Metal-porphyrin complexes for the inactivation of the biological activity of opioids
Inventors
Nag, Okhil • Ellis, Gregory • Walper, Scott • Deschamps, Jeffrey R. • Knight, D. Andrew • Delehanty, James B.
Assignees
Publication Number
US-11744834-B2
Publication Date
2023-09-05
Expiration Date
2040-04-01
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Abstract
A rhodium-loaded porphyrin complex, comprising the porphyrin (meso-tri(4-sulfonatophenyl) mono(4-carboxyphenyl)porphine (C1S3TPP)) with coordinated with rhodium, effectively neutralizes the biological activity of naturally-occurring and synthetic opioids.
Core Innovation
The invention involves a rhodium-loaded porphyrin complex, specifically meso-tri(4-sulfonatophenyl) mono(4-carboxyphenyl)porphine (C1S3TPP) coordinated with rhodium chloride trihydrate, which effectively neutralizes the biological activity of naturally-occurring and synthetic opioids. This complex binds and deactivates opioids, demonstrated by its ability to inhibit opioid-induced intracellular signaling pathways in cultured mammalian cells, including the inhibition of cyclic AMP formation and consequent ion channel deactivation.
The problem addressed is the opioid overdose crisis, exacerbated by the limitations of the state-of-the-art treatment naloxone (NARCAN®). Naloxone acts as a competitive opioid receptor antagonist but requires repeated dosing as it only displaces opioids from receptors without neutralizing them chemically. Naloxone usage is further limited by the potential induction of withdrawal symptoms and receptor overexpression, which can reduce its effectiveness. There is a critical need for alternative treatments capable of directly neutralizing opioids.
The invention provides a novel therapeutic approach by chemically inactivating opioids using the rhodium-porphyrin complex rather than merely blocking receptor binding. This complex can degrade synthetic opioids such as fentanyl, significantly reducing their biological activity by 1,000 to 10,000-fold in vitro. The complex may be conjugated to nanoparticles, such as gold nanoparticles, which enhances its catalytic activity and opioid neutralization efficiency.
Claims Coverage
The patent includes two independent claims covering material compositions and associated configurations with inventive features focused on the rhodium-coordinated porphyrin and its nanoparticle conjugates.
Material comprising porphyrin coordinated with rhodium
A material comprising the porphyrin meso-tri(4-sulfonatophenyl) mono(4-carboxyphenyl)porphine (C1S3TPP) coordinated with rhodium, where the porphyrin has the specified structure.
Nanoparticle conjugation of rhodium-coordinated porphyrin
The rhodium-coordinated porphyrin material is in a state of being conjugated to the surface of a nanoparticle.
The claims primarily cover the rhodium-loaded porphyrin complex and its configuration when conjugated to nanoparticles, focusing on the composition and its enhanced functional state for opioid neutralization.
Stated Advantages
Effectively neutralizes the biological activity of both naturally-occurring and synthetic opioids.
Overcomes limitations of naloxone by chemically inactivating opioids rather than merely displacing them from receptors.
Significantly reduces opioid activity by 1,000 to 10,000 times, demonstrated in cell-based assays.
Conjugation to nanoparticles enhances catalytic activity and opioid neutralization efficiency.
Documented Applications
Treatment of opioid overdose by administering a medicament comprising the rhodium-coordinated porphyrin complex in conjunction with a pharmaceutically-acceptable carrier.
Interested in licensing this patent?