Acetyl Tetrapeptide-5
Acetyl Tetrapeptide-5 (Eyeseryl) is a Lipotec-developed peptide that targets undereye puffiness and edema by reducing vascular permeability and inhibiting glycation, researched for periorbital anti-aging applications.
Acetyl Tetrapeptide-5 is a synthetic peptide developed by Lipotec under the trade name Eyeseryl. It is specifically designed to address periorbital edema (undereye puffiness) -- a common aesthetic concern that is distinct from wrinkle formation.
Overview
Undereye puffiness results from fluid accumulation in the periorbital soft tissue, driven by increased capillary permeability, impaired lymphatic drainage, and age-related changes in tissue architecture. The periorbital area is particularly susceptible due to its thin skin, minimal subcutaneous fat, and rich vascular supply. Contributing factors include sleep disruption, dietary sodium, allergies, and aging-related loss of connective tissue integrity.
Acetyl Tetrapeptide-5 was developed to address this multifactorial problem through coordinated intervention on several pathways. The peptide reduces vascular leakage by decreasing capillary filtration rate, inhibits the glycation of extracellular matrix proteins that contributes to tissue stiffening and impaired drainage, and modulates the renin-angiotensin system locally to influence fluid balance.
Clinical studies have demonstrated that topical application of Eyeseryl significantly reduces undereye puffiness as measured by both instrumental assessment and clinical scoring. The peptide is typically used at 0.01-0.05% in eye contour products and serums.
Mechanism of Action
Acetyl Tetrapeptide-5 exerts its anti-edema effect through three complementary mechanisms:
Vascular permeability reduction: The peptide decreases capillary filtration rate by stabilizing endothelial cell junctions. This reduces the transudation of plasma from capillaries into the surrounding interstitial tissue, directly addressing the primary cause of puffiness. The mechanism involves strengthening of tight junction proteins between vascular endothelial cells.
Anti-glycation activity: Glycation is the non-enzymatic cross-linking of sugars with proteins, forming advanced glycation end-products (AGEs). In the periorbital region, glycation of collagen and other matrix proteins impairs tissue elasticity and lymphatic drainage capacity. Acetyl Tetrapeptide-5 inhibits the glycation process, helping to maintain tissue flexibility and fluid drainage efficiency. The histidine residues in the peptide sequence are believed to chelate metal ions that catalyze glycation reactions.
ACE pathway modulation: The peptide modulates the local angiotensin-converting enzyme pathway, which plays a role in vascular tone and fluid balance. By influencing this pathway, Eyeseryl helps regulate the pressure gradient that drives fluid from capillaries into tissue, further reducing edema formation.
The acetyl group enhances the peptide's stability and membrane permeability, improving delivery to the target tissue in the periorbital region.
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Research
Anti-Edema Efficacy
Clinical evaluation of Eyeseryl at recommended concentrations applied twice daily for 60 days demonstrated significant reduction in undereye puffiness. Instrumental measurements showed decreased tissue volume in the infraorbital region, while clinical grading by dermatologists confirmed visible improvement in 70% of participants. Morning puffiness (the most severe presentation) showed the greatest improvement.
Capillary Permeability Studies
In vitro assays using endothelial cell monolayers demonstrated that Acetyl Tetrapeptide-5 reduces transendothelial permeability in a dose-dependent manner. Fluorescent tracer studies showed decreased paracellular flux, consistent with tightening of endothelial junctions. This effect was observed at concentrations achievable through topical application.
Anti-Glycation Activity
The peptide demonstrated significant inhibition of protein glycation in vitro, reducing the formation of AGEs when collagen was incubated with ribose in the presence of Acetyl Tetrapeptide-5. This anti-glycation activity helps preserve the mechanical properties of periorbital connective tissue and maintains lymphatic drainage efficiency.
Dark Circle and Comprehensive Eye Care
While primarily targeting puffiness, Eyeseryl has been incorporated into comprehensive eye contour formulations alongside peptides targeting dark circles (such as chrysin-based complexes) and crow's feet (such as Argireline). The multi-peptide approach addresses the distinct pathologies contributing to periorbital aging simultaneously.
Safety Profile
Acetyl Tetrapeptide-5 has an excellent safety profile for topical use in the sensitive periorbital area. Ophthalmological testing confirms no eye irritation at recommended concentrations. Dermatological patch testing shows no irritation, sensitization, or phototoxicity. The peptide is non-comedogenic and compatible with the thin, delicate skin of the eye contour area. Systemic absorption is negligible. No adverse effects have been reported in clinical studies. The ingredient is compatible with standard cosmetic formulation ingredients and stable under normal storage conditions.
Pharmacokinetic Profile
Acetyl Tetrapeptide-5 — Pharmacokinetic Curve
TopicalQuick Start
- Route
- Topical
Molecular Structure
- Formula
- C₂₀H₂₉N₇O₇ (approximate)
- Weight
- 474.8 Da
- CAS
- 820959-17-9
- PubChem CID
- 11532993
- Exact Mass
- 474.3529 Da
- TPSA
- 35.5 Ų
- H-Bond Donors
- 0
- H-Bond Acceptors
- 3
- Rotatable Bonds
- 18
- Complexity
- 515
Identifiers (SMILES, InChI)
InChI=1S/C29H50O3Si/c1-9-14-29(32-33(23(2)3,24(4)5)25(6)7)18-13-17-28(30)20-19-26(8)21-31-22-27-15-11-10-12-16-27/h9-12,15-16,23-26,29H,1,13-14,17-22H2,2-8H3/t26-,29-/m0/s1
NVSNLHXXGPBULI-WNJJXGMVSA-NResearch Protocols
subcutaneous Injection
The periorbital area is particularly susceptible due to its thin skin, minimal subcutaneous fat, and rich vascular supply.
topical
Clinical studies have demonstrated that topical application of Eyeseryl significantly reduces undereye puffiness as measured by both instrumental assessment and clinical scoring. This effect was observed at concentrations achievable through topical application.
Frequently Asked Questions
References (6)
- [5]
- [6]Negari et al -- Peptide-based cosmeceuticals: an evolving field of investigation Int J Mol Sci (2023)
- [7]
- [1]
- [2]Lintner K et al Cosmetic peptides Int J Cosmet Sci (2009)
- [4]Gkogkolou P, Bohm M Advanced glycation end products: key players in skin aging? Dermatoendocrinol (2012)
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