Chlorhexidine Nanoparticles for Sustained Antimicrobial Release

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Solution Overview

Problem

Current antimicrobial compositions using chlorhexidine (CHX) suffer from short-term delivery and limited release of CHX, necessitating frequent application and restricted antimicrobial efficacy due to solubility limitations, which is not easily controllable and may not be sufficient for extended periods.

Innovation Solution

Development of antimicrobial micro- or nanoparticles (MNPs) comprising CHX salts with sparingly soluble anions like phosphates, particularly cyclic metaphosphates, which provide a tailored release profile, enabling extended release of CHX over months or sustained release for up to 90 days, and can be used in various applications including medical articles and composite materials.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If soluble CHX salts (e.g., CHX digluconate) are used in antimicrobial compositions, then CHX can be delivered to target areas, but the delivery is limited to very short-term and levels are severely depleted within minutes

Engineering Contradiction:
Improveduration of CHX deliveryVSAvoidamount of CHX released
Core Design Contradiction:
Duration of action of moving objectVSQuantity of substance

Solution Approach 1:

The patent changes the solubility parameter of CHX salts by selecting sparingly soluble salts (e.g., CHX diacetate, CHX sulfate, CHX phosphate) instead of highly soluble salts like CHX digluconate. This parameter change enables the CHX to be released slowly over extended periods (days to weeks) rather than being rapidly depleted within minutes, thereby resolving the contradiction between delivery duration and quantity released.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If the concentration of CHX solution is increased to improve antimicrobial efficacy, then the amount of CHX per unit surface area increases, but the release becomes uncontrollable and may not be sufficient for extended periods

Engineering Contradiction:
Improveantimicrobial efficacyVSAvoidcontrollability of release
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent changes the solubility parameter of the CHX salt to achieve a balanced release profile. Sparingly soluble CHX salts provide a controlled, steady release of CHX over extended periods, maintaining reliable antimicrobial efficacy without the uncontrollable rapid release associated with high-concentration soluble CHX solutions.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material systems where CHX salts are integrated with various substrates (polymer coatings, medical devices, wound dressings). These composite structures control the release kinetics of CHX, providing both sustained antimicrobial efficacy and controllable release profiles.

Inventive Principle:
Principle #40Composite materials

3Productivity

If CHX is released rapidly in high amounts, then decontamination of stubborn infections can be achieved, but the release duration is too short requiring repeat treatments

Engineering Contradiction:
Improverate of CHX releaseVSAvoidduration of CHX release
Core Design Contradiction:
ProductivityVSDuration of action of moving object

Solution Approach 1:

The patent utilizes sparingly soluble CHX salts that inherently provide both adequate release rates and extended duration. The controlled solubility ensures sufficient CHX is released to treat infections while maintaining release over days or weeks, eliminating the need for frequent repeat treatments.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates sustained periodic release of CHX from the sparingly soluble salts, where CHX is continuously released at controlled rates over extended periods. This periodic action maintains therapeutic levels without requiring repeated applications, resolving the contradiction between release rate and duration.

Inventive Principle:
Principle #19Periodic action

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 CHX MNPs offer a controlled and prolonged release of antimicrobial agents, providing enhanced antimicrobial efficacy and prolonged protection against microbial growth on surfaces and in medical applications, with the ability to release higher doses quickly or maintain steady levels over extended periods.

Implementation Method 1

provide extended release of CHX over months rather than simply days or weeks

Methodology Applied
Scientific EffectDissolution:

Data Source

PatentEP2996468B1Antibacterial micro- and nanoparticles comprising a chlorhexidine salt, method of production and uses thereof
Publication Date: 2019.04.10 PERTINAX PHARMA LTD
  • EP2996468B1 patent drawingFigure 1a~1d
  • EP2996468B1 patent drawingFigure 2e~2g
  • EP2996468B1 patent drawingFigure 3~4

AI summary

Antimicrobial micro- or nanoparticles comprising a chlorhexidine salt and an anion, and a method of making the antimicrobial micro-or nanoparticle, are disclosed. The anion in the salt is selected from oxoanions and partially hydrogenated oxoanions of phosphorus, carbon, nitrogen, and sulfur.