Nail Antifungal Patch Using Crosslinking Hydrogel

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Solution Overview

Problem

Conventional external preparations for nail mycosis have low permeability to the nail, leading to unsatisfactory therapeutic effects, and existing solutions face issues with stability, complexity, and adverse effects from organic solvents.

Innovation Solution

A pharmaceutical composition for nail comprising an antifungal drug, alkylpyrrolidone or its derivative, and a crosslinking hydrogel, applied as an adhesive patch to enhance drug permeability and stability, eliminating the need for ethanol and simplifying the treatment process.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If a water-insoluble film forming agent is used to achieve film strength and water resistance, then film strength is improved, but drug discharge from the film increases and permeability to nail decreases

Engineering Contradiction:

Improvefilm strengthVSAvoiddrug retention

Core Design Contradiction:

StrengthVSReliability

Solution Approach 1:

The patent changes the chemical nature of the film-forming agent from water-insoluble to water-soluble, fundamentally altering the system's properties. This enables the film to maintain structural integrity while allowing antifungal drugs to permeate through and reach the nail, resolving the contradiction between film strength and drug retention

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite formulation combining water-soluble film-forming agents with antifungal drugs, where the hydrophilic matrix enables both film formation and drug delivery. This composite approach allows simultaneous achievement of film strength and drug permeability

Inventive Principle:

Principle #40Composite materials

2Strength

If organic agents such as acetone, ethyl acetate, and toluene are used to harden the nail, then film hardness is improved, but drug permeability to nail decreases due to nail dehydration

Engineering Contradiction:

Improvenail hardnessVSAvoiddrug permeability

Core Design Contradiction:

StrengthVSReliability

Solution Approach 1:

The patent eliminates harmful organic solvents that dehydrate the nail and instead uses water-based formulations. The hydrophilic film-forming agent creates a moist environment that softens the nail slightly, actually enhancing drug permeability while avoiding the harmful dehydration effect of organic agents

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent changes the solvent system from organic to aqueous, fundamentally altering how the nail is treated. Instead of dehydrating and hardening the nail with organic solvents, the water-based system maintains nail hydration, creating optimal conditions for drug penetration

Inventive Principle:

Principle #35Parameter changes

3Stability of the object's composition

If a water content of 3% to 10% is used in the composition, then composition stability is improved, but drug permeability to nail decreases

Engineering Contradiction:

Improvecomposition stabilityVSAvoiddrug permeability

Core Design Contradiction:

Stability of the object's compositionVSReliability

Solution Approach 1:

The patent dramatically increases the water content from 3-10% to 70-90%, fundamentally changing the composition's properties. This high water content creates a hydrophilic environment that enhances drug solubility and permeability while the crosslinked polymer network maintains composition stability through gel formation

Inventive Principle:

Principle #35Parameter changes

4Quantity of substance

If a hydrochloride salt is used to increase water-solubility of slightly water-soluble antifungal drugs, then water-solubility is improved, but the method is not versatile as not every antifungal drug responds to this transformation

Engineering Contradiction:

Improvewater-solubilityVSAvoidmethod versatility

Core Design Contradiction:

Quantity of substanceVSAdaptability or versatility

Solution Approach 1:

The patent changes the approach from chemical modification (hydrochloride salt formation) to physical formulation (water-based gel system). This formulation strategy universally enhances water-solubility for all antifungal drugs without requiring chemical transformation, making the method universally applicable to different drug classes

Inventive Principle:

Principle #35Parameter changes

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 composition significantly enhances drug permeability and retention, providing effective treatment for nail tinea with improved stability and convenience, as demonstrated by increased antifungal drug accumulation in nail plates and long-term storage stability.

Implementation Method 1

a crosslinking hydrogel

Methodology Applied

Scientific EffectHydrogel: Hydrogel

Implementation Method 2

alkylpyrrolidone or a derivative thereof

Methodology Applied

Scientific EffectSolvation: Solvation

Data Source

PatentUS9579297B2Pharmaceutical composition for application to nail

Publication Date: 2017.02.28 TEIKOKU SEIYAKU CO LTD

AI summary

Since treatment effects of conventional external preparations were not satisfactory, it is aimed to provide a novel external preparation that is excellent in drug permeability to nail, capable of fully exhibiting effects of an antifungal drug, and effective for treatments of diseases such as nail mycosis and nail candidiasis, particularly, treatments for nail tinea. The external preparation of this invention is a pharmaceutical composition for nail characterized by containing an antifungal drug, alkylpyrrolidone or a derivative thereof, and a crosslinking hydrogel.