Topical Corticosteroid Formulation with Multiplexed Penetration Enhancers
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current topical formulations face challenges in delivering active agents through the skin due to the skin's impermeable nature, particularly the stratum corneum, limiting the number of effective molecular penetration enhancers and transdermal drug administration options.
Innovation Solution
A topical formulation comprising a corticosteroid combined with specific multiplexed molecular penetration enhancers such as N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate, and sodium lauryl sulfoacetate, which improve the flux and stability of the corticosteroid when applied to the skin.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If molecular penetration enhancers are used to increase skin permeability, then the delivery of active agents through the skin is improved, but the number of suitable enhancers is limited due to skin irritation
Solution Approach 1:
The patent combines multiple penetration enhancers (N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate, and sodium lauryl sulfoacetate) into a composite formulation. This composite approach allows the synergistic interaction of different enhancers to achieve high skin permeability while reducing individual irritancy, thus expanding the range of usable penetration enhancers beyond what any single substance could provide.
2Reliability
If the stratum corneum barrier is reduced to facilitate drug penetration, then transdermal delivery is improved, but skin irritation and damage may occur
Solution Approach 1:
The patent optimizes the concentration parameters of each penetration enhancer in the formulation. By carefully controlling the amounts of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate, and sodium lauryl sulfoacetate, the formulation achieves effective stratum corneum disruption for drug delivery while maintaining skin tolerance and minimizing irritation.
Solution Approach 2:
The multiple penetration enhancers act as intermediaries that mediate between the active agent and the skin barrier. They temporarily reduce stratum corneum resistance to facilitate drug penetration, then allow the skin barrier to recover, thus enabling effective transdermal delivery without permanent damage or severe irritation.
3Object-affected harmful factors
If only a limited number of small lipophilic drugs are used for transdermal administration, then skin compatibility is maintained, but the range of treatable conditions is restricted
Solution Approach 1:
The composite penetration enhancer formulation enables the transdermal delivery of a broader range of active agents including corticosteroids and other drugs that would otherwise be unsuitable for skin administration. This expands the range of treatable conditions beyond what is achievable with traditional single-enhancer formulations limited to small lipophilic drugs.
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 significantly enhances the penetration of corticosteroids through the skin, achieving increased delivery and stability, with up to 8000% greater penetration and improved physical and chemical stability compared to formulations without these enhancers, leading to enhanced therapeutic efficacy and extended shelf life.
Implementation Method 1
Molecular penetration enhancers or MPETMs can enhance the application to and/or diffusion of molecules across the skin by, for example, disrupting the lipid bilayers of the stratum corneum.
Implementation Method 2
Molecular penetration enhancers or MPETMs can enhance the application to and/or diffusion of molecules across the skin
Implementation Method 3
The first and second compound can improve the flux and/or stability of the topical formulation when compared to a comparative formulation devoid of the first compound and the second compound
Data Source
AI summary
The present disclosure is drawn to topical formulations and related methods. In one embodiment, a topical formulation is provided that includes at least one corticosteroid, a first compound, and a second compound. The first compound and second compound are different and each is selected from the group consisting of N-lauroyl sarcosine, sodium octyl sulfate, methyl laurate, isopropyl myristate, oleic acid, glyceryl oleate, and sodium lauryl sulfoacetate.