PEG Hydrogel Prodrugs for Sustained Drug Release
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Solution Overview
Problem
Conventional hydrogels are limited in their ability to sustainably release larger drug molecules, such as proteins, due to structural obstructions that prevent access to the inner space, leading to low drug load and unpredictable release profiles.
Innovation Solution
A hydrogel process involving a mixture of backbone and crosslinker reagents with specific molecular weights and compositions, polymerized in suspension, allows for the controlled and sustained release of larger drug molecules by enabling their entry and attachment within the hydrogel network.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional hydrogels are used for drug delivery, then they can carry drug molecules, but they cause burst release and unpredictable drug release profiles
Solution Approach 1:
The patent changes the chemical parameters of the hydrogel by introducing specific crosslinking densities and using PEG-based polymers with controlled molecular weights. This creates a hydrogel network with optimized pore sizes and diffusion pathways that enable controlled, sustained drug release rather than burst release, improving both reliability and duration of action.
Solution Approach 2:
The patent creates a composite hydrogel system combining PEG-based polymers with specific crosslinking agents and drug molecules. This composite structure allows the hydrogel to provide both structural integrity and controlled drug release, resolving the contradiction between reliable release and sustained duration.
2Quantity of substance
If conventional hydrogels are used for carrying larger drug molecules, then they can provide a carrier function, but structural obstructions prevent access to inner space resulting in low drug load
Solution Approach 1:
The patent optimizes the hydrogel's physical parameters by controlling the molecular weight of PEG-based polymers (1-100 kDa) and crosslinker density to create an open network structure. This allows larger drug molecules to penetrate and access the inner space of the hydrogel, significantly increasing drug load while maintaining ease of access.
Solution Approach 2:
The patent creates local variations in hydrogel density and porosity through controlled crosslinking, allowing different regions of the hydrogel to have optimized properties for drug molecule access and retention, thereby increasing overall drug load without compromising accessibility.
3Adaptability or versatility
If hydrogels are used for controlled release of smaller drug molecules, then they can provide sustained release, but they do not provide sufficient access for larger drug molecules
Solution Approach 1:
The patent designs a universal hydrogel platform using PEG-based polymers with adjustable molecular weights and crosslinking densities that can accommodate both small and large drug molecules. This multi-functional hydrogel system maintains controlled release performance across different drug sizes by optimizing the network structure to be adaptable rather than size-specific.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The hydrogel effectively serves as a carrier for larger drug molecules, facilitating controlled and sustained release, overcoming previous limitations of structural access and drug load, and providing a stable release profile.
Implementation Method 1
polymerizing the mixture of step (a) in a suspension polymerization to a hydrogel
Implementation Method 2
Conventional hydrogels are three-dimensional, hydrophilic or amphiphilic polymeric networks capable of taking up large quantities of water
Implementation Method 3
These networks may be composed of various polymers and are insoluble due to the presence of covalent chemical and/or physical crosslinks
Data Source
AI summary
The present invention relates to a process for the preparation of a hydrogel and to a hydrogel obtainable by said process. The present invention further relates to a process for the preparation of a hydrogel-spacer conjugate, to a hydrogel-spacer conjugate obtainable by said process, to a process for the preparation of a carrier-linked prodrug and to carrier- linked prodrugs obtainable by said process, in particular to carrier- linked prodrugs that provide for a controlled or sustained release of a drug from a carrier. In addition, the invention relates to the use of the hydrogel for the preparation of a carrier-linked prodrug.