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Publication Number
US-10406241-B2
Publication Date
2019-09-10
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 disclosed invention provides a hydrogel prodrug delivery system that includes a copolymer comprising a prodrug which generates a native form of a drug upon hydrolysis. The prodrug is covalently bound within the copolymer during polymerization through chemical linkages selected from ester, thioester, amide, or acid anhydride, and degradation of the copolymer via hydrolysis releases the native form of the drug.
The system further includes a primary linker molecule and a secondary linker molecule to enable covalent association between the prodrug and the copolymer. The primary linker molecule is terminated on each end by at least two functional groups that are reactive and configured to form said 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. The provided material also describes sustained, near-linear or zero-order release behavior with minimal initial burst, with release completion coinciding with hydrogel degradation.
Claims Coverage
Independent claim clm-00001 defines a hydrogel prodrug delivery system with five core inventive features: hydrolysis-based release of native drug, covalent prodrug incorporation through defined linkages, a primary linker with reactive termini in excess equivalents, and a hydrophilic secondary linker that cross-links to the prodrug.
Hydrogel prodrug copolymer that releases native drug on hydrolysis
A hydrogel prodrug delivery system comprising a copolymer, comprising a prodrug which generates a native form of a drug upon hydrolysis, and wherein the copolymer is formulated to release a native form of the drug upon degradation of the copolymer via hydrolysis.
Covalent prodrug incorporation via hydrolysable linkages during polymerization
The prodrug is covalently bound within the copolymer during polymerization of the copolymer by one or more chemical linkages selected from ester, thioester, amide, or acid anhydride.
Primary linker with dual reactive termini forming chemical linkages to the prodrug
The primary linker molecule is terminated on each end by at least two functional groups, which are reactive and configured to form said one or more chemical linkages with at least two functional groups on said prodrug.
Primary linker used in greater molar equivalents than prodrug
The molar equivalents of said primary linker molecule exceed the molar equivalents of said prodrug.
Hydrophilic secondary linker with two functional groups for cross-linking
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.
Independent claim clm-00001 centers on a hydrogel prodrug copolymer in which a hydrolysis-cleavable covalent linkage connects the prodrug to the polymer, supported by a primary linker with reactive dual termini used in excess equivalents and a hydrophilic secondary linker that cross-links to the prodrug, enabling release of the native drug upon hydrolytic degradation.
Stated Advantages
Releases a native form of the drug upon degradation of the copolymer via hydrolysis.
Provides hydrolysis-based degradation associated with drug release, described as hydrolysis-triggered release of native, unaltered drug.
Described to target sustained, near-linear or zero-order release behavior with minimal initial burst, with release completion coinciding with hydrogel degradation.
Documented Applications
Therapeutic use for cancer.
Therapeutic use for HIV and viral infections.
Therapeutic use for pain.
Therapeutic use for bacterial infection.
Therapeutic use for neurological disorder, including multiple sclerosis.
Therapeutic use for diabetes.
Therapeutic use for hypertension.
Therapeutic use for Alzheimer’s.
Therapeutic use for antifungal growth.
Therapeutic formulation as a compressed sheet.
Therapeutic formulation as a scaffold, support, or wound dressing.
Therapeutic formulation as a subcutaneous tumor implant.
Therapeutic formulation as injectable microparticles.
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