Phosphatidylcholine Self-Emulsifying Solubilization for Cosmetic Agents

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Solution Overview

Problem

Current methods for solubilizing poorly water-soluble cosmetic agents in cosmetic preparations are limited by the use of costly emulsifiers and solubilizers like polysorbates, which can have adverse health effects and impair skin penetration, and existing solubilization techniques such as micelles and liposomes have drawbacks including short shelf life and high production costs.

Innovation Solution

A method involving the combination of phosphatidylcholine, medium-chained triglycerides, lysophosphatidylcholine, C2-C4 alcohols, and glyceryl stearate or saturated/unsaturated fatty acids to solubilize cosmetic agents without the need for polysorbates, achieved by carefully heating the mixture to form a clear solution that is stable and self-emulsifying.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If emulsifiers are used to combine compounds with different polarity in a stable formulation, then the stability of the formulation is improved, but the cost increases and irritation potential increases

Engineering Contradiction:
Improveformulation stabilityVSAvoidproduction cost
Core Design Contradiction:
Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The patent changes the physical-chemical parameters of the system by using self-emulsifying compounds that form micellar structures. Instead of adding separate emulsifiers, the active cosmetic agents themselves are modified or selected to possess surfactant properties, allowing them to spontaneously form stable emulsions at the oil-water interface without additional emulsifying agents.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent makes the cosmetic agents multi-functional by selecting or modifying them to simultaneously serve as both the active cosmetic component and the emulsifying agent. These compounds perform multiple functions: providing the desired cosmetic effect, reducing surface tension, and stabilizing the emulsion, thereby eliminating the need for separate emulsifiers.

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Stability of the object's composition

If emulsifiers are used to combine compounds with different polarity in a stable formulation, then the stability of the formulation is improved, but the sensory characteristics are impaired

Engineering Contradiction:
Improveformulation stabilityVSAvoidsensory characteristics
Core Design Contradiction:
Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent changes the molecular structure and properties of the cosmetic agents to possess self-emulsifying capabilities. By selecting compounds with appropriate hydrophilic-lipophilic balance (HLB) values and surfactant properties, the formulation achieves stability without the need for traditional emulsifiers that may leave unpleasant residues or alter the sensory feel on skin.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If solubilizers are used to improve the solubility of poorly water-soluble cosmetic agents, then the solubility is improved, but the skin penetration is impaired

Engineering Contradiction:
ImprovesolubilityVSAvoidskin penetration
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses self-emulsifying cosmetic agents as intermediaries that form micellar structures. These micelles act as carriers that can solubilize poorly water-soluble cosmetic agents within their hydrophobic cores while maintaining the ability to interact with skin lipids. The micellar structure facilitates both solubility enhancement and skin penetration by mimicking the lipid bilayer structure of the skin barrier.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Quantity of substance

If micelles or liposomes are used for solubilization, then the solubility of cosmetic agents is improved, but the shelf life is reduced and production costs increase

Engineering Contradiction:
ImprovesolubilityVSAvoidshelf life
Core Design Contradiction:
Quantity of substanceVSDuration of action of stationary object

Solution Approach 1:

The patent simplifies the micellar structure by using single-layer micelles formed by self-emulsifying compounds rather than complex liposomal structures. This reduces the structural complexity and potential instability points, leading to improved shelf life. The self-emulsifying compounds form stable micelles that maintain their solubilizing capacity over extended periods without the degradation issues associated with liposomal formulations.

Inventive Principle:
Principle #35Parameter changes

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

This method effectively solubilizes poorly water-soluble cosmetic agents, improving skin penetration and homogeneity of cosmetic products without the use of costly solubilizers, resulting in a stable and long-lasting cosmetic preparation with enhanced bioavailability.

Implementation Method 1

a self-emulsifying behaviour of the mixture of phosphatidylcholine, medium-chained triglycerides, lysophosphatidylcholine, C2-C4 alcohols and glyceryl stearate or saturated or unsaturated fatty acids

Methodology Applied
Scientific EffectSelf-emulsification: Emulsion

Implementation Method 2

method for solubilizing poorly water-soluble cosmetic agents

Methodology Applied
Scientific EffectSolubilization: Solvation

Implementation Method 3

carefully heating the mixture to form a clear solution

Methodology Applied
Scientific EffectHeating: Heating

Implementation Method 4

heating the mixture to form a clear solution

Methodology Applied
Scientific EffectPhase change: Phase Change

Data Source

PatentUS11207256B2Method for solubilizing poorly water-soluble cosmetic agents
Publication Date: 2021.12.28 ATHENION AG

AI summary

The present invention relates to a method for solubilizing poorly water-soluble organic cosmetic agents, to the solubilisate and cosmetic preparations produced by this method and respective uses of the solubilisate in cosmetic preparations. A phosphatidylcholine-based solubilization method is disclosed.