5-ALA Cosmetic Composition Liposomal Stability

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Solution Overview

Problem

Current cosmetic treatments using 5-aminolevulinic acid (5-ALA) derivatives often result in undesirable side effects such as pain, itching, burning, erythema, and edema, while also being unstable and requiring cold storage due to high water content, which limits their shelf life and user convenience.

Innovation Solution

A composition comprising 2% or less of 5-ALA derivative or skin-compatible salts, combined with 70% or more water and 2-25% lipid carrier, along with emulsifiers, which is stable at room temperature and minimizes side effects, enhancing skin appearance by reducing wrinkles, fine lines, and improving firmness and elasticity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If compositions with high water content are used to improve skin hydration and cosmetic效果, then skin appearance is improved, but stability deteriorates and cold storage is required

Engineering Contradiction:
Improveskin appearance qualityVSAvoidcomposition stability
Core Design Contradiction:
Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The patent changes the concentration parameter of 5-ALA derivative to 2% or less, which is lower than conventional photodynamic therapy compositions. This parameter change reduces the instability and side effects while maintaining cosmetic efficacy when combined with liposomal delivery and controlled light exposure

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces liposomes as an intermediary delivery system for 5-ALA derivative. The liposomal encapsulation protects the active ingredient, enables controlled release, and improves stability without requiring cold storage, while still achieving skin penetration and cosmetic effects

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If conventional 5-ALA compositions are used for cosmetic treatment, then skin rejuvenation is achieved, but side effects such as pain, itching, burning, erythema and edema occur

Engineering Contradiction:
Improveskin rejuvenation effectVSAvoidside effects
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent reduces the concentration of 5-ALA derivative to 2% or less, which is significantly lower than the 10-20% concentrations used in conventional photodynamic therapy. This parameter reduction minimizes painful side effects while maintaining cosmetic benefits through liposomal delivery and controlled illumination

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

Liposomes serve as a mediator that delivers 5-ALA derivative to target skin cells in a controlled manner, reducing direct irritation and side effects while maintaining therapeutic and cosmetic efficacy

Inventive Principle:
Principle #24Intermediary (Mediator)

3Object-affected harmful factors

If high concentration of 5-ALA is used to achieve cosmetic effects, then skin improvement is enhanced, but stability and shelf life deteriorate

Engineering Contradiction:
Improvecosmetic effect intensityVSAvoidshelf life
Core Design Contradiction:
Object-affected harmful factorsVSDuration of action of stationary object

Solution Approach 1:

Liposomes act as stable carriers that protect 5-ALA derivative from degradation, enabling room temperature storage and extending shelf life while maintaining cosmetic efficacy through controlled release mechanisms

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent uses low concentration (≤2%) of 5-ALA derivative combined with liposomal formulation, which stabilizes the composition for long-term storage at room temperature while maintaining cosmetic effectiveness

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

The composition effectively improves skin appearance with minimal side effects and maintains stability at room temperature, extending shelf life and user convenience, while providing quick absorption and deep skin penetration.

Implementation Method 1

5-ALA is converted into its photoactive metabolite, protoporphyrin IX (PpIX)

Methodology Applied
Scientific EffectPhotochemical conversion: Photopolymerisation

Implementation Method 2

PpIX accumulates in the epidermis and dermis and can be activated by illumination with a light source

Methodology Applied
Scientific EffectLight absorption: Absorption (EM radiation)

Implementation Method 3

topical photodynamic therapy with 5-aminolevulinic acid (5-ALA) or a derivative of 5-ALA

Methodology Applied
Scientific EffectPhotodynamic reaction: Photo-oxidation

Implementation Method 4

it can provide protection against uncontrolled oxidation processes which are photochemically induced and even quench singlet oxygen

Methodology Applied
Scientific EffectSinglet oxygen generation: Photo-oxidation

Data Source

PatentUS8992954B2Compositions comprising a derivative of 5-aminolevulinic acid
Publication Date: 2015.03.31 BELLUS MEDICAL LLC
  • US8992954B2 patent drawing

AI summary

The present invention relates to compositions comprising a derivative of 5-aminolevulinic acid (5-ALA), e.g. an ester of 5-ALA or a skin compatible salt thereof. Further, the invention relates to use of such compositions in methods of cosmetic treatment, particularly in methods of improving or otherwise enhancing the appearance of the skin.