Cyclic Peptides for Topical Skin Care via Integrin Modulation

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Solution Overview

Problem

Cosmetic peptides face challenges such as conformational flexibility, easy digestion by proteases, poor membrane transport, and solubility issues, leading to reduced efficacy and potential immunogenic reactions.

Innovation Solution

Development of cyclic peptides with enhanced stability and integrin modulating activity, specifically designed to inhibit or activate integrins like αvβ3 and αvβ5, which are formulated for topical application to improve skin and hair care by reducing wrinkle formation, promoting wound healing, and addressing aging processes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If linear peptides are used in cosmetic compositions, then they can provide functional attributes such as enzyme inhibition and antiviral activity, but they suffer from conformational flexibility and easy digestion by proteases leading to poor efficacy

Engineering Contradiction:

Improvepeptide stabilityVSAvoidpeptide structural stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by cyclizing the peptide structure, transforming linear peptides into cyclic forms. This structural parameter change confers conformational stability and resistance to proteolytic degradation, directly resolving the contradiction between maintaining functional activity and improving structural stability.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material strategies by combining cyclic peptide structures with specific amino acid sequences containing integrin-binding motifs (such as RGD sequences). This composite design integrates structural stability with targeted biological activity, enhancing both reliability and functional efficacy.

Inventive Principle:

Principle #40Composite materials

2Reliability

If peptides are used in cosmetic formulations, then they can provide therapeutic benefits, but they face poor solubility in cosmetic vehicles and difficult transport across membranes

Engineering Contradiction:

Improvepeptide efficacyVSAvoidsolubility and membrane transport

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent utilizes parameter changes by modifying the peptide's structural parameters through cyclization and incorporating specific amino acid compositions. These changes improve solubility characteristics and facilitate membrane permeation while maintaining therapeutic efficacy.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If peptides are incorporated into cosmetics, then they can provide functional attributes, but they pose a risk of immunogenic reactions

Engineering Contradiction:

Improvepeptide functionalityVSAvoidimmunogenic reaction risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by transforming linear peptides into cyclic structures and optimizing amino acid sequences. These structural modifications reduce immunogenicity while preserving the desired functional attributes such as integrin modulation and anti-aging effects.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP2259768B1Compositions containing cyclic peptides and methods of use

Publication Date: 2019.05.22 MERCK PATENT GMBH

AI summary

The invention relates generally to cyclic peptides and their use in compositions, especially topical, cosmetic and/or personal care compositions, and compositions containing said cyclic peptides.