"Botox In a Bottle"

The desire to maintain a youthful appearance has driven the development of many cosmetic products and procedures. In recent years, Argireline has been in the spotlight as a new popular option to treat aging skin. In particular, the skin care brand The Ordinary's Argireline Solution 10% has gained a lot of attention. You may have even heard of the claims that this product is like a botox in a bottle. This product retails at a price of only $8.50 for 30 ml. If you're familiar with The Ordinary, then the price point is not really surprising. To those who may not be familiar with the brand, The Ordinary is known to be an affordable skin care brand with high quality products. They tend to focus on putting only high concentrations of active ingredients in all of their products. The active ingredient in Argireline Solution 10%, as the name suggests, is Argireline or acetyl hexapeptide-8 (Figure 1). So, what is Argireline and why is this product called “botox in a bottle?”  

Figure 1. The sequence of peptide Ac-Glu-Glu-Met-Gln-Arg-Arg-NH2 (Argireline). From Kluczyk, A., Ludwiczak, J., Modzel, M., Kuczer, M., Cebrat, M., Biernat, M, Bachor, R. (2021). Argireline: Needle-Free Botox as Analytical Challenge. Chemistry and Biodiversity, 18 (3). doi: https://doi-org.dml.regis.edu/10.1002/cbdv.202000992

Argireline, produced by Lipotec (a chemical manufacturing company in Spain), is a synthetic hexapeptide that mimics the N-terminal end of the SNAP-25 protein (Kluczyk, 2021). Recall the SNARE hypothesis we learned in class. As a brief overview, the SNARE hypothesis explains the mechanism by which synaptic vesicles containing neurotransmitters fuse with the presynaptic membrane and release neurotransmitters into the synapse by Ca2+ dependent exocytosis. SNAP-25 is one of the three proteins needed to form the ternary SNARE complex. The three SNAREs form a tight bundle of alpha helices, which then help provide the force needed for vesicle fusion. In voluntary skeletal muscles, the SNARE complex induces release of acetylcholine into the synapse, which eventually leads to muscle contraction. Because Argireline mimics one of the proteins in the SNARE complex (SNAP-25), it competes with this protein for the position in the ternary SNARE complex. It inhibits the formation of the ternary SNARE complex, which destabilizes the complex, and thus it inhibits vesicle fusion. As a result, acetylcholine is not released into the synapse and muscle contraction does not occur (Kluczyk, 2021). 

The reason why Argireline is called "botox in a bottle" is because it mimics the action of botulinum neurotoxins (BoNTs). BoNTs are metalloproteases that cleave synaptic proteins—membrane proteins SNAP-25 and syntaxin, and vesicular protein VAMP/synaptobrevin (Blanes-Mira, 2002). Similar to what I just described above, these toxins block the fusion of synaptic vesicles. If there’s no vesicle fusion, then there is no release of acetylcholine and in the end, there’s no muscle contraction or muscle movement. 

Although the effects of Argireline may not be as drastic as getting an actual botox injection, some studies have shown that it can help reduce the intensity of existing facial wrinkles. For example, one study conducted among healthy women volunteers showed that using Argireline solution (10%) reduced the depth of the wrinkles up to 17% after 15 days and 30% after 30 days (Blanes-Mira, 2002). Studies have also suggested that this synthetic peptide is relatively safer than botulinum neurotoxin type A (BoNTA) and could serve as a bio-safe alternative to BoNTAs.

However, there's not a lot of information about the long-term effects or adverse effects of this product so make sure to do your own research first or consult a dermatologist for any specific questions or concerns.

References: 

Blanes-Mira, C., Clemente, J., Jodas, G., Gil, A., Fernandez-Ballester, G., Ponsati, B., Guitierrez, L., Perez-Paya, E., Ferrer-Montiel, A. (2022). A Synthetic Hexapeptide (Argireline) With Anti-Wrinkle Activity. International Journal of Cosmetic Science, 24 (5), 303-310. doi: https://doi-org.dml.regis.edu/10.1046/j.1467-2494.2002.00153.x

Kluczyk, A., Ludwiczak, J., Modzel, M., Kuczer, M., Cebrat, M., Biernat, M, Bachor, R. (2021). Argireline: Needle-Free Botox as Analytical Challenge. Chemistry and Biodiversity, 18 (3). doi: https://doi-org.dml.regis.edu/10.1002/cbdv.202000992