Argireline (Acetyl Hexapeptide-3)

Known as 'topical Botox,' Argireline is a peptide that reduces the appearance of expression lines by partially inhibiting the SNARE complex — the same mechanism targeted by botulinum toxin, but through topical application rather than injection. The effect is much milder than Botox (roughly 30% wrinkle reduction vs 80%+) but provides a non-invasive option for forehead lines, crow's feet, and frown lines.

Concentration & Usage

Typically used at 5-10% concentration. Apply twice daily to expression line areas (forehead, around eyes, between brows). Effects visible after 2-4 weeks. Must be used continuously — effects reverse when stopped.

Application

Topical (serum, cream). Water-soluble. Apply directly to expression line areas.

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Mechanism of Action

Argireline (acetyl hexapeptide-3) mimics the C-terminal region of SNAP-25, a core SNARE complex component. The SNARE complex (SNAP-25, syntaxin, synaptobrevin) mediates vesicle fusion at the neuromuscular junction for acetylcholine release. Argireline competes with SNAP-25 for syntaxin binding, partially disrupting SNARE assembly and reducing neurotransmitter exocytosis. This decreases acetylcholine release and attenuates facial muscle contraction intensity. The effect is dose-dependent, localized, and reversible—unlike botulinum toxin's enzymatic cleavage of SNAP-25. Clinical studies show ~30% wrinkle reduction versus 80%+ with injectable neurotoxins. Provides non-invasive expression line softening.

Regulatory Status

Cosmetic ingredient. Available OTC worldwide. Developed by Lipotec (now part of Lubrizol).

Risks & Safety

Common

Very well-tolerated. Occasional mild tingling.

Serious

None documented.

Rare

Allergic reaction. At very high concentrations, some users report a slight 'droopy' feeling in the treated area.

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Research Papers

10
Skin scars and wrinkles temporary camouflage in dermatology and oncoesthetics: focus on acetyl hexapeptide-8.

Published: November 4, 2020

AI Summary

The aim of study is to evaluate the aesthetic outcome of specific formulated cosmeceutical product to mask and reduce the appearance surgical scars or unappealing skin tags in chronic diseases, such as cancer

In vitro skin penetration of acetyl hexapeptide-8 from a cosmetic formulation.

Published: March 21, 2015

AI Summary

Claims for one cosmetic peptide, acetyl hexapeptide-8 (Ac-EEMQRR-amide), suggest interference with neuromuscular signaling as its anti-wrinkle mechanism of action. The results (percent of applied dose) showed that the majority of the Ac-EEMQRR-amide was washed from the surface of both HGP and human skin.

The anti-wrinkle efficacy of Argireline.

Published: August 5, 2013

AI Summary

Argireline, a synthetic peptide, which is patterned from the N-terminal end of the protein SNAP-25, can both reduce the degree of existing facial wrinkles and demonstrate effectively against their development. In our past studies, we found out that Argireline had a significant anti-wrinkle effect in

Enhanced Skin Permeation of Anti-wrinkle Peptides via Molecular Modification.

Published: January 24, 2018

AI Summary

Argireline (Arg0), a mimetic of Botox, has been found to be safer than Botox and effective in reducing wrinkles, with efficacies up to 48% upon 4 weeks of twice daily treatment. Enhanced human skin permeation was demonstrated by both Arg2 and Arg3 in vitro.

The anti-wrinkle efficacy of argireline, a synthetic hexapeptide, in Chinese subjects: a randomized, placebo-controlled study.

Published: April 18, 2013

AI Summary

It is reported to inhibit vesicle docking by preventing formation of the ternary SNARE complex and by interfering in catecholamine release. The anti-wrinkle efficacy of argireline has not been studied in Chinese subjects.

The study of cellular cytotoxicity of argireline - an anti-aging peptide.

Published: March 16, 2014

AI Summary

The argireline inhibitory concentration, IC50 values were calculated and the results were compared to the IC50 value of the reference compound: doxorubicin. However, the significant cytotoxicity of argireline solution was observed under 18 to 10 000 fold higher concentrations (depending on cells that were examined) in comparison to doxorubicin.

Influence of the modification of the cosmetic peptide Argireline on the affinity toward copper(II) ions.

Published: March 25, 2024

AI Summary

Additionally, based on density functional theory (DFT) calculations, we propose the most likely structures of the resulting Cu-peptide complexes. The biological results were subsequently compared with free Argireline, its Cu(II)-complexes, and the previously studied AN2 derivative (EAHQRR).

Topical delivery of acetyl hexapeptide-8 from different emulsions: influence of emulsion composition and internal structure.

Published: February 19, 2015

AI Summary

By applying LC-MS/MS for quantification of AH-8, we demonstrated that a multiple water-in-oil-in-water (W/O/W) emulsion can significantly increase penetration of AH-8 into porcine skin compared to simple O/W and W/O emulsions.

Preparation and stability of cosmetic formulations with an anti-aging peptide.

Published: November 20, 2007

AI Summary

We prepared two formulations: an emulsion with an external aqueous phase for normal to dry skin, and a gel for oily skin. Laboratory analyses, rheology tests and in vitro release assays were used to evaluate the stability of these formulations for cosmetic treatment.

Frequently Asked Questions

What is Argireline (Acetyl Hexapeptide-3) used for?

Known as 'topical Botox,' Argireline is a peptide that reduces the appearance of expression lines by partially inhibiting the SNARE complex — the same mechanism targeted by botulinum toxin, but through topical application rather than injection. The effect is much milder than Botox (roughly 30% wrinkle reduction vs 80%+) but provides a non-invasive option for forehead lines, crow's feet, and frown lines.

What are the side effects of Argireline (Acetyl Hexapeptide-3)?

Common: Very well-tolerated. Occasional mild tingling. Serious: None documented. Rare: Allergic reaction. At very high concentrations, some users report a slight 'droopy' feeling in the treated area.

How is Argireline (Acetyl Hexapeptide-3) administered?

Argireline (Acetyl Hexapeptide-3) is administered via topical (serum, cream). water-soluble. apply directly to expression line areas..

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