Oil-in-Water Retinoid Emulsion Without Emulsifiers
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Solution Overview
Problem
Retinoids used in topical applications often cause skin irritation due to the presence of emulsifiers and have chemical stability issues in solvents, necessitating a stable and well-tolerated pharmaceutical composition for effective dermatological use.
Innovation Solution
A pharmaceutical composition comprising a retinoid with a specific formula, formulated as an oil-in-water emulsion without emulsifiers, using a polyacrylamide gelling agent to enhance skin penetration and stability, and including specific solvents and co-solvents to maintain chemical integrity and reduce irritation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If emulsifiers are used in topical retinoid preparations, then the emulsion stability and skin penetration are improved, but cutaneous irritation increases
Solution Approach 1:
The patent removes emulsifiers from the formulation entirely, using a simple oil-in-water mixture where the oil phase contains the retinoid and water phase is separate. This extraction of the harmful emulsifier component eliminates cutaneous irritation while maintaining basic emulsion functionality through the natural properties of the oil and water phases.
2Quantity of substance
If conventional solvents are used for retinoids, then the solubility and delivery are improved, but chemical stability deteriorates
Solution Approach 1:
The patent changes the chemical parameters of the solvent system by selecting specific oils with appropriate polarity and chemical properties. The oil phase is chosen to provide both solubility for the retinoid compound and chemical stability, avoiding solvents that would cause degradation while maintaining adequate dissolution of the active ingredient.
3Stability of the object's composition
If emulsifiers are included in the formulation, then the homogeneity and delivery efficiency are improved, but the number of ingredients and complexity increase
Solution Approach 1:
The patent extracts and removes emulsifiers from the ingredient list, resulting in a simplified two-phase formulation consisting only of oil phase (containing retinoid) and water phase. This reduction in ingredient count eliminates the need for additional emulsifying agents while maintaining adequate mixture homogeneity through simple mechanical mixing.
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 composition achieves high skin penetration and stability, reducing irritation and maintaining the retinoid's chemical integrity, thereby providing effective dermatological treatment with minimal side effects.
Implementation Method 1
at least one gelling agent of the aqueous phase
Implementation Method 2
at least one principal solvent of the compound (I) and at least one co-solvent oil of the compound (I)
Data Source
AI summary
A composition in the form of an oil in water emulsion, preferably without emulsifier, is described. The composition can include, in a physiologically acceptable environment, at least one new retinoid. Also described, is the method of preparing the composition and its use in cosmetics and dermatology.