Anionic Silica Particles Adsorbed with Chlorhexidine for Antibacterial Barriers

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Solution Overview

Problem

Current antimicrobial compositions using colloidal silica or titanium dioxide particles lack efficacy in forming a barrier against external microbes and have limited cutaneous tolerance, necessitating a new product that is effective against infections and inflammations while avoiding infections on epithelial surfaces.

Innovation Solution

Development of anionic silicon or titanium dioxide particles with an average size of at least 200 nm, adsorbed with chlorhexidine cations and cationic silver complexes through electrostatic interactions, forming a derivative that acts as an antibacterial, antimycotic, and antiviral agent, which can be used in topical formulations like creams or gels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Volume of moving object

If colloidal silica or titanium dioxide particles are used as antimicrobial compositions, then the particle size can be small (3-150 nm), but the efficacy in forming a barrier against external microbes is limited

Engineering Contradiction:
Improveparticle sizeVSAvoidbarrier formation efficacy
Core Design Contradiction:
Volume of moving objectVSReliability

Solution Approach 1:

The patent combines multiple active cationic species (chlorhexidine and silver complexes) on the same anionic二氧化硅 particle surface, creating a composite structure that merges antimicrobial efficacy with barrier formation capability. This merging allows the particles to simultaneously achieve small size and high reliability in preventing microbial infections.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention creates composite particles consisting of anionic二氧化硅 core with adsorbed cationic antimicrobial agents (chlorhexidine and/or silver complexes). This composite structure integrates the physical barrier properties of二氧化硅 with the chemical antimicrobial activity of the cationic species, resolving the contradiction between small particle size and effective barrier formation.

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If colloidal silica particles are used, then the dispersions are stable in pH range 8-10.5, but the cutaneous tolerance is limited

Engineering Contradiction:
Improvedispersion stabilityVSAvoidcutaneous tolerance
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent changes the surface charge parameter of the二氧化硅 particles from cationic to anionic, which fundamentally alters both the stability characteristics and biocompatibility. The anionic surface allows for electrostatic adsorption of cationic antimicrobial agents while improving cutaneous tolerance, thus resolving the contradiction between stability and skin compatibility.

Inventive Principle:
Principle #35Parameter changes

3Ease of manufacture

If silica is produced by acidic hydrolysis, then the silica structure is formed, but it cannot bind chlorhexidine through electrostatic interaction

Engineering Contradiction:
Improvesilica productionVSAvoidelectrostatic binding capability
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

Instead of producing cationic二氧化硅 particles and attempting to bind anionic species, the patent inverts the approach by producing anionic二氧化硅 particles and binding cationic antimicrobial agents (chlorhexidine and silver complexes). This inversion enables effective electrostatic interaction and resolves the binding capability issue while maintaining ease of manufacture through standard sol-gel methodology.

Inventive Principle:
Principle #13The other way round (Inversion)

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 anionic particles provide a synergistic antibacterial activity, forming a barrier against external microbes, effectively treating cutaneous irritations and infections with enhanced pharmacological activity, and can be used in medical devices for topical application.

Implementation Method 1

adsorbed with chlorhexidine cations and cationic silver complexes through electrostatic interactions

Methodology Applied
Scientific EffectElectrostatic interaction: Electrostatics

Implementation Method 2

anionic silicon or titanium dioxide particles, adsorbed with one or more pharmaceutical active cations

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentEP3003251B1Antibacterial powders based on anionic silicon or titanium dioxide adsorbed with pharmaceutically active cations
Publication Date: 2019.07.10 PAVIA FARM
  • EP3003251B1 patent drawingFigure 1
  • EP3003251B1 patent drawingFigure 2
  • EP3003251B1 patent drawingFigure 3

AI summary

The present invention relates to a dioxide silicon or titanium derivative of formula (I): (MO2)- (Am+) y, as active ingredient for the preparation of a composition having antibacterial properties useful, e.g. for topical administration. The dioxide derivatives of the present invention comprises anionic silica (SiO2)n- or anionic titanium dioxide particles (TiO2) n-, adsorbed with at least one cationic pharmaceutical active moiety (Am+), which may include, for instance, known antibacterial agents such as chlorexidine and the like. Furthermore, the invention relates to a composition for topical use, which may form an efficacious barrier against external microbes, substantially avoiding any infection on the affected skin.