Compositions of drug delivery agents and methods of use thereof
Inventors
Barnes, Jonathan C. • Li, Xuesong • Delawder, Abigail • Li, Ruihan
Assignees
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Publication Number
US-12589157-B1
Publication Date
2026-03-31
Expiration Date
Abstract
Provided herein are compositions and methods of making and using drug-binding polymers or nanoparticles for targeted therapies. In some embodiments the drug-binding polymers or nanoparticles can deliver two or more of an antibiotic, an alkali or transition metal cation, or anticancer agents.
Core Innovation
The invention relates to a drug-delivery agent comprising a self-assembled nanoparticle formed from a plurality of polymer components. The polymer components self-assemble into a micelle arrangement with an inner core comprising hydrophobic regions and an outer shell comprising hydrophilic regions.
The hydrophobic block polymers comprise norbornene-polymerized backbones formed from hydrophobic monomers in which a first and a second macrocyclic moiety are covalently linked to norbornene. Each hydrophobic monomer includes an active compound non-covalently bound to its macrocyclic moiety, and the first and second macrocyclic moieties are different and selected from cyclodextrin, calixarene, crown ether, and cyclophane.
The hydrophilic block polymer is formed from norbornene-polymerized hydrophilic monomers covalently linked to a hydrophilic moiety selected from a protonated L-arginine-glucosamine (LARGE) group, a protonated tert-butyloxycarbonyl (Boc)-protected arginine group, and poly(ethylene glycol). The platform provides sustained release without prodrug linkage through non-covalent, receptor-governed loading.
Claims Coverage
The partial content provides one independent claim that defines a micelle-forming self-assembled nanoparticle drug-delivery agent constructed from norbornene-polymerized polymer components featuring two different macrocyclic moiety-bearing hydrophobic blocks and a hydrophilic block. The independent claim includes four inventive features: micelle core-shell arrangement, hydrophobic block polymer composition, macrocyclic moiety selection with non-covalent active-compound binding, and hydrophilic moiety selection.
Self-assembled micelle nanoparticle with hydrophobic core and hydrophilic shell
A drug-delivery agent having a self-assembled nanoparticle made of a plurality of polymer components that assemble into a micelle arrangement with an inner core comprising hydrophobic regions and an outer shell comprising hydrophilic regions.
Hydrophobic block polymers with norbornene-polymerized backbones and different macrocyclic moieties
At least two hydrophobic block polymers comprise norbornene-polymerized backbones formed from hydrophobic monomers covalently linked to a first and a second macrocyclic moiety, where the macrocyclic moieties are different and selected from cyclodextrin, calixarene, crown ether, and cyclophane.
Non-covalently bound active compounds on macrocyclic moieties
Each hydrophobic monomer includes an active compound non-covalently bound to its macrocyclic moiety.
Hydrophilic block polymer with selected hydrophilic moieties
At least one hydrophilic block polymer comprises norbornene-polymerized hydrophilic monomers covalently linked to a hydrophilic moiety selected from a protonated LARGE group, a protonated Boc-protected arginine group, and poly(ethylene glycol).
The claim coverage centers on a micelle-forming, self-assembled drug-delivery nanoparticle built from norbornene-polymerized polymer components. It specifies two different hydrophobic block polymers with macrocyclic moieties covalently linked to norbornene and active compounds non-covalently bound to those macrocycles, plus a hydrophilic block polymer bearing selected hydrophilic moieties.
Stated Advantages
Provides sustained release without prodrug linkage through non-covalent, receptor-governed loading.
Enables combination antibacterial therapy for multidrug-resistant infections, including co-delivery of Ag+ with antibiotics.
Supports bacterial membrane targeting and disruption associated with oxidative stress and disruption of disulfide bond formation.
Induces collagen synthesis during wound healing.
Documented Applications
Combination antibacterial therapy for multidrug-resistant infections, including synergy effects involving Ag+ and antibiotics and antibacterial effects described as targeting bacterial membranes and promoting disruption via oxidative stress and disulfide bond formation.
Combination anticancer therapy enabling plug-and-play loading of multiple small-molecule chemotherapeutics with controlled release governed by receptor binding.
Wound healing application using a dual-syringe system with sodium alginate for hemostasis alongside drug-loaded micelles.
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