Cosmeceuticals are cosmetics that claim to have medicinal properties, with bioactive ingredients that may produce anti-aging effects. In this 10-minute video, I walk through how formulators can choose the best cosmeceutical actives for their application. I'll review:
- Picking the most effective cosmeceutical actives for your formulations
- What to consider when comparing cosmeceutical actives
- Ensuring efficacy
Click below to view the video.
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Cosmetics today are able to give consumers better results than ever before and a lot of that has to do with cosmeceutical active ingredients. But as a formulator how do you know what's out there and how do you know the best ones to pick for your application? This video will go through some of the selection criteria you should be using when selecting actives for your next cosmeceutical developments.
- The first and most important principle is that active ingredients should be used in finished products the way they were to obtain the test results. What this means is if the ingredient was used at 2% in a cream applied twice daily to obtain the results in the in vivo efficacy data, you would need to use it at 2% in a cream also, with the directions to apply twice daily.
- You could not use the evidence from a twice-a-day leave-on product for a once-a-day wash-off or once-a-week leave-on product, for example.
- In vitro and ex vivo data won't necessarily give you a formulation input to use.
- So look for in vivo use and efficacy data to ensure you're using the active ingredient in an amount that will get proven results. You can find multiple product and technical data sheet on Prospector, giving efficacy results for in vivo tests by conducting searches of their extensive database.
What to consider when comparing cosmeceutical actives
When comparing actives, you need to consider:
- Product, form, and compatibility: We're going to take a good look at this in the next section.
- Amount to be used: This can impact your formula but also cost. A more expensive material used in small quantities may work out cheaper than using a cheaper material in larger quantities.
- Company philosophy: How green and natural does the formula need to be and how does that then limit your active ingredient selection?
- Look for strong marketing claims from in vivo results and compare these between actives. This may give you very clear indications of which material will give you the best performance results. If you have a few materials that compare on cost, philosophy and in vivo performance, comparing in vitro and ex vivo data may then help you determine which active will work best for your application.
- Request samples of the actives and trial them in your formula. What sounds good in theory may have an unexpected and undesirable effect in the finished formula, and that may make your decision for you. Use the Prospector database extensively to get active ingredient information and then contact your supplier for samples.
When ensuring efficacy of a finished product, there are two key things to remember.
- The first is to ensure that you are formulating a compatible base with the active so that your active remains available in the formulation.
- And two, you need to make sure you get that active to the target delivery site. Where will it be effective? So you need to create your formula to ensure delivery of your active ingredient to where it needs to be to get the desired result.
Active ingredients may have specific pH and temperature compatibilities. They may also be affected by charge. They may also be oil- or water-soluble and you'll need to make sure you disperse them into the right medium to ensure stability in the formula over a long shelf life. Some other considerations may include:
- pH: Make sure the active is used in a formula with a suitable pH, otherwise it may be inactivated or degraded. Look specifically for this information on supplier data sheets.
- Temperature of addition: Again, adding an active to a hot product may inactive it. Most actives need to be added below 40 degrees. But refer to supplier data sheets to be sure you're adding your active at the right temperature.
- Shear may impact some actives. Another important piece of information to check for on supplier information sheets, especially if the active is provided in a liposome or encapsulated form.
- Some actives may be inactivated when too much water is present. So check this feature carefully too and adjust the product form or water input, if required.
- Your formula will need to be stable when the active is added and the active may have very specific pH, temperature or other compatibility requirements. Make sure you check for this information carefully, which can be obtained through the Prospector database.
Delivering cosmeceutical actives to the target site
The skin is a relatively thick and complex organ designed, amongst other features, to protect tissues and organs within the body from externally applied substances. To be their most effective, cosmetic ingredients need to penetrate the epidermal layers sufficiently to perform their specific function, and this will vary depending on the type of product you're creating.
