Vitamin C Topical Formulations with Anhydrous Urea Stabilization
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Solution Overview
Problem
Existing topical Vitamin C formulations are unstable and degrade quickly, especially when urea is included, leading to unpleasant odors and decreased biological activity, and there is a need for non-oily, non-greasy formulations with high Vitamin C and urea concentrations.
Innovation Solution
Topical formulations of L-ascorbic acid dissolved in a combination of a urea agent and a non-aqueous skin-compatible solvent, optionally with cinnamic acid, to stabilize Vitamin C and enhance its penetration and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If water-containing formulations are used for Vitamin C, then skin compatibility and moisturizing properties are improved, but stability deteriorates causing rapid degradation
Solution Approach 1:
The patent changes the fundamental parameter of the carrier system from aqueous to non-aqueous (anhydrous) formulations. This parameter change fundamentally alters the stability landscape, preventing water-related degradation pathways while maintaining skin compatibility through carefully selected non-aqueous carriers and co-solvents.
Solution Approach 2:
The patent employs composite formulation strategies combining multiple non-aqueous carriers (such as silicone oils, ester oils, and anhydrous bases) with Vitamin C and stabilizing agents. This composite approach creates a synergistic system that enhances both stability and skin compatibility simultaneously.
2Quantity of substance
If higher concentrations of Vitamin C are used, then efficacy for anti-aging and skin lightening is improved, but stability deteriorates leading to rapid degradation
Solution Approach 1:
The patent changes the formulation parameter from aqueous to non-aqueous base, which fundamentally alters the stability-concentration relationship. This enables higher Vitamin C concentrations (e.g., 10-50%) to be maintained without the rapid degradation that occurs in water-based systems at equivalent concentrations.
Solution Approach 2:
The patent introduces non-aqueous carriers and co-solvents as intermediary substances that mediate between the high Vitamin C concentration and skin compatibility requirements. These intermediaries create a stable environment that allows high concentrations to be maintained while preventing degradation pathways.
3Ease of operation
If urea is included in aqueous formulations for penetration enhancement, then skin penetration is improved, but stability deteriorates causing hydrolysis, odor, and pH increase
Solution Approach 1:
The patent changes the fundamental parameter of the formulation base from aqueous to non-aqueous. This parameter change eliminates the hydrolysis reaction pathway that occurs in aqueous systems, thereby preventing urea degradation, odor formation, and pH increase while maintaining penetration enhancement capabilities.
Solution Approach 2:
The patent converts the potential harm of urea hydrolysis into a benefit by using non-aqueous carriers. In this environment, urea remains stable without hydrolyzing, thereby eliminating the harmful effects (odor, pH change, degradation) while preserving the beneficial penetration enhancement property.
4Stability of the object's composition
If non-aqueous carriers are used for Vitamin C, then stability is improved, but skin compatibility and moisturizing properties deteriorate
Solution Approach 1:
The patent employs composite formulation strategies combining multiple non-aqueous carriers (silicone oils, ester oils, anhydrous bases) with Vitamin C and skin-compatible co-solvents. This composite approach creates a synergistic system that maintains stability while improving skin compatibility through the combined properties of multiple ingredients.
Solution Approach 2:
The patent applies local quality modifications by selecting specific non-aqueous carriers and co-solvents with particular skin-compatible properties. Different ingredients are chosen with specific functions: some provide stability, others provide skin compatibility, and others enhance penetration, creating a locally optimized formulation.
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 maintain high Vitamin C concentrations without degradation for extended periods, providing effective treatment for cosmetic and dermatological conditions and enhancing wound healing.
Implementation Method 1
Topical formulations of L-ascorbic acid dissolved in a combination of a urea agent and a non-aqueous skin-compatible solvent
Implementation Method 2
The topical formulations can include cinnamic acid or derivatives thereof as a penetration enhancer and stabilizing component of ascorbic acid
Implementation Method 3
Ascorbic acid (also commonly known as Vitamin C) is a potent antioxidant and is widely used in topical compositions to treat or prevent a range of cosmetic and/or dermatological conditions
Implementation Method 4
Vitamin C can help neutralize the damaging effects of free radicals and plays a role in stimulating the growth and bundling of collagen, important in maintaining skin elasticity
Implementation Method 5
Tyrosinase is a copper-containing enzyme that catalyzes the production of melanin and other pigments from tyrosine by oxidation. The antioxidant activity of ascorbic acid is reported to mediate, and thereby reduce (inhibit) the rate of melanogenesis
Data Source
AI summary
Topical formulations of L-ascorbic acid dissolved in a combination of a urea agent and 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 in the composition, are have desirable physical properties. The topical formulations can include high concentrations of the L-ascorbic acid. The topical formulations can include cinnamic acid or derivatives thereof as a penetration enhancer and stabilizing component of ascorbic 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 chronological and/or environmentally-caused skin aging.