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Publication Number
US-11331395-B2
Publication Date
2022-05-17
Expiration Date
Abstract
Aspects of the invention described herein include a hydrogel prodrug and methods of making a hydrogel prodrug for drug delivery. Also contemplated are methods of treating, inhibiting, ameliorating or inhibiting a disease or disorder. Without being limiting, the methods for treatment can be directed to a cancer, HIV, a virus, pain, a bacterial infection, a neurological disorder, hemorrhaging, multiple sclerosis, diabetes, high blood pressure, Alzheimer's, or inhibiting a fungal growth in a subject in need.
Core Innovation
The invention relates to a hydrogel prodrug delivery system in which a prodrug generates a drug upon hydrolysis and is covalently bound within a copolymer during polymerization. The covalent incorporation uses one or more chemical linkages selected from ester, thioester, amide, or acid anhydride, and the copolymer is formulated to release the drug upon degradation of the copolymer via hydrolysis.
The copolymer includes a prodrug, a primary linker molecule, and a secondary linker molecule. The primary linker molecule is terminated on each end by at least two functional groups that are reactive and configured to form the selected chemical linkages with at least two functional groups on the prodrug, and the molar equivalents of the primary linker molecule exceed the molar equivalents of the prodrug.
The secondary linker molecule is hydrophilic and comprises two functional groups configured to form covalent bonds with functional groups on the primary linker molecule thereby cross-linking to the prodrug molecule. In embodiments, the hydrogel prodrug is a microparticle having a diameter within the range of 1 to 300 microns, and drug release occurs through hydrolytic degradation of the copolymer.
Claims Coverage
The document includes one independent claim directed to a hydrogel prodrug delivery system with five core inventive features: hydrolysis-generated drug prodrug incorporation, specified linkage chemistries, dual-ended reactive primary linker functionality with primary-linker molar excess, a hydrophilic bifunctional secondary linker that cross-links, and hydrolytic release with a microparticle size limitation.
Hydrogel prodrug delivery system with hydrolysis-generated drug
A hydrogel prodrug delivery system comprising a copolymer with a prodrug which generates a drug upon hydrolysis and is formulated to release the drug upon degradation of the copolymer via hydrolysis.
Covalent prodrug incorporation during polymerization using specified linkages
The prodrug is covalently bound within the copolymer during polymerization by one or more chemical linkages selected from ester, thioester, amide, or acid anhydride.
Primary linker with reactive termini and excess molar equivalents
The primary linker molecule is terminated on each end by at least two functional groups that are reactive and configured to form the chemical linkages with at least two functional groups on the prodrug, and the molar equivalents of the primary linker molecule exceed the molar equivalents of the prodrug.
Hydrophilic secondary linker cross-linking to the prodrug
The secondary linker molecule is hydrophilic and comprises two functional groups configured to form covalent bonds with functional groups on the primary linker molecule thereby cross-linking to the prodrug molecule.
Microparticle hydrogel prodrug with defined diameter range
The hydrogel prodrug is a microparticle comprising a diameter within the range of 1 to 300 microns.
The claim coverage centers on a copolymer-embedded prodrug system where drug release is driven by hydrolysis of the copolymer, with a reactive primary linker in molar excess, a hydrophilic secondary linker that cross-links, and a microparticle diameter range of 1 to 300 microns.
Stated Advantages
Release of the drug upon degradation of the copolymer via hydrolysis.
Biodegradation via hydrolysis to release native, unaltered drug from ester linkages.
Sustained release formulations are described.
Documented Applications
Therapeutic use across multiple disease areas with sustained release formulations.
Formulation and manufacturing into mold casting, films, dressings, scaffolds, tablet, implantable device, capsule, 3D printing, injectable microparticles, microparticles, and microparticle-based dosage forms.
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