Enamel-Binding Antibacterial Peptide Compositions for Remineralization

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Solution Overview

Problem

Current oral care products are inadequate in preventing and treating dental caries due to issues with antibacterial adhesion, sensitivity to oxidative damage, and toxicity, and they fail to effectively induce mineralization of tooth surfaces.

Innovation Solution

Development of peptides with high affinity for tooth enamel that possess both antimicrobial and mineralizing properties, such as histatin 5 segments and phosphoserine domains, to prevent bacterial adhesion, reduce demineralization, and promote remineralization.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If chemical surface modifications such as polyethylene glycol and zwitterion are used as nonspecific coatings, then anti-adhesive properties are demonstrated, but low surface densities and sensitivity to oxidative damage result in failure of antibacterial adhesion for long-term applications

Engineering Contradiction:
Improveantibacterial adhesionVSAvoidsurface coating stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent changes the chemical parameters of the surface coating by using phosphoserine-containing peptides instead of conventional polyethylene glycol or zwitterion coatings. This parameter change provides both antibacterial adhesion and oxidative stability, resolving the contradiction between reliability and compositional stability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite surface coating system that combines phosphoserine residues with peptide structures. This composite approach integrates the adhesive properties needed for antibacterial function with the chemical stability required for long-term performance, overcoming the limitations of single-material coatings.

Inventive Principle:
Principle #40Composite materials

2Reliability

If antibiotics are used to prevent caries pathogen biofilm formation, then antibacterial activity is achieved, but potential to result in antibiotic resistance and subsequent side effects occurs

Engineering Contradiction:
Improveantibacterial activityVSAvoidantibiotic resistance
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs short peptides with antibacterial activity that can be continuously applied through oral care products. These peptides serve as disposable, renewable antibacterial agents that do not accumulate in the body, thereby avoiding the development of resistance while maintaining continuous protective activity.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The phosphoserine-containing peptides act as intermediary substances that provide antibacterial protection through a different mechanism than traditional antibiotics. They interfere with bacterial adhesion and biofilm formation rather than killing bacteria directly, reducing selective pressure for resistance development.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If fluorides are used to show certain antibacterial activities, then antibacterial effect is achieved at very high concentrations, but difficulty to continuously sustain their topical concentrations on the tooth and toxicity concerns arise

Engineering Contradiction:
Improveantibacterial activityVSAvoidtopical concentration
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention changes the concentration parameter by using peptides that are effective at much lower concentrations than fluorides. The phosphoserine-containing peptides achieve antibacterial and anti-adhesive effects at trace levels, eliminating the need for high concentrations and associated toxicity concerns.

Inventive Principle:
Principle #35Parameter changes

4Reliability

If fluoride- and calcium phosphate-based reagents such as casein phosphopeptide-amorphous calcium phosphate are used to induce mineral deposits on tooth surfaces, then mineralization is promoted, but the deposits do not actually become part of the enamel microstructure

Engineering Contradiction:
Improvemineralization capabilityVSAvoidenamel microstructure integration
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The phosphoserine-containing peptides serve as molecular intermediaries that facilitate the integration of mineral deposits into the enamel microstructure. The phosphoserine residues interact with both the peptide and the mineral components, enabling proper incorporation of calcium phosphate deposits into the enamel matrix rather than forming separate surface layers.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 peptides effectively bind to tooth surfaces, reducing bacterial biofilm formation, preventing demineralization, and promoting mineralization, thereby enhancing oral health and reducing the risk of dental caries.

Implementation Method 1

Peptides that bind with high affinity to oral cavity surfaces, such as tooth enamel

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 2

inducing its remineralization

Methodology Applied
Scientific EffectMineralization: Crystallisation

Data Source

PatentUS20250275905A1Antibacterial and mineralizing compositions and methods of use thereof
Publication Date: 2025.09.04 THE UNIVERSITY OF HONG KONG
  • US20250275905A1 patent drawing
  • US20250275905A1 patent drawing
  • US20250275905A1 patent drawing

AI summary

Peptides that bind with high affinity to oral cavity surfaces, such as tooth enamel, have been discovered. The peptides exhibit antibacterial and mineralizing abilities, and are useful in many aspects of oral care. A preferred peptide includes the amino acid sequence AKRHHGYKRKFH-SpSp. The peptides can be included in oral care compositions such as toothpastes and mouthwashes. The oral care compositions can be used in methods to treat or prevent diseases or conditions induced by acidophilic oral bacteria. Exemplary methods include reducing or preventing tooth decay or demineralization, biofilm or dental plaque formation, and/or bacterial adhesion to a tooth surface; and promoting mineralization of teeth surfaces.