Cyclodextrin-Methylglyoxal Complexes for Stable Antimicrobial Activity

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Solution Overview

Problem

Manuka honey's antimicrobial activity is unstable and requires frequent application or ingestion for effective treatment of microbial infections, necessitating the development of compositions that maintain or enhance its antimicrobial properties for prolonged durations.

Innovation Solution

Formulating antimicrobial compositions containing methylglyoxal and cyclodextrin, with manuka honey as a primary component, to maintain or enhance the antimicrobial activity, suitable for various applications including pharmaceuticals, consumer goods, and industrial use.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If manuka honey is used for treatment of microbial infections, then antimicrobial activity is achieved, but the activity is unstable and requires frequent application

Engineering Contradiction:
Improveantimicrobial activity stabilityVSAvoidduration of antimicrobial activity
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent introduces cyclodextrin as an intermediary substance that forms inclusion complexes with methylglyoxal from manuka honey. This complexation stabilizes the antimicrobial agent, preventing its rapid degradation and extending its active lifespan in the composition, thereby resolving the instability issue without requiring frequent reapplication

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If manuka honey is applied frequently to maintain effectiveness, then antimicrobial activity is sustained, but dosage frequency and convenience are reduced

Engineering Contradiction:
Improveantimicrobial activity maintenanceVSAvoidapplication frequency convenience
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent formulates a composition where cyclodextrin-methylglyoxal inclusion complexes provide continuous release and sustained antimicrobial activity. This eliminates the need for frequent applications while maintaining effective treatment levels, as the complexed form releases methylglyoxal progressively over time

Inventive Principle:
Principle #20Continuity of useful action

3Reliability

If manuka honey concentration is increased to enhance antimicrobial activity, then efficacy is improved, but composition stability and safety are compromised

Engineering Contradiction:
Improveantimicrobial efficacyVSAvoidcomposition stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

Cyclodextrin serves as a stabilizing intermediary that binds to methylglyoxal molecules, preventing their premature reaction or degradation. This allows the composition to maintain high antimicrobial efficacy through sustained methylglyoxal availability while preserving composition stability and safety profiles

Inventive Principle:
Principle #24Intermediary (Mediator)

4Reliability

If manuka honey is used in pharmaceutical formulations, then antimicrobial treatment is achieved, but manufacturing complexity and formulation stability are challenges

Engineering Contradiction:
Improveantimicrobial treatment effectivenessVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent employs cyclodextrin as a formulation intermediary that simplifies the integration of manuka honey extracts into pharmaceutical compositions. The inclusion complex formation provides a stable, pre-formed delivery mechanism that reduces formulation complexity and enhances storage stability while maintaining treatment effectiveness

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 compositions sustain antimicrobial activity for extended periods, reducing dosage frequency and enhancing efficacy, while being safe for human use and applicable in treating microbial infections and promoting wound healing.

Implementation Method 1

The present invention is based on the finding that by admixing, for example by mixing and powderizing, materials comprising methylglyoxal and materials comprising cyclodextrin, the antimicrobial activity of the original materials is at least maintained or preferably is enhanced

Methodology Applied
Scientific EffectInclusion complex formation:

Data Source

PatentEP2344170B1Antimicrobial compositions
Publication Date: 2016.02.24 MANUKA HEALTH NEW ZEALAND LIMITED
  • EP2344170B1 patent drawingFigure 1~2
  • EP2344170B1 patent drawingFigure 3~4
  • EP2344170B1 patent drawingFigure 5

AI summary

This invention provides antimicrobial compositions containing methylglyoxal and material with methylglyoxal contained (such as manuka honey). The antimicrobial activity of methylglyoxal, or material with a methylglyoxal presence, is maintained and/or enhanced by mixing methylglyoxal or material with a methylglyoxal presence with cyclodextrin. Methods of preparing such compositions, including powder composition, and methods of using such compositions are also provided.