Skin and Cosmetic · 2002

A synthetic hexapeptide (Argireline) with antiwrinkle activity

Um hexapeptídeo sintético (Argireline) com atividade antirrugas

Blanes-Mira C, Clemente J, Jodas G, Gil A, Fernández-Ballester G, Ponsati B, Gutierrez L, Pérez-Payá E, Ferrer-Montiel A

Int J Cosmet Sci

DOI: 10.1046/j.1467-2494.2002.00153.x PubMed: 18498523

Summary

This pioneering study, published in the International Journal of Cosmetic Science, characterized for the first time the mechanism of action and clinical efficacy of Argireline (acetyl hexapeptide-3, or Ac-EEMQRR-NH2). The peptide was developed as a topical, non-invasive alternative to botulinum toxin for the treatment of facial expression wrinkles.

The mechanism of action of Argireline was elucidated through in vitro biochemical assays: the peptide competes with SNAP-25, an essential protein of the SNARE complex responsible for the fusion of synaptic vesicles with the plasma membrane. By inhibiting the formation of this complex, Argireline reduces neurotransmitter release at the neuromuscular junction, decreasing the muscle contraction that causes expression wrinkles — a mechanism analogous to botulinum toxin, but in a milder and non-invasive manner.

In the clinical phase, an emulsion containing 10% Argireline was applied topically to the periocular region of volunteers for 30 days. Analysis by silicone replicas and digital profilometry revealed a reduction of up to 30% in wrinkle depth, a statistically significant result. Skin tolerability was excellent, with no irritation or sensitization.

This work was fundamental in introducing the concept of "topical Botox" in cosmeceuticals, demonstrating that peptides of small molecular size can modulate neuromuscular activity when applied to the skin. Argireline subsequently became one of the most widely used peptide ingredients in the global cosmetic industry, present in thousands of anti-aging formulations.

Related Peptide

Argireline

Acetyl Hexapeptide-8, Acetil Hexapeptídeo-8

Acetylated hexapeptide with anti-wrinkle action that inhibits the SNARE complex, reducing facial muscle contraction. Known as a non-invasive alternative to botulinum toxin for the treatment of expression lines.