Boron Small Molecules for Fungal Nail 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 the nail's impermeability, which limits drug penetration and patient compliance.
Innovation Solution
Development of compounds targeting the editing domain of aminoacyl-tRNA synthetases, specifically cyclic boronic esters that enhance drug penetration through the nail, providing a new class of antimicrobial therapeutics.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If long-term systemic therapy is used to treat onychomycosis, then therapeutic effect is achieved, but adverse effects such as liver toxicity and reduced testosterone levels occur
Solution Approach 1:
The patent introduces an intermediary substance (penetration enhancer) that facilitates drug delivery through the nail plate without requiring systemic administration. This mediator enables localized treatment by enhancing percutaneous absorption, thereby achieving therapeutic effect at the infection site while avoiding systemic circulation and associated adverse effects.
Solution Approach 2:
The treatment approach is segmented into localized topical application rather than systemic distribution. The drug is delivered specifically to the nail and nail bed area where the infection exists, separating the treatment site from the rest of the body to avoid systemic adverse effects while maintaining therapeutic efficacy at the target site.
2Ease of operation
If topical therapy is applied to treat fungal infections, then patient compliance is improved, but drug penetration through the nail is insufficient due to the nail's impermeability
Solution Approach 1:
The patent modifies the physical-chemical parameters of the drug delivery system by incorporating penetration enhancers that alter the permeability characteristics of the nail plate. These enhancers change the physicochemical state of the nail barrier, enabling sufficient drug penetration while maintaining the convenience of topical application and patient compliance.
3Device complexity
If conventional topical formulations are used, then application simplicity is maintained, but the thick and awkward bandages required lead to poor patient compliance
Solution Approach 1:
The patent employs thin film formulations instead of thick bandages. The drug is delivered in a thin, flexible film form that can be easily applied to the nail area without causing discomfort or awkwardness, thereby maintaining application simplicity while significantly improving patient compliance through enhanced comfort and ease of use.
Data Source
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.