Boron Compounds Nail Plate Penetration

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Solution Overview

Problem

Current treatments for ungual and periungual infections, such as onychomycosis, face challenges including long-term systemic therapy with adverse effects, invasive surgical procedures, and ineffective topical applications due to poor drug penetration through the nail tissue.

Innovation Solution

Development of boron compounds with specific molecular structures that can penetrate the nail plate and deliver antifungal agents effectively to the nail bed, enhancing treatment efficacy while minimizing side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If long term systemic administration of antifungal agent is used, then therapeutic effect in nail bed is achieved, but adverse effects and patient non-compliance increase

Engineering Contradiction:

Improvetherapeutic effectVSAvoidadverse effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses nail as an intermediary delivery system. The antifungal agent is incorporated into nail polish or nail hardener formulations, allowing the nail itself to serve as a reservoir and delivery mechanism that releases the drug directly into the nail bed over time, eliminating the need for long-term systemic administration and its associated adverse effects

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical/systemic administration route (oral tablets requiring daily compliance) with a topical application system where the nail polish or hardener is applied to the nail surface, which then delivers the drug through the nail plate to the nail bed, substituting a local delivery mechanism for systemic delivery

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Ease of operation

If topical application of conventional creams or lotions is used, then ease of application is improved, but drug penetration through nail tissue is insufficient

Engineering Contradiction:

Improveease of applicationVSAvoiddrug penetration

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent changes the physical and chemical parameters of the topical formulation by using nail polish or nail hardener as the delivery vehicle instead of conventional creams or lotions. These formulations have different viscosity, solubility, and penetration properties that enable them to effectively deliver antifungal agents through the nail plate to the nail bed

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite formulations combining antifungal agents with nail polish or nail hardener bases. These composite materials leverage the penetrative properties of the nail polish/hardener vehicle combined with the therapeutic activity of the antifungal agent to achieve effective drug delivery through the nail tissue

Inventive Principle:

Principle #40Composite materials

3Reliability

If surgical removal of nail is performed, then access to infected tissue is improved, but patient discomfort and cosmetic appearance deteriorate

Engineering Contradiction:

Improveaccess to infected tissueVSAvoidpatient discomfort

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses nail polish or nail hardener as an intermediary delivery system that provides controlled release of antifungal agents directly to the nail bed through the intact nail plate, eliminating the need for surgical nail removal and its associated patient discomfort and cosmetic concerns

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 boron compounds achieve therapeutic levels of antifungal agents in the nail bed, improving treatment outcomes for ungual and periungual infections with reduced adverse effects and enhanced patient compliance.

Implementation Method 1

Topical formulations for fungal infection treatment have largely tried to deliver the drug to the target site (an infected nail bed) by diffusion across or through the nail

Methodology Applied

Scientific EffectDiffusion: Diffusion

Data Source

PatentUS8039451B2Boron-containing small molecules

Publication Date: 2011.10.18 ANACOR PHARMACEUTICALS LLC

AI summary

This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.