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Publication Number
US-10413616-B2
Publication Date
2019-09-17
Expiration Date
Abstract
Aspects of the invention described herein include a hydrogel prodrug and methods of making a hydrogel prodrug for drug deliver}′. 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. The method includes providing at least one drug comprising at least one amine group and reacting the amine group with at least one acrylate in a polymerization reaction to produce a polymer having the prodrug bound within the polymer. The hydrogel prodrug comprises a backbone structure in which the backbone structure comprises polymerized polymer prodrug.
The polymer prodrug is then cross-linked in the presence of a free radical initiator in a reaction mixture to make the hydrogel prodrug. This combines polymerization of the drug with acrylate and hydrogel network formation via free radical initiator cross-linking.
The disclosure further supports hydrogel prodrug delivery systems formed by polymerizing a drug containing amine groups with acrylates and cross-linking the polymer prodrugs with a free-radical initiator. It includes selected acrylates including diacrylates, chemical spacers that contain free primary and/or secondary amine groups incorporated into the hydrogel backbone, and multi-drug hydrogel prodrug formulations.
Claims Coverage
The patent includes one independent claim directed to a method of making a hydrogel prodrug by polymerizing an acrylate with a drug containing amine groups and then cross-linking the resulting polymer prodrug in the presence of a free radical initiator. Dependent claims refine particular acrylates and diacrylates, drugs, initiators, and an amine-containing chemical spacer. The core inventive coverage centers on a backbone structure comprising polymerized polymer prodrug.
Polymerizing an amine-containing drug with an acrylate to form a polymer-bound prodrug
Providing at least one drug that comprises at least one amine group; providing at least one acrylate; reacting the acrylate with the amine group of the drug in a polymerization reaction, thereby producing a polymer having the prodrug bound within said polymer.
Cross-linking the polymer prodrug with a free radical initiator to make the hydrogel prodrug
Cross-linking said at least one polymer prodrug in the presence of a free radical initiator in a reaction mixture, thereby making the hydrogel prodrug.
Hydrogel prodrug having a backbone structure comprising polymerized polymer prodrug
Wherein the hydrogel prodrug comprises a backbone structure, wherein the backbone structure comprises polymerized polymer prodrug.
Across the independent claim, the coverage is directed to binding an amine-group drug to an acrylate-containing polymer through polymerization, then converting the resulting polymer prodrug into a hydrogel prodrug by cross-linking in the presence of a free radical initiator. Dependent claims further narrow specific acrylates and diacrylates, specified drug entities or classes, specified free radical initiators, and a chemical spacer with free primary and/or secondary amine groups incorporated into the hydrogel backbone.
Stated Advantages
Provides synchronized polymer degradation and drug release with minimal initial burst drug release.
Enables tunable degradation and release behavior by selection of diacrylates as described in the disclosure.
Supports longer-term drug release behavior described as hours to days/weeks/months in the disclosure.
Documented Applications
Hydrogel prodrug forms intended for therapeutic use where targeting moieties and multiple cancer antigen examples are mentioned, including EGFR, HER2, and Mesothelin.
Example therapeutic contexts described in the disclosure include polymer prodrug formation using mesalamine and tranexamic acid.
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