Argireline®, the “topical Botox™”. How well did it age?

When I last wrote about Argireline in the oldSkin Actives forum (now inactive), I had two main objections: 1) that the (scant) research asserting its activity came from the same lab that sells it and 2) that they sell the peptide greatly diluted in a solution that does not promote peptide stability.

I always suspected a gimmick.  Why? Botulinum toxin is a neurotoxic protein of molecular weight of about 150K produced by the bacterium Clostridium botulinum. This is serious business, a toxin that kills. However, in the hands of expert MDs, this toxin can treat some uncomfortable problems, including muscle spasms and some migraines.

MDs, and some reckless people with no fear of lawsuits treat some wrinkles by temporarily paralyzing some facial muscles by injecting Botox.  Anyone considering “getting Botox” should read about the side effects and signs of an allergic reaction—caveat emptor.

Then, in 2002, a Spanish company came out with a synthetic, short peptide that could be applied topically and do the same job as Botox at a much lower price and without injections or side effects!  But…

Proteins are big, expensive, and hard to make and keep active

Why do we (biochemists, Skin Actives) bother to make proteins, which are expensive, long, fragile, and require high skills, if a short peptide (inexpensive, made to order by any number of companies) would do?

Because peptides can’t do what a complex protein can, folding in space in such a way that allows it to bind to the receptor or substrate (if the protein is an enzyme).

Does Argireline work?

What we decided to do at the time was to sell the concentrated peptide in a solution that WILL keep the peptide alive (protecting its integrity) so at least our customers could have a chance to test the peptide, so that they could try Argireline by adding it to a cream or serum base.

Now we have some further evidence (Lungu et al, 2012).  Topical Argireline was tried by doctors on patients suffering from blepharospasm and found that it didn’t replace Botox. Surprise!

So, the answer is no. A short peptide applied topically can’t replace an injected powerful toxin.

We at Skin Actives will keep working hard at making proteins, like epidermal growth factor or superoxide dismutase, because they work. If a short peptide is shown to be able to replace a large complex protein, we will let you know but don’t hold your breath.

The take-home message

Don’t expect peptides, even those with pretty names, to be effective. On the other hand, most of them are safe, destined to be broken down into amino acids. The exception are the peptides that have copper with them, which is because of the toxicity of copper at high concentrations and not because of the peptide!

Remember those fabulous proteins known to be effective at rejuvenating your skin inside and out: epidermal growth factor, antioxidant proteins, and those ingredients backed by so much research. Those are your tools; use them!

Hannah

References

Blanes-Mira, C.; Clemente, J.; Jodas, G.; Gil, A.; Fernandez-Ballester, G.; Ponsati, B.; Gutierrez, L.; Perez-Paya, E.; Ferrer-Montiel, A. (2002)  A synthetic hexapeptide (Argireline) with antiwrinkle activity    International Journal of Cosmetic Science,  24(5),  303-310. 10.1046/j.1467-2494.2002.00153.x

Lungu, C., Considine, E., Zahir, S., Ponsati, B., Arrastia, S., & Hallett, M. (2012). Pilot study of topical acetyl hexapeptide-8 in the treatment for blepharospasm in patients receiving botulinum toxin therapy. European Journal of Neurology, 20(3), 515–518. doi:10.1111/ene.12009