Metal-olsalazine coordination polymers for medical applications

Patent · 20 July 2021

OSTI ID:1840266

Levine, Dana A.; Long, Jeffrey R.; Gonzalez, Miguel I.

Olsalazine (H₄olz), a prodrug of the anti-inflammatory 5-aminosalicylic acid, is used as a ligand to synthesize a suite of M(H₂olz) and M₂(olz) materials, where M is a dication (e.g. Mg, Ca, Sr, Fe, Co, Ni, Cu, Zn). A family of metal olsalazine coordination polymers, coordination solids, and metal organic frameworks are described, which include 1-, 2-, and 3-dimensional structures. The materials resist degradation at acidic pH and release olsalazine preferentially at neutral pH. The mesoporous M₂(olz) frameworks exhibit high surface areas with hexagonal pore apertures that are approximately 27 Å in diameter and contain coordinatively unsaturated metal sites. Biologically active molecules containing a Lewis-basic functional group can be grafted directly to the open metal sites of the frameworks. Dissolution of the frameworks under physiological conditions releases olsalazine (H₄olz) and the grafted molecules so that multiple therapeutic components can be delivered together at different rates.

• Research Organization: Univ. of California, Berkeley, CA (United States)
• Sponsoring Organization: USDOE
• DOE Contract Number: SC0001015
• Assignee: The Regents of the University of California (Oakland, CA)
• Patent Number(s): 11,065,264
• Application Number: 16/209,480
• OSTI ID: 1840266
• Country of Publication: United States
• Language: English