Azelaic Acid Solubilization in Urea-Based Non-Aqueous Topical Formulations
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Solution Overview
Problem
Azelaic acid, used for treating dermatocosmetic conditions, faces challenges due to its difficulty in solubilization, leading to irritation and inefficiency in topical formulations, as it is often applied in undissolved states, requiring high concentrations that can cause skin irritation and has limited solubility in common solvents.
Innovation Solution
Topical formulations of azelaic acid dissolved in a combination of a urea agent and a non-aqueous skin-compatible solvent, allowing for high concentrations of azelaic acid (1-20% by weight) to be solubilized, reducing skin irritation and improving absorption and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If azelaic acid is applied in undissolved state (dispersion), then high concentration can be delivered, but skin irritation increases and absorption is reduced
Solution Approach 1:
The patent introduces a urea-based solvent system as an intermediary medium to dissolve azelaic acid. The urea acts as a mediating substance that enables complete solubilization of azelaic acid at high concentrations while preventing the skin irritation and burning sensations associated with undissolved formulations. This intermediary solvent system allows the active ingredient to be delivered in a non-irritating, fully dissolved state.
2Stability of the object's composition
If azelaic acid is solubilized in water, then complete dissolution is achieved, but the solution becomes unstable and ineffective
Solution Approach 1:
The patent fundamentally changes the solvent parameter from water to a non-aqueous urea-based system. This parameter change enables azelaic acid to be completely solubilized at high concentrations while maintaining formulation stability. The non-aqueous environment prevents the instability and degradation that occur in water-based solutions, creating a reliable and effective topical composition.
3Stability of the object's composition
If azelaic acid is solubilized in cosmetic oils, then some dissolution is achieved, but the formulation becomes greasy and less effective
Solution Approach 1:
The patent employs a urea-based solvent as an intermediary that provides optimal solubilization characteristics. This intermediary system achieves complete dissolution of azelaic acid while maintaining a non-greasy, skin-compatible formulation. The urea solvent system avoids the drawbacks of cosmetic oils (greasiness and reduced efficacy) while providing better dissolution than water-based systems.
4Productivity
If high concentration of azelaic acid is used to compensate for poor absorption, then effectiveness is achieved, but skin irritation and burning increase
Solution Approach 1:
The urea-based solvent system acts as a mediating carrier that enables high concentrations of azelaic acid to be delivered in a fully dissolved, non-irritating state. This intermediary system allows the formulation to achieve high productivity (treatment effectiveness) without the harmful skin burning and stinging that would otherwise occur at such concentrations with undissolved formulations.
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 solubilized azelaic acid formulations are less irritating, more effective at lower concentrations, and maintain stability, effectively treating various dermatocosmetic conditions without causing skin irritation, improving skin compatibility and reducing the appearance of skin discolorations.
Implementation Method 1
Topical formulations of azelaic acid dissolved in a combination of a urea agent and a non-aqueous skin-compatible solvent are provided. The topical formulations can include high concentrations of the azelaic acid of 1% to 20% by weight.
Implementation Method 2
When applied to the skin, undissolved azelaic acid is not readily absorbed and as a result an excess of azelaic acid must be present to be effective. The higher the concentration of azelaic acid, the more likely irritation (burning, stinging and redness) to the skin will occur.
Data Source
AI summary
Topical formulations of azelaic acid dissolved in a combination of a urea agent and a non-aqueous skin-compatible solvent are provided. The formulations are completely solubilized in the composition and have desirable physical properties, such as non-grittiness. The topical formulations can include high concentrations of azelaic acid. Topical compositions of this disclosure find use in treating or preventing a variety of cosmetic and/or dermatological conditions as well as to reduce the appearance of skin discolorations.