Hydrotrope Solubilization of Phenolic Compounds in Aqueous Cosmetics

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Solution Overview

Problem

The limited water solubility of phenolic compounds and adenosine/adenosine analogues restricts their effectiveness in cosmetic applications, as it hampers their ability to penetrate the skin and combat aging and skin damage effectively, necessitating improved solubility and transdermal delivery methods.

Innovation Solution

The use of hydrotropes such as nicotinamide, caffeine, sodium PCA, and sodium salicylate in aqueous cosmetic compositions to enhance the water solubility of phenolic compounds and adenosine/adenosine analogues, allowing for increased bioavailability and transdermal penetration by forming stable solutions that maintain stability even upon dilution.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If phenolic compounds and adenosine are used in cosmetic compositions, then their antioxidant and anti-aging effects are improved, but their water solubility deteriorates

Engineering Contradiction:
Improveantioxidant effectivenessVSAvoidwater solubility
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent employs hydrotropes as intermediary substances that mediate between the hydrophobic phenolic compounds/adenosine and the aqueous cosmetic formulation. These hydrotropes create a bridging environment that allows the active ingredients to dissolve in water without compromising their structural integrity or biological activity, thereby resolving the solubility contradiction while preserving antioxidant effectiveness.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical-chemical parameters of the formulation by introducing hydrotropes that change the solvation environment. This parameter change enables the hydrophobic active ingredients to achieve adequate water solubility through altered molecular interactions, without requiring chemical modification of the active compounds themselves.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If chemical modification of polyphenols is performed to improve solubility, then water solubility is improved, but the activity of phenol/polyphenols deteriorates

Engineering Contradiction:
Improvewater solubilityVSAvoidbiological activity
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

Instead of chemically modifying the polyphenols, the patent uses hydrotropes as intermediary agents that facilitate solubility through physical interactions. This approach preserves the intact molecular structure and biological activity of the polyphenols while achieving the desired solubility enhancement, avoiding the trade-off between modification and activity retention.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Quantity of substance

If strong organic solvents are used to increase solubility, then water solubility of phenol/polyphenols is improved, but safety and compatibility with cosmetic formulations deteriorate

Engineering Contradiction:
Improvewater solubilityVSAvoidsafety and compatibility
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent replaces potentially harmful strong organic solvents with safer, cosmetically acceptable hydrotropes that achieve solubility enhancement through milder mechanisms. These alternative substances provide the necessary solubility improvement without introducing safety concerns or compatibility issues, effectively substituting harmful agents with benign alternatives.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

4Quantity of substance

If delivery systems such as gel carriers or nano crystals are used, then water solubility is improved, but device complexity and manufacturing costs increase

Engineering Contradiction:
Improvewater solubilityVSAvoidformulation complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent extracts the solubility-enhancing function from complex delivery systems like gel carriers and nano crystals, achieving the same solubility improvement through simpler hydrotrope additives. This extraction of the essential function eliminates the need for complicated formulation structures while maintaining effective solubility enhancement.

Inventive Principle:
Principle #2Taking out (Extraction)

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 incorporation of hydrotropes significantly increases the solubility and bioavailability of phenolic compounds and adenosine/adenosine analogues, enabling them to effectively combat skin aging and damage by enhancing their penetration through the skin, while maintaining solution stability without the drawbacks of organic solvents.

Implementation Method 1

The use of hydrotropes such as nicotinamide, caffeine, sodium PCA, and sodium salicylate in aqueous cosmetic compositions to enhance the water solubility of phenolic compounds and adenosine/adenosine analogues, allowing for increased bioavailability and transdermal penetration by forming stable solutions

Methodology Applied
Scientific EffectSolvation: Solvation

Data Source

PatentEP2906547B2Cosmetic compositions containing at least one hydrotrope and at least one active compound
Publication Date: 2022.10.26 LOREAL SA
  • EP2906547B2 patent drawingFigure 1~2
  • EP2906547B2 patent drawingFigure 3~4A
  • EP2906547B2 patent drawingFigure 4B

AI summary

Aqueous compositions comprising at least one hydrotrope and at least one active compound. The at least one hydrotrope is present in an amount: (a) effective to solubilize said at least one active compound in water; and/or (b) effective to increase transdermal penetration of said at least one active compound; and/or (c) effective to increase the bioavailability of said at least one active compound. The aqueous compositions are provided for cosmetic and other uses. Also provided are methods for preparing and using said compositions.