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Publication Number
US-12083184-B2
Publication Date
2024-09-10
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 invention relates to a method of making a hydrogel prodrug by providing at least one drug that comprises at least one amine group and providing at least one acrylate. The acrylate reacts with the amine group of the drug in a polymerization reaction to produce at least one polymer prodrug, and the resulting hydrogel prodrug comprises a backbone structure comprising polymerized polymer prodrug.
The method further includes cross-linking the polymer prodrug in the presence of a free radical initiator and a catalyst in a reaction mixture to make the hydrogel prodrug. The acrylate-to-drug molar ratio is between about 1.05:1 and about 5:1.
The disclosure includes hydrogel prodrug embodiments in which selected acrylate/diacrylate components and varying ratios tune degradation and release kinetics. The document describes hydrogel prodrug examples using amine-containing drugs such as mesalamine and tranexamic acid, with controlled or zero-order drug release synchronized with degradation.
Claims Coverage
The independent claim covers three inventive features: forming a polymer prodrug by reacting an amine-containing drug with an acrylate via a polymerization reaction, cross-linking the polymer prodrug with a free radical initiator and a catalyst to form a hydrogel prodrug backbone comprising polymerized polymer prodrug, and satisfying a defined acrylate-to-drug molar ratio.
Acrylate/amine polymerization to form a polymer prodrug
Providing at least one drug that comprises at least one amine group; providing at least one acrylate; reacting said at least one acrylate with the at least one amine group of the at least one drug, thereby producing at least one polymer prodrug, wherein the reacting comprises a polymerization reaction.
Free radical initiator and catalyst cross-linking to make a hydrogel prodrug backbone
Cross-linking said at least one polymer prodrug in the presence of a free radical initiator and a catalyst in a reaction mixture, thereby making the hydrogel prodrug, wherein the hydrogel prodrug comprises a backbone structure, wherein the backbone structure comprises polymerized polymer prodrug.
Acrylate-to-drug molar ratio constraint
Wherein the molar ratio of the at least one acrylate to the at least one drug is between about 1.05:1 and about 5:1.
Overall, the claim coverage centers on forming a polymer prodrug by polymerizing an acrylate with an amine-containing drug, then cross-linking the polymer prodrug with a free radical initiator and a catalyst to obtain a hydrogel prodrug backbone comprising polymerized polymer prodrug, under a defined acrylate-to-drug molar ratio.
Stated Advantages
Preferred zero-order release kinetics to provide a constant drug level.
Reduced initial burst compared to conventional systems.
Controlled/zero-order drug release.
Drug release synchronized with degradation.
Documented Applications
Treatment of cancer.
Treatment of HIV and viral infections.
Treatment of pain.
Treatment of bacterial disorders.
Treatment of neurological disorders.
Treatment of hemorrhaging.
Treatment of multiple sclerosis.
Treatment of diabetes.
Treatment of hypertension.
Treatment of Alzheimer’s.
Treatment of fungal growth.
Therapeutic use for sustained release targeting diseases including cancer, HIV/viruses, pain, infections, neurological disorders, hemorrhaging, multiple sclerosis, diabetes, hypertension, Alzheimer’s, and fungal growth.
Hydrogel prodrug examples using amine-containing drugs including mesalamine.
Hydrogel prodrug examples using amine-containing drugs including tranexamic acid.
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