For example, a moisture protective product only needs to penetrate and preferably provide some sort of film forming at the stratum corneum level. While a product designed to boost hydration over a prolonged period will need its ingredients to penetrate to the mid-layers of the epidermis, whilst also preferably providing some moisture protective properties at the stratum corneum level.
Cosmeceutical ingredients, particularly advanced cosmeceutical ingredients that activate dermal-epidermal communications, need to penetrate to the stratum basale level. The key thing to remember when formulating is where do you need the ingredients to go and how are you going to get them there?
Stratum cornea hydrophilic pathways require water soluble substances to be less than 0.4 nanometers in diameter to penetrate past this layer. While the stratum corneum lipid by-layer will allow passage of much larger lipophilic substances on a nano scale of less than 13 nanometers. The stratum corneum inter-corneocyte space will allow passage of lipophilic substances with a diameter of 20 to 75 nanometers, but then you face the challenge of the substance being able to pass through the protective intercellular lipids, which have a stratum corneum thickness of 10 to 40,000 nanometers.
To help actives penetrate to the mid-layers of the epidermis or stratum granulosum, use osmolytic substances such as:
- propylene glycol
- butylene glycol
Many actives will come combined with these substances to protect them and enhance delivery. Substances used to reduce the polarity index of the skin such as dimethyl isosorbide can also enhance delivery of actives, particularly water soluble actives, to mid-layers of the epidermis.
To help actives penetrate into the deeper layers of the epidermis or stratum basale, and this is where you want most peptides and actives with an action on melanocytes, dermal-epidermal junction, elastin, and collagen synthesis to reach, use emulsions with very fine droplet size or small liposomal delivery. Be careful, though, because emulsions with very small droplet size may appear translucent, blue-gray or cloudy compared to a pretty white. While that very small droplet size may be ideal for delivery, it may not be aesthetically pleasing for your consumer.
You may also use micro or nano-encapsulated substances to help enhance delivery. But be careful of how you introduce and stabilize these in your formulas.
High shear, for example, can break the capsules during mixing and yet if they aren't mixed into formulas homogeneously or stabilized effectively, actives may settle to the bottom or top, over the shelf life, and not be delivered in their required doses. So you may need to use a couple of these delivery systems to ensure your active ingredients get to their target site. Remember it's not just about delivery, but also ensuring compatibility of your base formulation.
So you may need to check and double check those product information sheets from your suppliers to ensure you're not only getting the material to their active site, but also formulating a compatible base.
Finally, here's an active checklist to help you make sure you're selecting the right active for your next development and using it appropriately.
|Active ingredient consideration||Check|
|Most effective in vivo results?|
|Most effective in vitro/ex vivo results?|
|Most bio-available pH range/best stability|
|Temperature and/or shear of addition checked?|
|pH, shear and temperature requirements compatible with all other ingredient/method/compounding requirements?|
|Delivery enhancing formulations methods incorporated?|
|Suits company philosophy? (Check also 'green'/naturalness, incidental preservatives and additives.)|
[Download the CHECKLIST: Selecting an effective cosmeceutical active PDF]
Happy formulating for great results from your next cosmeceutical development.
|ACTIFCOL™ advanced botanical ingredient by Lipotec S.A.U. - ACTIFCOL™ advanced botanical ingredient is a shiitake mushroom-based extract, selected to boost the synthesis, improve the quality and reduce the deterioration of collagen, a key protein in imparting tensile strength. An improvement in collagen quality is known to imply a firming effect on the skin.|
|REPROAGE™ peptide solution by Lipotec S.A.U. - REPROAGE™ peptide solution is a peptide that modulates the levels of microRNA-145 (miR-145), which is involved in the regulation of epidermal differentiation. It may support cell reprogramming to boost radiance and youthfulness of the skin complexion. This product can be incorporated into any anti-aging formulation to cope with the slowdown in skin regeneration that takes place with age. It can also be used in formulations designed to rejuvenate the skin.|
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