in a fashion that allows efficient vascular access 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 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 migrates across the endothelium, or epi-endothelial or subendothelial barriers, such that a lower total drug dose is required to obtain the desi…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.