Topical Formulation with Polyol-in-Silicone Emulsion for Skin Penetration
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current topical dermatological formulations face challenges with poor skin penetration and adverse skin feel, leading to low patient adherence due to their inability to maintain high saturation of active compounds and diffusion coefficient enhancers while incorporating emollients, resulting in reduced therapeutic efficacy.
Innovation Solution
The formulation combines diol partition coefficient enhancers, dimethicone macromers, and diffusion coefficient enhancers like C12-C14 acids and alcohols with hydrocarbyl methyl siloxane emollients, creating a polyol-in-silicone emulsion that enhances skin penetration and stability, improving skin feel and adherence.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If emollients are incorporated into topical formulations to improve skin feel, then patient adherence is improved, but the saturation of diffusion coefficient enhancers is reduced, worsening skin penetration
Solution Approach 1:
The patent changes the chemical parameters of the formulation by selecting specific C12-C14 fatty acids and C14 alcohols as diffusion coefficient enhancers, and using polyol-in-silicone emulsion systems with controlled water content (5-50%), thereby maintaining both emollient benefits and enhanced skin penetration without compromising saturation levels
Solution Approach 2:
The patent employs composite material systems by combining dimethicone macromers with hydrocarbyl methyl siloxane emollients to create polyol-in-silicone emulsions, which integrate the skin-feel benefits of emollients with the penetration-enhancing properties of the composite structure, resolving the contradiction between comfort and efficacy
2Reliability
If high saturation of active compounds is maintained to improve therapeutic efficacy, then treatment effectiveness is improved, but the formulation complexity increases, making it difficult to incorporate emollients
Solution Approach 1:
The patent applies multi-functionality by designing a formulation system where the polyol-in-silicone emulsion matrix simultaneously serves as a vehicle for high saturation of active compounds, a source of emollient benefits, and a stable delivery system, thereby achieving therapeutic efficacy without proportionally increasing formulation complexity
3Reliability
If diffusion coefficient enhancers are used at high saturation to improve skin penetration, then active delivery is improved, but the skin feel becomes poor and greasy, reducing patient adherence
Solution Approach 1:
The patent applies local quality by using C12-C14 fatty acids and C14 alcohols specifically targeted for their optimal balance between penetration enhancement and skin feel, and by localizing the diffusion coefficient enhancers within the polyol-in-silicone emulsion structure, thereby achieving high active delivery without the greasy feel that would reduce adherence
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
This approach results in efficient and predictable delivery of active compounds, reducing adverse reactions and the need for higher doses, while enhancing therapeutic outcomes and patient adherence by providing a smooth, non-greasy skin feel.
Implementation Method 1
a partition coefficient enhancer, having a structure of the general formula: CnH2n+2O2 where n represents an integer from 3 to 6 inclusive
Implementation Method 2
a diffusion coefficient enhancer (DC enhancer) selected from the group consisting of a C12 to C14 straight chain fatty acid and a C14 straight chain primary alcohol
Data Source
Figure 1~2
Figure 3~4
Figure 5~6
AI summary
A formulation for topical dermatological delivery of a medicinal or cosmeceutical or cosmetic active including a functional co-enhancer delivery system. The delivery system generally comprises a water-miscible solvent and C12 or C14 fatty acids or C14 alcohol in combination with a hydrocarbyl methyl siloxane emollient.