“Botox in a bottle” cosmeceutical: Argireline serum (acetyl hexapeptide 8)

Because of its anti-aging properties, argireline is a bioactive neuropeptide and cosmetic ingredient that is increasingly being used in skincare formulations. Argireline, also known as acetyl hexapeptide-3 or acetyl hexapeptide-8 depending on the source, is commonly referred to as “Botox in a bottle” due to its ability to reduce facial muscle contraction ability and wrinkle formation with daily skin applications.

argireline aka botox in a bottle or acetyl hexapeptide 8

How does argireline work?

Argireline was created specifically to have a Botox-like mechanism of action, interfering with a protein called SNAP-25 in the same way that Botox does. Argireline inhibits the release of acetylcholine, a neurotransmitter that is released to activate skeletal muscles. Acetyl hexapeptide 8 reduces the ability of mimic facial muscles to contract over time and with daily applications, which is beneficial in terms of anti-aging and dynamic wrinkle formation.

How to use argireline serum and cream?

For quick and visible results, apply argireline in a 5-10% concentration twice daily for at least 30 days. Because the molecule struggles to cross the epidermal barrier on its own, using skin penetration enhancing techniques such as iontophoresis, electroporation, microneedling, and others may result in better and faster results.

What are argireline effects on the skin?

Incorporating argireline into your skincare regimen can bring numerous benefits. Research shows that acetyl hexapeptide 8 can effectively:

  • Smooth out fine lines and wrinkles, reducing their depth by 30-50% after 30 days of twice daily use of a 5 to 10% solution
  • Reduce skin roughness
  • Prevent the formation of new dynamic wrinkles
  • Reduce trans-epidermal water loss (TEWL)
  • Increase the synthesis of Type I collagen fibers, which make up over 80% of collagen fibers in the dermis
  • Prolong the effects of Botox, leading to fewer units needed per session or longer intervals between sessions, resulting in significant savings.

It is also possible that argireline, like Botox, may help reduce the frequency and severity of tension headaches or migraines, as well as symptoms related to TMJ disorder, though further clinical trials are needed to confirm these effects.

Does acetyl hexapeptide 8 have the same risks of real Botox?

Because it is applied topically rather than through injections, the use of argireline eliminates the potential risks and complications associated with injections, such as pain, bruising, redness, swelling, and infection. Additionally, argireline serums and creams do not carry the risk of facial asymmetry, brow or eyelid drooping, or the “Spock eyebrows” that can result from improper Botox injection techniques.

What are the side effect and possible complications on argireline use?

Acetyl hexapeptide 8 is considered safe for use on all skin types. Its size and chemical properties prevent it from penetrating the skin, reducing the likelihood of an allergic reaction. However, as with any new skincare ingredient, it is always recommended to perform a patch test first. There have been no reported complications or side effects from the use of argireline in medical literature and it is generally considered safe with no known adverse effects.

There have been anecdotal reports of skin sagging when using argireline, but these claims require further objective evaluation. In theory, this could occur in some individuals and in specific areas of the face, especially if they have a predisposition to sagging. As we age, sagging can occur naturally, but it can also be counteracted by the activation of facial muscles, as is common in eyebrow and eyelid drooping. By reducing the muscle activation force in these areas, the muscles are unable to compensate for the drooping, making it more noticeable. Aside from this purely theoretical scenario, at the moment there are no other reasons to believe that argireline would cause skin sagging.

Limitations of argireline and of studies focusing on it

Like many other skincare ingredients, argireline faces the challenge of poor skin penetration. For skincare ingredients to be effective, they must cross the skin barrier and reach their targets, but peptides like argireline often have difficulty achieving this due to their relatively large molecular weight. Additionally, argireline’s hydrophilic nature further impedes skin absorption. In one study, only 0.01% of a 10% argireline oil-in-water solution applied to the skin for 24 hours was able to penetrate the outermost layer of the epidermis (stratum corneum), with the remaining 99.99% being washed away and not absorbed. However, it is worth noting that with peptides, only small amounts at the nanomolar concentration level are needed for visible effects.

It is also important to note that studies performed on skincare ingredients, including argireline, often have limitations that prevent definitive conclusions. These limitations may include small sample size, subjective evaluation, lack of control, studies conducted in vitro or in animals, and industry funding, among others.

Are there other cosmeceutical peptides alternatives to argireline?

Acetyl hexapepetide is not the only promising cosmeceutical ingredient with a botox-like effect. Among the others there are:

  • Calmosensine (Acetyl Dipeptide-1 Cetyl ester). Besides increasing elastic fibers in the skin and having skin soothing and analgesic properties, calmosensine also exerts muscle relaxant activity through a different mechanism of action.
  • Vialox (Pentapeptide-3)
  • Leuphasyl (Pentapeptide-18)
  • Syn-Ake (Tripeptide-3)
  • The efficacy study of the combination of tripeptide-10-citrulline and acetyl hexapeptide-3. A prospective, randomized controlled study.
    V Raikou – Journal of Cosmetic Dermatology, Jun 2017
    DOI: https://doi.org/10.1111/jocd.12314
  • The anti-wrinkle efficacy of argireline, a synthetic hexapeptide, in Chinese subjects: a randomized, placebo-controlled study.
    Y Wang – American Journal of Clinical Dermatology, Aug 2013
    DOI: https://doi.org/10.1007/s40257-013-0009-9
  • Cosmetic Dermatology – Products and Procedures, 3rd Edition
    ZD Draelos – Wiley Blackwell, 2022
    ISBN: 978-1-119-67683-6


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