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Resveratrol
I should have a sample of pure Resveratrol arriving mid-week. This is being evaluated as a potential ingredient for a melasma treatment. Has anyone used this ingredient before? I’m interested in determining the correct usage % for skin lightening.
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31 Replies
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Well it looks like 1% and 1% vitamin E (I guess the resveratrol is dissolved in the vitamin E, it’s a hydrophobic molecule) from a piece in the Dermatology Times. Interestingly, it has a similar pseudo-estrogenic effect as that possessed by glycyrrhizic acid.
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How are you going to evaluate it?
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testers; I will have to evaluate it as a single ingredient of course (I can’t avoid the vitamin E though)
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Is there any evidence that resveratrol or pterostilbene (photoisomerised or not) have any definable activity in a cosmetic product?
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T-Resveratrol is a cox 1 inhibitor and thus an anti-inflammatory http://iovs.arvojournals.org/article.aspx?articleid=2378029
Has also been shown to demonstate bacterioststic activity agaaint p. acnes-https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4257953/—-I am sure you can find more if you search.We are currently doing applied research for various applications including a proposed clinical IRB. -
My concern is that the investigative work on resveratrol is directed at pharmaceuticals:
T-Resveratrol is a cox 1 inhibitor and thus an anti-inflammatory
its cytotoxic effect on p. acnes is demonstrated in multiple studies
Even the initial post here states that the intended use is as
potential ingredient for a melasma treatment.
Key word there being “treatment”.
References to Dermatology Times are made which emphasises further the medical or potential drug, rather than cosmetic, use of the material.
All of this is research work and out of the scope of the definition of a cosmetic product.
I appreciate that Belassi is in Mexico where normal definitions of a cosmetic might not apply but the thread has been resurrected by others - one of whom states:
I’m not a cosmetic chemist and I’m new to formulating with tRes.
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#JOHNUB-??????-Cosmetic Ingredient listed as follows and marketed as such. Ingredientingredienthttp://www.paulaschoice.com/cosmetic-ingredient-dictionary/definition/skin-soothing/resveratrol.
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I don’t doubt that resveratrol may be listed by paulaschoice and that it may be used as a cosmetic ingredient but the uses being advocated in this thread are distinctly referred to medicines and, as such, do not fall within the remit of cosmetic chemistry.
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@johnb is absolutely right. In Cosmetics all you can essentially say “great anti-oxidant” and then build the claims on diffuse benefits from anti-oxidant activity. Even exploring the Medical benefits is a dead end.
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Retinol, a cosmetic ingredient, followed a similar pathway and hardly ended up in a dead end.
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I’ve been testing a COSMOS formulation using Eve’s t-resveratrol. I chose the COSMOS formulation because (a) I wanted to evaluate whether a typical COSMOS formula compared well with a more traditional approach; and (b) I wanted to compare (empirically) the effects of using t-r versus Showa Denko’s exotic form of Vitamin C.
- first I want to say that these are my personal opinions only and I am not a formally qualified chemist -
1. The COSMOS formulation relied for preservation on a combination of alcohols / glycols, including ethanol at 15%. This is the reason I chose this formula as a vehicle for the trans-resveratrol; it is pretty much impossible to dissolve in anything except ethanol. Therefore the first step was to dissolve the t-r in pure ethanol. To preserve the efficacy of the finished product it was put in airless pump containers.2. The Vitamin C formula is my own design and its intention is to preserve the efficacy of the Vitamin C as long as possible. To this end, it also includes pine bark extract which acts to prevent oxidation of the Vitamin C. However, it should be noted that pycnogenol is also regarded as an active ingedient in that it acts as a lightener. So, at the moment I am unable to compare on a single-ingredient basis as far as the C cream is concerned.
3. We tested the product using it as a night cream on my wife and myself and other family members, and the wives of friends.
4. After a couple of weeks we evaluated the results. (Treated area vs untreated area)
My opinion is that the Vitamin C / pine bark combo had less lightening effect than we wanted - we did notice paler skin in the treated area after about 3 weeks use. The T-R had about the same effect. Noticeable but not wow.
On the other hand, the C / pine bark combo had a marked effect on skin tone; the skin seemed to become thicker, wrinkles were reduced. On the volar forearm, using it on one area only, produced a demarcation line between relatively smooth and wrinkled skin. We didn’t see much of an effect with the T-R.
We’re in test batch production of the Vitamin C version at the moment, having designed a label, box, and box leaflet. -
@DRBOB@VERDIENT.BIZ I actually was contracted to do some work on the NDA for Retinol for Acne. The NDA is still wallowing. In fact, Retinol has the same limitation. There are possible medically supported claims, but you must limit claims to Cosmetic claims. It is in fact, the same exact situation. Trans-retinoic acid aka Tretinoin (Retin-A, Renova) is the prescription post-cursor which fulfills most of the Medical uses at this time.
