Retinoic Acid-Alcohol Amine Complex for Topical Skin Penetration
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Solution Overview
Problem
Retinoic acid has poor solubility in water and low skin penetration due to its fat-solubility and insolubility in conventional drug forms, leading to limited medicinal use and skin irritation at higher dosages.
Innovation Solution
A retinoic acid-alcohol amine complex is formed with alcohol amine compounds like diethanolamine, allowing for a liquid form at room temperature with improved water solubility and skin penetration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If retinoic acid is used in conventional drug forms, then it can be applied topically, but it has poor water solubility and low skin penetration
Solution Approach 1:
The patent applies composite materials by forming a complex between retinoic acid and alcohol amine compounds. This complex combines the properties of both components, creating a new material with improved water solubility while maintaining the active ingredients' efficacy. The complex is formed through chemical interaction between the carboxyl group of retinoic acid and the amino group of alcohol amine, resulting in a composite structure that overcomes the solubility limitation of pure retinoic acid.
Solution Approach 2:
The patent applies parameter changes by modifying the chemical state of retinoic acid through complex formation. By changing the molecular structure and chemical properties through interaction with alcohol amine compounds, the solubility parameter is improved. The complex formation alters the physical and chemical parameters of retinoic acid, enabling better water solubility and skin penetration without losing the active ingredient's therapeutic effects.
2Reliability
If the dosage of retinoic acid is increased to overcome skin barrier, then penetration improves, but skin irritation increases
Solution Approach 1:
The patent applies the intermediary principle by using alcohol amine compounds as mediators between retinoic acid and the skin. The alcohol amine complex acts as a carrier that facilitates the delivery of retinoic acid through the skin barrier. This intermediary structure allows retinoic acid to penetrate the skin at lower concentrations, reducing direct irritation while maintaining therapeutic effectiveness. The complex serves as a bridge that enables controlled delivery and reduces harsh effects.
3Adaptability or versatility
If retinoic acid is formulated for topical use, then it can treat skin diseases, but the stratum corneum barrier limits ingredient penetration
Solution Approach 1:
The patent applies parameter changes by modifying the physical and chemical properties of retinoic acid through complex formation with alcohol amine compounds. This changes the molecular characteristics, size, and solubility parameters, enabling the formulation to penetrate the stratum corneum barrier more effectively. The parameter modification allows the active ingredient to maintain stability while achieving better penetration and effective concentration at the skin site.
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 complex achieves good water solubility and skin penetration, overcoming solubility limitations and reducing skin irritation, suitable for drug products including pharmaceuticals and cosmetics.
Implementation Method 1
reacting the retinoic acid with the alcohol amine compound to obtain the complex
Data Source
AI summary
A retinoic acid-alcohol amine complex has retinoic acid and an alcohol amine compound. The complex is in liquid form at room temperature, has good water solubility/water dilution resistance and good skin penetration effect.