Topical Composition Permeability via Penetration Enhancers
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Solution Overview
Problem
Topical compositions for treating fungal infections in the stratum corneum, particularly on the heels, have not been adequately developed to enhance antifungal agent permeability effectively.
Innovation Solution
A topical composition combining tolnaftate or its pharmaceutically acceptable salts with ester compounds of fatty acids, dihydric alcohols, lysine acyl glutamate, diethylene glycol-based glycol ethers, cyclohexanedicarboxylic acid polyoxyethylene alkyl ethers, mannosylerythritol lipids, and sucrose fatty acid esters to improve permeability through the stratum corneum.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional topical compositions are used for fungal infections in the stratum corneum, then the antifungal agent can be applied to the skin surface, but the permeability of the antifungal agent into the stratum corneum is insufficient
Solution Approach 1:
The patent employs penetration enhancers as intermediary substances that facilitate the transfer of antifungal agents through the stratum corneum barrier. These enhancers temporarily modify the skin barrier properties or interact with the antifungal agent to improve its permeation, thereby resolving the contradiction between surface application and deep penetration effectiveness.
Solution Approach 2:
The invention modifies physical and chemical parameters of the topical composition, including pH, solvent composition, and molecular structure of excipients, to optimize antifungal agent permeability. By adjusting these parameters, the formulation achieves better penetration into the stratum corneum while maintaining therapeutic effectiveness.
2Length of stationary object
If the stratum corneum thickness is increased (as in heel infections), then the fungal infection can be protected deeper in the skin, but the permeability of topical antifungal agents decreases
Solution Approach 1:
For thicker stratum corneum regions like heels, the patent uses potent penetration enhancers that can effectively traverse increased barrier thickness. These intermediaries create sufficient concentration gradients or temporary pathways that allow antifungal agents to reach deeper fungal infections despite the increased stratum corneum thickness.
Solution Approach 2:
The invention creates composite topical formulations combining multiple penetration enhancers with different mechanisms of action. This composite approach addresses the increased barrier thickness by providing multiple pathways for drug penetration, overcoming the reduced permeability associated with thicker stratum corneum in heel infections.
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 the permeation of antifungal agents into the stratum corneum, effectively treating fungal infections by improving the delivery of tolnaftate, thereby addressing the challenge of inadequate permeability in existing treatments.
Implementation Method 1
the use of both (A) one antifungal agent or two or more antifungal agents selected from the group consisting of tolnaftate and pharmaceutically acceptable salts thereof, and (B) one compound or two or more compounds selected from the group consisting of ester compounds of fatty acids having from 8 to 18 carbon atoms and dihydric alcohols having from 2 to 4 carbon atoms, lysine acyl glutamate, lysine diacyl glutamate, pharmaceutically acceptable salts of lysine acyl glutamate or lysine diacyl glutamate, diethylene glycol-based glycol ethers, cyclohexanedicarboxylic acid polyoxyethylene alkyl ethers, mannosylerythritol lipids, and sucrose fatty acid esters yielded a topical composition that improved permeability of component (A) in the stratum corneum
Data Source
AI summary
Problem: To provide a topical composition having excellent permeability in the stratum corneum. Solution: A topical composition is prepared that comprises: (A) one antifungal agent or two or more antifungal agents selected from the group consisting of tolnaftate and pharmaceutically acceptable salts thereof; and (B) at least one compound selected from the group consisting of ester compounds of fatty acids having from 8 to 18 carbon atoms and dihydric alcohols having from 2 to 4 carbon atoms, lysine acyl glutamate, lysine diacyl glutamate, pharmaceutically acceptable salts of lysine acyl glutamate or lysine diacyl glutamate, diethylene glycol-based glycol ethers, cyclohexanedicarboxylic acid polyoxyethylene alkyl ethers, mannosylerythritol lipids, and sucrose fatty acid esters.