Argireline Research & Studies

Botulinum toxin type A (BoNT-A) is increasingly recognized for tissue-level effects beyond neuromuscular blockade, but its impact on dermal collagen composition remains incompletely characterized. Acetyl hexapeptide-8 (Argireline) is a SNAP-25 mimetic cosmeceutical peptide whose biological activity at the tissue level is unclear. This study evaluated the effects of BoNT-A, Argireline, and their combination on dermal collagen type I/III and Substance P (SP) expression in a flap model.

We propose a new facial lifting protocol using polydioxanone (PDO) threads embedded in acetyl hexapeptide-8 (Argireline [Arg]). We assume that Arg reinforces the effects of PDO threads, as it is a mimetic of botulinum toxin. Because the PDO suture is hydrolyzable, this assumption is analyzed by instrumental analysis.

Argireline-containing cosmetics attract public interest due to their confirmed reduction of facial wrinkles. Argireline is a peptide that works by inhibiting the release of neurotransmitters in the neuromuscular junction, producing a botox-like effect. Therefore, it is used as a safe needle-free alternative to botox treatment. In this work we investigated the presence of Argireline in cosmetic creams and sera by application of reversed phase liquid chromatography and tandem mass spectrometry (RP-HPLC/MS and MS/MS). The analysis revealed the presence of argireline and its oxidized form in several different cosmetics. The methionine residue in Argireline sequence was indicated as oxidation point according to neutral loss MS studies. The developed sample preparation strategy minimizes and monitors methionine oxidation, bringing to our attention the question of impact of ingredients on the stability of cosmetic product.

Argireline is well know, innovative anti-aging product used in the cosmetic market. This short chain peptide is used as active ingredient in dermal ointment and creams. Argireline prevents formation of skin lines and wrinkles in a very similar way to the botulinum toxin (Botox), inhibiting neurotransmitter release at the neuromuscular junction. Argireline does not require under skin muscle injections and it is believed to be relatively safe. However, despite the fact that some toxicity data has been provided by the product manufacturer, there is an evident lack of reliable information about cytotoxicity of argireline in the literature. The aim of the presented study was to estimate the antiproliferation effect of argireline solution in several concentrations. The influence of argireline on cellular proliferation was examined against: human embryonic kidney HEK-293 cell line, human neuroblastoma IMR-32 cell line, and human primary skin fibroblasts. Tests were performed using formazan-based cell proliferation assay: EZ4U, which allows to measure the efficiency of mitochondrial oxidative activity in living cells. The argireline inhibitory concentration, IC50 values were calculated and the results were compared to the IC50 value of the reference compound: doxorubicin. In conclusion, the considered method resulted in dose-dependent argireline anti-proliferation effects. 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.

Abstract Background: This is the first multicenter clinical and experimental study of the anti wrinkle efficacy of Argireline in Chinese subjects. Objective: To evaluate the safety and efficacy of Argireline in the treatment of periorbital lines in Chinese subjects, and to observe the effect of Argireline on microstructural changes of the skin in the aged mice induced by D-galactose. Methods: The study was comprised of two parts: i) Clinical study: A total of 60 subjects received a single treatment in a 3:1 randomization ratio of Argireline: placebo. Argireline or placebo was applied to their periorbital wrinkles twice daily for 4 weeks, evaluations were made for the improvements in wrinkles. ii) Animal study: Argireline was applied to the aged mice twice daily for 6 weeks and the histopathological changes of skin tissue were evaluated. Results: In humans, the total anti wrinkle efficiency in the Argireline group was 48.9%, the depth of the wrinkles was notably reduced(P<0.01). In the aged mice, there was improvements in the morphology of skin tissue, the amount of typeⅠcollagen fibers increased(P<0.01) while type Ⅲ collagen fibers decreased (P<0.05). Conclusions: The studies revealed that Argireline had significant anti wrinkle effects in Chinese subjects.

Argireline is a synthetic peptide that is patterned from the N-terminal end of the protein SNAP-25 and has been shown to reduce the degree of facial wrinkles. 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.

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 Chinese subjects and that it was safe and well tolerated.

Botulinum neurotoxins (BoNTs) represent a revolution in cosmetic science because of their remarkable and long-lasting antiwrinkle activity. However, their high neurotoxicity seriously limits their use. Thus, there is a need to design and validate non-toxic molecules that mimic the action of BoNTs. The hexapeptide Ac-EEMQRR-NH(2) (coined Argireline) was identified as a result of a rational design programme. Noteworthy, skin topography analysis of an oil/water (O/W) emulsion containing 10% of the hexapeptide on healthy women volunteers reduced wrinkle depth up to 30% upon 30 days treatment. Analysis of the mechanism of action showed that Argireline significantly inhibited neurotransmitter release with a potency similar to that of BoNT A, although as expected, it displayed much lower efficacy than the neurotoxin. Inhibition of neurotransmitter release was due to the interference of the hexapeptide with the formation and/or stability of the protein complex that is required to drive Ca(2+)-dependent exocytosis, namely the vesicular fusion (known as SNARE) complex. Notably, this peptide did not exhibit in vivo oral toxicity nor primary irritation at high doses. Taken together, these findings demonstrate that Argireline is a non-toxic, antiwrinkle peptide that emulates the action of currently used BoNTs. Therefore, this hexapetide represents a biosafe alternative to BoNTs in cosmetics.