Stable Vitamin C Peeling Formulations via Urea Complexation
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Solution Overview
Problem
There is a need for non-oily, non-greasy topical formulations that maintain high concentrations of Vitamin C and urea without degradation, addressing the challenges of instability and biological activity loss in existing formulations.
Innovation Solution
Topical formulations combining L-ascorbic acid with a urea agent and a chemical exfoliant dissolved in a non-aqueous skin-compatible solvent, providing stable liquid compositions with high concentrations of Vitamin C (10-28%) for treating dermatocosmetic conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If high concentrations of Vitamin C (10-28%) are used in topical formulations, then the efficacy for treating dermatocosmetic conditions is improved, but the stability of the formulation deteriorates due to oxidation and degradation of L-ascorbic acid
Solution Approach 1:
The patent introduces a urea agent as an intermediary substance that mediates between the high concentration of L-ascorbic acid and the formulation stability requirements. The urea agent forms a stable complex with ascorbic acid, preventing oxidation and degradation while maintaining high concentrations (10-28%) of Vitamin C in the topical formulation.
Solution Approach 2:
The patent changes the chemical state and physical parameters of L-ascorbic acid by combining it with a urea agent in a non-aqueous solvent system. This parameter change transforms the unstable free ascorbic acid into a stable complex, allowing high concentrations to be maintained without degradation while preserving biological activity.
2Object-affected harmful factors
If aqueous formulations are used to maintain skin compatibility, then skin compatibility is improved, but the stability of Vitamin C deteriorates due to oxidation and phase separation
Solution Approach 1:
The urea agent acts as a stabilizing intermediary that prevents phase separation and oxidation in the formulation. It maintains the integrity of the Vitamin C molecules while allowing the formulation to remain compatible with skin, effectively mediating between stability requirements and skin compatibility.
Solution Approach 2:
The patent creates a composite formulation system combining L-ascorbic acid, urea agent, and non-aqueous solvent. This composite material approach stabilizes the Vitamin C through the urea-ascorbic acid complex while maintaining overall formulation stability and skin compatibility, avoiding the problems of pure aqueous systems.
3Reliability
If urea is added to enhance penetration and treat skin conditions, then the therapeutic efficacy is improved, but the formulation stability deteriorates due to hydrolysis and pH increase
Solution Approach 1:
The patent changes the formulation parameters by using a non-aqueous solvent system instead of water-based formulations. This parameter change prevents hydrolysis of urea and avoids pH increase, maintaining both the therapeutic efficacy of urea (for penetration and skin condition treatment) and formulation stability over time.
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 formulations are storage-stable, maintaining Vitamin C and urea stability, and effective in treating various cosmetic and dermatological conditions, including skin aging, with enhanced skin compatibility and reduced side effects.
Implementation Method 1
Ascorbic acid is a potent antioxidant and is widely used in topical compositions to treat or prevent a range of cosmetic and/or dermatological conditions... The antioxidant activity of ascorbic acid is reported to mediate, and thereby reduce (inhibit) the rate of melanogenesis.
Implementation Method 2
Topical formulations including a combination of L-ascorbic acid, a urea agent and a chemical exfoliant dissolved in a non-aqueous skin-compatible solvent are provided... The formulations are storage stable for an extended period of time without significant degradation of the L-ascorbic acid or urea in the composition.
Implementation Method 3
In topical compositions, the use of urea (and substituted ureas) is known, including for moisture retention (as a humectant), for keratolytic activity, as well as for penetration enhancement, both for itself and other active ingredients.
Data Source
AI summary
Topical formulations including a combination of L-ascorbic acid, a urea agent and a chemical exfoliant dissolved in a non-aqueous skin-compatible solvent are provided. The topical formulations including a chemical exfoliant can be used as a chemical peeling solution. The formulations are storage stable for an extended period of time without significant degradation of the L-ascorbic acid or urea in the composition, are have several desirable physical properties when topically applied to skin. 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 chronological and/or environmentally-caused skin aging. In some embodiments, the topical composition finds use as a chemical peeling solution, e.g., to facilitate shedding of the top layers of skin cells after topical administration.