Pal-LLAN Tetrapeptide for Skin Firmness and Hair Growth
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Solution Overview
Problem
Current cosmetic peptides are insufficient in effectively stimulating the synthesis of extracellular matrix (ECM) proteins, such as collagen I and fibrillin 1, and do not adequately address hair growth stimulation, leading to suboptimal skin and hair treatment outcomes.
Innovation Solution
A novel tetrapeptide, Pal-LLAN, is developed, which mimics a fragment of the dermal ECM glycoprotein Emilin 1, enhancing skin penetration through terminal modifications, and is used in topical compositions to stimulate collagen I and fibrillin 1 synthesis, promoting skin and hair health.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing cosmetic peptides are used to stimulate ECM protein synthesis, then some skin improvement effects are achieved, but the stimulation of collagen I and fibrillin 1 synthesis is insufficient and hair growth stimulation is inadequate
Solution Approach 1:
The patent modifies the peptide sequence parameters by using the specific tetrapeptide sequence LLAN (Leu-Leu-Ala-Asn) instead of conventional peptides, and optimizes terminal modifications (N-terminal acylation with fatty acids like palmitic acid, myristic acid, or lauric acid) to enhance binding affinity and stimulation effectiveness on fibroblasts, thereby achieving superior collagen I and fibrillin 1 synthesis stimulation
Solution Approach 2:
The invention creates a composite active ingredient system by combining the tetrapeptide sequence LLAN with specific terminal modifications (acyl groups) and potentially combining multiple modified tetrapeptides in a composition, achieving synergistic effects that enhance ECM protein synthesis stimulation and hair growth promotion beyond what single conventional peptides can achieve
2Reliability
If peptide concentrations are increased to improve stimulation effects, then better skin and hair treatment outcomes are achieved, but cost and potential irritation increase
Solution Approach 1:
The patent changes the molecular parameters of the peptide through terminal modifications (adding fatty acid chains) that enhance cell membrane penetration and receptor binding affinity, allowing the peptide to achieve effective stimulation of collagen I and fibrillin 1 synthesis and hair growth at much lower concentrations (e.g., 0.01-5% in cosmetic compositions), thereby reducing both cost and potential irritation
3Reliability
If terminal modifications are added to enhance skin penetration, then biodisponibility is improved, but peptide complexity increases
Solution Approach 1:
The patent modifies only the terminal parameters of the peptide (adding fatty acid groups at the N-terminus) while keeping the core tetrapeptide sequence LLAN simple and unchanged, achieving enhanced skin penetration and biodisponibility through a straightforward chemical modification rather than complex structural changes
Solution Approach 2:
The invention separates the functional elements into distinct segments: the simple tetrapeptide sequence LLAN provides the biological activity for ECM stimulation, while the terminal fatty acid modifications (acyl groups) provide the skin penetration function, allowing each segment to be optimized independently without increasing overall complexity
Data Source
AI summary
The tetrapeptide has the general Formula X-LLAN-Z wherein at the N-terminal end X is selected from H, —CO—R1, —SO2—R1 or a biotinoyl group, at the C-terminal end Z is selected from OH, OR1, NH2, NHR1 or NR1R2, and R1 and R2 are selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy, saccharide and aryloxy, said group having from 1 to 24 carbon atoms. A preferred peptide is the Pal-LLAN. This tetrapeptide can stimulate the synthesis of molecules constituting the dermal extracellular matrix, in particular collagen 1 and fibrilin 1, and can be used for a cosmetic treatment, in particular anti-aging, anti-wrinkle and fine lines, to improve the skin mechanical properties, firmness/tone/elasticity/flexibility, to increase skin density and volume, for a restructuring effect and/or to fight against stretch marks, and skin sagging. The peptide is also adapted to stimulate hair growth.