Oral Chelating Formulation with MSM Permeation Enhancer

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Solution Overview

Problem

Current treatments for dental and gingival diseases, such as periodontitis and gingivitis, face challenges due to the resistance of biofilm bacteria to antibiotics and antimicrobial agents, and the complexity of using multiple formulations for various oral disorders often results in cross-reactions between different active agents.

Innovation Solution

A multifunctional oral formulation comprising a biocompatible chelating agent like EDTA and a permeation enhancer like methylsulfonylmethane, administered as a solution, suspension, paste, gel, or liposomal dispersion, or in a controlled release implant, which effectively targets and treats multiple oral conditions by facilitating the delivery of the chelating agent through oral tissues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If antibiotic doses are increased to kill biofilm bacteria, then bacterial elimination is improved, but patient safety deteriorates due to higher toxicity risk

Engineering Contradiction:
Improvebiofilm bacteria eliminationVSAvoidpatient toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses chelating agents as intermediary substances that bind to metal ions in the biofilm, disrupting the biofilm structure and bacterial metabolism without requiring high doses of toxic antibiotics. The chelating agent acts as a mediator that attacks the biofilm's protective mechanisms rather than directly killing bacteria, thereby avoiding the toxicity problem of high-dose antibiotic therapy.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical/chemical killing mechanism of antibiotics with a chelation-based mechanism. Instead of using antibiotics that directly kill bacteria through biochemical pathways, the invention uses chelating agents that remove essential metal ions from the biofilm environment, causing bacterial death through nutrient deprivation rather than direct toxic action.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

2Adaptability or versatility

If multiple formulations with different active agents are used to treat various oral disorders, then treatment coverage is improved, but cross-reactions between agents worsen

Engineering Contradiction:
Improvetreatment coverageVSAvoidcross-reaction risk
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent creates a universal chelating agent formulation that can treat multiple different oral disorders (gingivitis, periodontitis, dental caries, oral cancer) through a single mechanism of action. The chelating agent works against diverse pathogens and conditions by removing metal ions that are common to all biofilm structures, eliminating the need for multiple specialized formulations and their associated cross-reaction risks.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Reliability

If mechanical removal is used to control dental plaque biofilms, then biofilm elimination is improved, but treatment complexity and patient discomfort worsen

Engineering Contradiction:
Improvebiofilm controlVSAvoidtreatment simplicity
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent replaces mechanical removal methods (scaling, root planing, surgery) with a chemical chelation approach. The chelating agent solution is applied topically to the oral tissues, where it penetrates and dissolves biofilm structures through metal ion chelation. This substitution transforms a complex, invasive mechanical procedure into a simple, non-invasive topical application.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

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 formulation effectively penetrates oral tissues, reduces biofilm resistance, and treats conditions like gingivitis and periodontal disease by chelating metal ions, reducing oxidative damage, and improving dental hygiene without the cross-reactivity issues of multiple formulations.

Implementation Method 1

an effective concentration of a permeation enhancer which is methylsulfonylmethane

Methodology Applied
Scientific EffectPermeation enhancement: Permeation

Implementation Method 2

a biocompatible chelating agent at a concentration of at least 0.1% by weight

Methodology Applied
Scientific EffectChelation: Chemical Bonding

Data Source

PatentEP2844344B1Treating inflammatory conditions and improving oral hygiene using metal modulators with methylsulfonylmethane as transport enhancer
Publication Date: 2021.01.13 BHUSHAN RAJIV
  • EP2844344B1 patent drawingFigure 1~1B

AI summary

Oral formulations provided for prevention and treatment of adverse oral conditions such as gingivitis, periodontal disease, removal of calculus to improve dental hygiene, and control of dental plaque and biofilm. Use of the formulations for prevention and treatment of other adverse oral conditions including inflammation and oxidative and/or free radical damage within the oral cavity are provided. Treatable conditions may relate to other conditions or diseases, including diabetes, AIDS and cancer. Oral formulations containing a biocompatible chelating agent, and a permeation enhancer such as methylsulfonylmethane (MSM) are disclosed. Components of the formulations are multifunctional and Generally Regarded As Safe.