ARGIRELINE®

INCI name: Acetyl Hexapeptide-8
The anti wrinkle hexapeptide ARGIRELINE® represents the discovery of a positive hit based on a scientific pathway from rational design to GMP production. The study of the basic biochemical mechanisms of anti-wrinkle activity has led to this revolutionary hexapeptide which has taken the cosmetic world by storm. Finally, an anti-wrinkle treatment which can compete with the efficacy of Botulinum Toxin A but leaves aside the risks, the injections and the high cost: ARGIRELINE®.
ARGIRELINE® reduces the depth of wrinkles on the face caused by the contraction of muscles of facial expression, especially in the forehead and around the eyes. ARGIRELINE® is a safer, cheaper, and milder alternative to Botulinum Toxin, topically targeting the same wrinkle-formation mechanism in a very different way.

Antiwrinkle Activity Units (AAUs)

Dose-response curves obtained from the catecholamine release tests yield IC50 values for the different peptides. We can therefore quantify and compare the exocytosis-blocking activity, which is directly related to the antiwrinkle power. This facilitates the definition of an Antiwrinkle Activity Unit (AAU) (A synthetic hexapeptide – Argireline- with antiwrinkle activity, Blanes-Mira C, Int.Journal Cosm Sci, 2002, 24, 303 – 310).
AAU SAMPLE = [IC50] ESUP E / [IC50] SAMPLE

Anti-wrinkle test on healthy volunteers (10% ARGIRELINE® Solution)

Skin topography analysis for measuring the effectiveness of an O/W emulsion containing 10% of ARGIRELINE® Solution were performed obtaining silicon imprints from around the eyes from 10 healthy women volunteers. Silicon imprints were obtained pre-test and after 30 days of twice a day applications. Analyses of the imprints were performed by confocal laser scanning microscopy to assess the evolution of the skin surface before and after the treatment. Skin topography images from the three dimensional reconstruction of optical sections are shown. It can be observed that the depth of the wrinkle has significantly decreased after 30 days of treatment which confirms the validation of the biochemical mechanism hypothesis.
Skin topography images before (left) and after a 30 day treatment with a cream containing 10% ARGIRELINE® Solution (right). The top pictures show an ordinary cream used as a negative control. The bottom pictures show a cream with the same formulation containing ARGIRELINE®.

Anti-wrinkle test on healthy volunteers (5% ARGIRELINE® Solution)

A cream containing 5% ARGIRELINE® SOLUTION (0.05%) was applied twice daily around the eyes of 14 volunteers, aged 39 to 64, for 28 days. Silicon imprints of the treated areas were obtained before the test and after 28 days, and roughness was measured by confocal profilometry. A decrease of 16.26% in wrinkle depth was accomplished, with maximum values up to –31.80%.
Representative images of the silicon replicas before (left) and after a 28 day treatment with a cream containing 5% ARGIRELINE® Solution (right). Dark blue colour indicates maximum depth – bright red colour indicates max height. The top pictures show and ordinary cream used as a negative control.
ANTI-WRINKLE TEST ON HEALTHY VOLUNTEERS (5% ARGIRELINE® SOLUTION)
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