Ceramide Formulation Stabilization via Triethyl Citrate

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Solution Overview

Problem

Ceramides in cosmetic formulations face challenges due to low solubility, high recrystallization tendency, and microbial stabilization issues, particularly at temperatures just above freezing, and preservatives often negatively affect physical stability.

Innovation Solution

A composition containing ceramides, sphingoid bases, and triethyl citrate, with a weight ratio of 2:6 to 1:2, which improves storage stability, tolerance to freeze-thaw cycles, sensory properties, and microbial stability, preventing ceramide recrystallization and enhancing absorption and spreadability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If ceramides are incorporated into cosmetic formulations, then skin barrier function is improved, but physical stability deteriorates due to recrystallization and inhomogeneities

Engineering Contradiction:

Improveskin barrier functionVSAvoidphysical stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

Triethyl citrate acts as an intermediary substance that mediates between the ceramide molecules and the formulation matrix. It forms a stable complex with ceramides, preventing direct interaction that would lead to recrystallization, while maintaining the skin barrier benefits of ceramides

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the physical-chemical parameters of the formulation by introducing triethyl citrate, which alters the solubility and crystallization behavior of ceramides. This parameter change prevents recrystallization at temperatures just above freezing while maintaining formulation homogeneity

Inventive Principle:

Principle #35Parameter changes

2Reliability

If preservatives are added to stabilize microbial growth, then microbial stability is improved, but physical stability deteriorates due to negative impact on ceramide stability

Engineering Contradiction:

Improvemicrobial stabilityVSAvoidphysical stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

Triethyl citrate serves as a protective intermediary that shields ceramides from the negative effects of preservatives. It forms a stable complex with ceramides that resists disruption by preservative agents, allowing microbial stabilization without physical degradation

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention converts the harmful effect of preservatives on ceramide physical stability into a beneficial outcome. By using triethyl citrate, the formulation can tolerate preservatives that would otherwise cause recrystallization, turning a harmful interaction into a stable formulation

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

3Reliability

If ceramide concentration is increased to improve skin benefits, then therapeutic effect is improved, but solubility and formulation stability deteriorate

Engineering Contradiction:

Improveskin benefitsVSAvoidsolubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

Triethyl citrate acts as a solubilizing intermediary that facilitates the dissolution of ceramide molecules in the formulation matrix. It forms stable complexes that maintain high ceramide concentrations while preserving solubility and preventing precipitation

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the solubility parameters of ceramides by introducing triethyl citrate, which alters the physical-chemical environment to enable higher ceramide concentrations without loss of solubility or formulation stability

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP3733157B1Composition containing at least one ceramide, at least one sphingoid base and triethyl citrate

Publication Date: 2023.08.30 EVONIK OPERATIONS GMBH

AI summary

The invention relates to a composition containing at least one ceramide, at least one sphingoid base and triethyl citrate, a method for producing a formulation containing at least one ceramide and the use of triethyl citrate for stabilizing a ceramide-containing formulation.