Hydrogel-forming composition for controlled release
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Solution Overview
Problem
Existing hydrogels for controlled drug release suffer from issues such as poor pharmacokinetic profiles, fast elimination, immunogenicity, toxicity, and non-uniform release properties, making them unsuitable for oral administration and requiring frequent injections, which negatively impact patient compliance.
Innovation Solution
Development of amphipathic peptide hydrogels with specific amino acid sequences that form stable, biocompatible networks for controlled release, allowing for sustained drug delivery without systemic absorption, thus reducing the need for frequent injections.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If chemical cross-linked hydrogels are used for controlled drug release, then the hydrogel structure stability is improved, but toxicity and immunogenicity increase
Solution Approach 1:
The patent changes the chemical composition parameters from synthetic cross-linked polymers to self-assembling peptides with specific amino acid sequences. This parameter change maintains hydrogel structural stability through peptide self-assembly while eliminating toxicity and immunogenicity associated with chemical cross-linkers like gluteraldehyde and degradation products of PLGA.
Solution Approach 2:
The patent uses composite peptide structures combining hydrophobic and hydrophilic amino acid residues to create amphipathic peptides. These composite structures enable self-assembly into stable hydrogel networks without requiring toxic chemical cross-linkers, thus maintaining structural stability while reducing harmful factors.
2Strength
If synthetic polymer hydrogels are used, then the mechanical strength is improved, but in vivo uncontrollable swelling causes pain
Solution Approach 1:
The patent changes the material composition from synthetic polymers to self-assembling peptides with controlled amino acid sequences. This enables tuning of the hydrogel's mechanical properties and swelling behavior through peptide sequence design, providing mechanical strength while controlling in vivo swelling to avoid pain.
Solution Approach 2:
The self-assembling peptides automatically regulate their own assembly and swelling behavior in response to physiological conditions without requiring external control mechanisms. The peptides self-regulate network formation and water uptake, providing mechanical strength while avoiding uncontrollable swelling and associated pain.
3Ease of manufacture
If non-uniform synthetic polymers are used, then the manufacturing process is simplified, but release properties become non-uniform
Solution Approach 1:
The patent changes from heterogeneous synthetic polymers to homogeneous self-assembling peptides with defined sequences. This enables precise control over release properties through sequence design while maintaining ease of manufacture through straightforward peptide synthesis and self-assembly processes.
Solution Approach 2:
The self-assembling peptides automatically form uniform structures through their inherent self-assembly properties, eliminating the need for complex manufacturing controls. The peptides self-organize into consistent nanofibrous networks with uniform pore sizes, ensuring uniform drug release without requiring sophisticated manufacturing precision.
4Quantity of substance
If large pore polymer networks are used, then the drug loading capacity is increased, but burst release effects occur
Solution Approach 1:
The patent changes the network structure from large-pore synthetic polymers to self-assembling peptide hydrogels with tunable pore sizes. By adjusting peptide concentration, sequence, and assembly conditions, the network can achieve optimal pore sizes that provide sufficient drug loading capacity while preventing burst release through controlled diffusion barriers.
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 amphipathic peptide hydrogels provide a controlled and slow release of drugs, improving patient compliance by maintaining therapeutic effects and reducing systemic absorption, while being biocompatible and non-toxic, suitable for oral administration.
Implementation Method 1
Self-assembling peptide hydrogels are formed by molecular self-assembly of the native peptides to nanoscale fibers
Implementation Method 2
The hydrogel network can encapsulate and release therapeutics via various mechanisms, such as (de)swelling, external triggers such as pH or temperature, erosion, or diffusion
Data Source
AI summary
The present invention provides peptide hydrogelators capable of forming hydrogels as carriers of active ingredients and acting as sustained or controlled release drug delivery systems.