Peptide Chemistry

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Peptide Chemistry

Tell a customer that your product contains peptides and you'll always spark their interest even if most of us don't really understand what they are and how they work. We just know that they have the capacity to do great things and great things is what we really want!


Boost Collagen and Elastic | Control Melanin Production | Manage Inflammation | Barrier Protection, Anti-Microbial.

Peptides are biologically active signalling molecules, made of amino acids (the same stuff that makes up proteins, the stuff that makes up around 20% of your lean body mass, another 60% being water and the rest a mix of stuff including your bone minerals). Amino acids arranged in certain shapes and sizes can act like keys for a range of biological processes where they typically deliver the signal that tells a process to move. In the cosmetic space some of these processes include the key to unlocking collagen synthesis, elastin arrangement, melanin production, inflammation, microbe fighting and barrier protection.

In cosmetic science we use peptides that are synthetic or man-made, the exact shapes and sizes we use don't exist naturally. Peptides are manufactured this way to give them a better chance of reaching the target tissue (don't forget that in real life, peptides are produced close to the site of action whereas ours have to be able to penetrate the rather tricky epidermal barrier as a minimum), of being stable outside of the skin environment (to that they can be supplied), to better control delivery over a period of time and to reduce toxicity. The down side about all of this work is that it is expensive. Peptide synthesis requires lots of high-tech science equipment and knowledge, refining the molecule shape and running testing is also time consuming and costly and coming up with novel anti-ageing technology is financially lucrative and is therefore always protected by patents and other instruments. So, all up you typically pay roughly (today's prices) at least $1000 AUD per Kg for a cosmetic peptide, as supplied, and most manufacturers supply them in presentations that require a dose rate of between 0.5-3% in a formula, that means a per-formula cost of at least $5 per Kg from one ingredient but more typically $15-$30 per Kg on top of other costs. To put this into perspective, a smallish to medium-sized brand with a cosmetic night cream that contains some natural ingredients typically comes in at around $40 per Kg for ingredients. In that scenario it isn't un-heard of for your peptide input to account for between 50-80% of your overall formula costs, a significant investment but one that can bring significant returns.

If we focus back to the structure again we can think of the peptides we use in cosmetics as having two regions to do two different jobs. There is the functional 'key' part which is the bit that interacts with whatever biological process we wish to influence, then there is the tail part which is the man-made 'motor' part if you like, the bit that gets the peptide to where it has to go. Typically, this 'motor' part has been a fatty acid onto which the amino acids that form the peptide can be attached. These fatty acid chains can be sourced from any feedstock, vegetable or mineral with saturated C16-C18 chains likely coming from palm (although not always).

Here is what Matrixyl 3000 look like. Chemically this is now known as Palmitoyl Pentapeptide-4.

Matrixyl 3000, chemically known as Palmitoyl Pentapeptide-4

Image by: Ed (Edgar181) - Own work, Public Domain

Palmitoyl - palmitic acid tail, the 'motor'. The name palmitoyl doesn't mean it comes from palm, it means that it is a 16-carbon fatty acid. Lots of vegetable and mineral origin materials have this configuration.

Penta - means 5. Because this is referring to the number of amino acids that make up the peptide chain, in this case, a lysine rich blend.

The number 4 at the end is an arbitrary number that is assigned by INCI regulators when the molecule is first listed so lower numbers were most likely registered earlier than larger numbers - this way of attributing numbers is not unusual, many (but not all) numbers you see in INCI names are about when the ingredient was registered. This is one reason why I find it amusing when people say they don't want chemicals with numbers on them as that means something bad.

Matrixyl 3000 came onto the market in 2000 and it has remained popular because it does work quite well as long as it reaches its target tissue - it stimulates collagen, fibronectin, elastin and Glycosaminoglycan production. It also has a high level of market acceptance and awareness and is relatively widely available.

So where does it need to get to?

Collagen and elastin synthesis occur in the dermis but can be triggered by signals from fibronectin. Fibronectin is part of the extracellular matrix and is synthesised, in part by keratinocytes which, luckily enough, are the cells at the base of our epidermis (the skin that we touch). Glycosaminoglycans include hyaluronic acid and this chemistry helps to support collagen and elastin health by, amongst other things, trapping moisture.

And does it work?

