Azelaic Acid Deep Eutectic Composition for Solubility and Stability

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Solution Overview

Problem

Azelaic acid exhibits poor solubility in water and oil, high melting point, and is prone to precipitation, making it difficult to formulate stable and effective large-area cosmetic and drug products.

Innovation Solution

A self-recognition DES system is formed by mixing azelaic acid with betaine and panthenol, enhancing solubility and stability through supramolecular interactions, allowing for a liquid state and direct dilution without phase separation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If azelaic acid is added in high amounts to improve efficacy, then treatment effectiveness increases, but precipitation occurs resulting in system roughness and instability

Engineering Contradiction:
Improveazelaic acid addition amountVSAvoidsystem stability
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent uses betaine as an intermediary substance that forms a supramolecular complex with azelaic acid through hydrogen bonding. This mediator prevents azelaic acid precipitation by creating a stable soluble complex, allowing high concentrations of azelaic acid to be maintained in the cosmetic formulation without causing system roughness or instability.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates a composite supramolecular system consisting of azelaic acid and betaine molecules self-assembled through hydrogen bonds. This composite material exhibits enhanced solubility and stability compared to pure azelaic acid, enabling high concentrations to be incorporated into water-based cosmetic formulations while maintaining system homogeneity and preventing precipitation.

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If encapsulation treatment is used to enhance solubility, then water solubility improves, but the inclusion system becomes sticky and causes poor skin feeling

Engineering Contradiction:
Improvewater solubilityVSAvoidskin feeling
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes the molecular state of azelaic acid from crystalline solid to soluble supramolecular complex by altering the chemical environment through betaine addition. This parameter change in molecular organization and solvation state enhances water solubility while maintaining a non-sticky, cosmetically acceptable formulation that provides good skin feeling.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If solubilization with stabilizers is used to form colloids, then solubility improves, but penetration of azelaic acid into skin is hindered

Engineering Contradiction:
ImprovesolubilityVSAvoidskin penetration
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent creates a supramolecular complex that replicates the molecular structure and properties of pure azelaic acid while improving solubility. The betaine-azelaic acid complex maintains the pharmacologically active structure of azelaic acid, enabling it to penetrate skin effectively while being soluble in water-based formulations, unlike bulky colloid stabilizers that would block penetration.

Inventive Principle:
Principle #26Copying

4Quantity of substance

If ultrafine grinding is used to improve solubility, then particle size decreases, but additional cost increases and significant solubilization is not achieved

Engineering Contradiction:
ImprovesolubilityVSAvoidmanufacturing cost
Core Design Contradiction:
Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent changes the chemical environment and molecular interactions by introducing betaine, which forms hydrogen-bonded supramolecular complexes with azelaic acid. This chemical parameter change dramatically enhances solubility without requiring mechanical size reduction, avoiding the high costs of ultrafine grinding equipment and processing while achieving superior solubilization效果.

Inventive Principle:
Principle #35Parameter changes

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 azelaic acid/betaine/panthenol DES system achieves high solubility and stability, enabling broad application in cosmetics and drugs with improved moisturizing performance and ease of formulation.

Implementation Method 1

azelaic acid self-recognition

Methodology Applied
Scientific EffectSelf-recognition: Self-Assembly

Implementation Method 2

supramolecular hydrogen bonds between molecules

Methodology Applied
Scientific EffectHydrogen bonding: Chemical Bonding

Data Source

PatentEP4714425A1Azelaic acid/betaine/panthenol self-recognition des system and preparation method
Publication Date: 2026.03.25 WUXI ZHIYAN BIOTECHNOLOGY CO LTD
  • EP4714425A1 patent drawingFigure 1~2
  • EP4714425A1 patent drawingFigure 3~4
  • EP4714425A1 patent drawingFigure 5~7

AI summary

Disclosed in the present invention are an azelaic acid/betaine/panthenol self-recognition DES system and a preparation method, belonging to the technical field of supermolecules. The preparation method for the azelaic acid/betaine/panthenol self-recognition DES system of the present invention comprises the following steps: mixing azelaic acid, betaine, and panthenol according to a molar ratio of 1:0.4-6:0.7-10, and stirring and heating to obtain an azelaic acid/betaine/panthenol self-recognition DES system. The azelaic acid/betaine/panthenol self-recognition DES system prepared according to the present invention is readily soluble in water, and can be directly diluted by adding water until the mass concentration of azelaic acid is 0.8%-35%, without phase separation and solid precipitation, thereby effectively improving the water solubility and stability of azelaic acid, with the degree of improvement far exceeding that of the prior art.