Silicone Vehicle Formulation for Polyunsaturated Ketone Permeation
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Solution Overview
Problem
Polyunsaturated long-chain ketones are hydrophobic and insoluble in water, limiting their bioavailability and stability, making it difficult to administer effective doses topically for conditions like psoriasis and dermatitis.
Innovation Solution
A pharmaceutical composition combining polyunsaturated long-chain ketones with a silicone vehicle, specifically a blend of cyclic, liquid linear, and elastomeric silicones, forming an oil-in-oil emulsion that enhances skin permeation and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polyunsaturated long-chain ketones are used as active ingredients, then therapeutic effect is achieved, but water solubility is poor limiting bioavailability
Solution Approach 1:
The patent uses amphiphilic surfactants as intermediary substances to bridge the hydrophobic polyunsaturated long-chain ketones and the aqueous environment. The surfactants have both hydrophilic and hydrophobic portions, allowing them to solubilize the ketones in water through micelle formation, thereby improving bioavailability without compromising therapeutic effect
Solution Approach 2:
The invention creates a composite pharmaceutical formulation by combining polyunsaturated long-chain ketones with amphiphilic surfactants and other excipients. This composite system allows the hydrophobic active ingredient to be delivered in an aqueous-based formulation, resolving the solubility contradiction while maintaining therapeutic efficacy
2Ease of operation
If polyunsaturated long-chain ketones are formulated for topical administration, then skin permeation is improved, but storage stability deteriorates due to degradation susceptibility
Solution Approach 1:
The patent incorporates antioxidants and stabilizing agents into the formulation before storage to prevent degradation of the polyunsaturated long-chain ketones. These protective ingredients are added in advance to cushion against oxidative damage and other degradation mechanisms that would otherwise occur during storage, especially given the multiple double bonds in the ketone structure
Solution Approach 2:
The formulation uses an oxygen-scavenging system and potentially inert packaging to create a protected environment that minimizes exposure to oxygen and light. This inert environment prevents oxidative degradation of the polyunsaturated ketones during storage while maintaining their permeation-enhancing properties for topical application
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 silicone-based formulation increases the permeation of active ingredients into the skin by 2 to 4 times compared to paraffin-based formulations, while maintaining excellent storage stability, ensuring a higher concentration of the active ingredient is absorbed effectively.
Implementation Method 1
the present inventors have found that the pharmaceutical compositions described herein typically form an oil-in-oil emulsion with the silicone-based vehicle which enhances use according to the invention
Implementation Method 2
the present inventors sought to increase the permeation of the active polyunsaturated ketones into the skin whilst ensuring storage stability
Data Source
AI summary
A pharmaceutical composition comprising polyunsaturated long-chain ketones and a silicone vehicle or a blend of silicone vehicles. The composition has utility in the treatment and prevention of inflammatory conditions including skin disorders.