Many dermatologists continue to have a slightly less rosy view of cosmetic peptides because of the evidence gap that exists for them. While cosmetic peptides have to go through some testing, that testing is typically carried out in small trials (20 people or less most often), by the ingredient manufacturers in short term trials (up to 60 days). Dermatologists have medical degrees and as scientists we are taught to look for more robust evidence than this, especially when it comes to mapping cause and effect. However, as cosmetic chemists we see the results that people get with peptides like Matrixyl and others which begs the question, are the dermatologists wrong? The answer to that is probably not.

It is likely that what happens in many cosmetic formulations is that the cause and effect relationship is somewhat more complex. Sure, the peptide gives visible results when used in a good formula base but it is likely to be contributing more through a topical action (hydration, barrier protection, catalyst for deeper processes) than it does through deep skin penetration. So yes, they work but they are doing slightly different work, albeit with similar results, to the work they advertised. Net result = happy customers with visibly improved skin.

Exciting new research.

The dermatology world is interested in peptides with over 340 papers published on the topic so far this year. New research includes the use of peptides to re-construct badly damaged skin such as full-thickness burns and other traumatic injury. Some particularly interesting advances have been made in using self-assembling peptide Nano fibre hydrogels to help stimulate the growth of bone and cartilage, heal complex wounds and better deliver drugs. Some research is even looking at using peptides to help repair the type of nerve damage that results in hearing loss! Now while not all of these applications relate to cosmetics, the technology is transferable. The use of peptide infused hydrogels is particularly interesting to me as that's essentially a super-powerful serum, the type that we commonly use in cosmetic science. It is likely that the learning from this type of research into partial thickness burns, ulcers and surgery wounds will filter up into cosmetic science and inform peptide manufacturers of the technology needed to get results at a 'maintenance' level in the cosmetic space.

New Peptides for your formulations.

Munapsys™

Topical 'Botox' actives have been on the market for almost as long as Matrixyl but traditionally they have relied on targeting one part of the muscle contraction cycle, Munapsys™ targets two. As you might expect from an upgraded model, this peptide has the capacity to reduce muscle contractions for longer and with a stronger effect than we've seen before. This dual effect does go a long way towards solving the deep skin penetration difficulties as it taps into a cascade reaction that starts much closer to the skin surface than traditional muscle relaxing peptides.

This peptide performs well with hyaluronic acid into fast-acting eye serums for an instant lift if you use the peptide at the maximum level. It can also be formulated into daily 'face-lift' serums and creams designed for use under make-up.

Epitensive®

This peptide builds on what we know about skin healing and repair by targeting a number of processes involved in skin regeneration. Its combination action makes this a great restore and repair active for deep moisturisation and the correction of premature ageing. This peptide can be formulated into a range of products but we like it in deep hydrating eye creams, night creams and serums. Pair with Pentavitin for a strongly moisturising action.

Stellight™

Uneven skin pigmentation is a marker of ageing and trauma and as such, reducing its visible impact is highly sought after. Stellight™ peptide reduces both melanin expression and transfer, again giving the product two changes to produce a visible effect. Peptides are a much safer way to reduce hyper-pigmentation than hydroquinone (which is not permitted in Australian cosmetics) and have a higher specificity than whole plant actives such as Bearberry extract. We recommend pairing this with our oil soluble vitamin C for customers looking for an all-over brightening effect with enhanced luminosity.

Progeline

The chemical signals produced by our skin to induce skin ageing are the target of this peptide. Progeline down-regulates production of the protein that speeds up cellular ageing, progerin, thus helping to maintain optimal cellular regeneration. This has the effect of improving skin firmness and elasticity, maintaining the complexion in good order. We recommend pairing this with our Ceramide complex and protective mineral complex to create a slow-release day cream or sheet mask that helps to boost the skins resilience and turn back the clock.

The future is biologically active!

Cosmetic peptides give brand owners the chance to tap into some very exciting skin regeneration science and give their customers a deeper level of efficacy. New generation peptides counter some of the problems faced by earlier peptide chemistry by focusing on beginning their activity further up the biological cascade. While this doesn't take away the need for a good skin delivery system, it does mean that it is more likely customers will see results quicker and to a greater level than before. Peptides can be combined to give multiple effects in one product or can be used alone as 'hero actives. You can experiment with some of our peptides in our hands-on 'Create your own Cosmetics' workshops which are held every quarter in Sydney. We can't wait to see what you create with this great range of active peptides and share your business success with you.

Amanda Foxon-Hill

9 August 2019

More about: Chemistry, Peptides

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