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I agree and went all through this at JNJ. Why go through an NDA with retinol which is a pro-drug and goes to all Trans retinoic acid in vivo?.Same is true for analogs of T-resveratrol as triacetyl analog is stable but is converted back to T-RES in melanocytes. both have cosmetic attributes so why not use them and avoid drug claims.I was at JNJ when they acquired ROC for the very reason we are discussing this.
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The NDA was in hopes of making Retinol an OTC and hence opening up all markets. I am not a fan of NDA’s since (at least for now) the FDA is glacial in approving them.
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@zwapp interesting to note that Paula uses Resveratrol in her sunscreen, maybe not well thought through or perhaps the SPF protects it? Looks like they’re using the 1% trick so hard to say how much there’s in it but definitely less than 1%.
@Microformulation why would someone sponsor a NDA for retinol or resveratrol? I’m all for it, but I’ve heard it’s beaucoup pesos and time to get an application through. How many bucks are we talking?
Tretinoin works, but Retinol has a better dose adjusted efficacy to side-effect profile long term so I actually see Tretinoin as an inferior compound.@Belassi have you measured the effect of pine bark on vit c oxidation? Is it demonstrated in literature? Where can I order your cream? Send me a pm if it’s available to the US!
@DRBOB@VERDIENT.BIZ Perhaps they would NDA retinol to reduce competition as OTC manufacturing is more expensive? Otherwise I’d think a company that size would look for patentable analogs like with T-resveratrol analogs which they could exclusively market the heck out of, bit risky though if it’s not actually superior to the real thing, but that hasn’t stopped drug companies in the past.
My 5 cents on resveratrol: 10% alcohol seems to do OK at solubilizing 1% and it’s most stable at pH > 4. Does not play well with Benzoyl Peroxide which coincidentally has a near identical chemical structure. Could be a great option for long term acne prevention as a nurturing BP alternative.
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@ZinkWell, I was just contracted to provide some Formulation work since I had designed the initial product for the company. I think one issue was the fact that Retinol is difficult to stabilize and the client had done so. I am not sure what the project costs were, but if I had to guess close to 750K.
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Packer also recently found that Pycnogenol extends the lifetime of vitamin C in the body, prolonging its beneficial effects as an antioxidant.
There are some other studies but at the moment I am eating breakfast.
@Zink: Unfortunately we don’t supply the USA as yet. -
#zinc That is what led to retinyl palmitate analog ;efficacy is similar to retinol and more stable.T-res likely needs a similar analog as triacetyl t-res is more stable and reverts back to T-res in vivo particularly in melanocytes for inhibition of melanogenesis.
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@Microformulation so would they get a NDA for the patentable? stabilization system retinol combo or make one leading to a monograph? Or to a prescription drug? Could a company block inclusion of retinol in non Rx formulas because they found a way to stabilize it or simple spent the money to prove it has drug like effects, would the FDA even be OK with that? It’d take hundreds of products off the market.
@Belassi thanks, interesting stuff. If only ascorbic acid didn’t break out people with acne more often than not, found any way around that?
@DRBOB@VERDIENT.BIZ Good example, because retinyl palmitate again has a higher side-effect to efficacy ratio than retinol.
See the paper “Unoccluded Retinol Penetrates Human Skin In Vivo More Effectively Than Unoccluded Retinyl Palmitate or Retinoic Acid” and then there’s concern about phototoxicity which might be unique to the palimate form or just more pressing due to less effective skin penetration and hence higher potential for UV exposure “Photo-induced DNA damage and photocytotoxicity of retinyl palmitate and its photodecomposition products”. -
@zink I have to be purposefully coy, as I have an NDA (the other kind) in place. The gist of it all is that retinol is a difficult material to stabilize and as such it would be difficult to meet the required listed concentrations. Their process (patented) achieved that. If you look at patents, there are hundreds with Cosmetic materials that do not necessarily eliminate others from using them, just not in the “same way” so to speak.
OTC Products have a much higher burden of proof and testing regarding the final claimed label percentage of the active, a fact which I am sure you are aware. With Retinol, meeting and maintaining this percentage was the real task.
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@Microformulation makes sense, so they would create a stabilized Rx version of Retinol that wouldn’t affect the legality of Retinol used in other products. Or if not going the NDA route find a way to market it as a cosmetic with patent protected stabilized Retinol, analogous to Ferulic Acid stabilized Vitamin C serums?
Must be a challenge to get a 1 year shelf-life and keep retinol degradation under 10% of the label claim; air and UV proof packaging and an anhydrous formula packed with Tocopherol(s) and other fat soluble retinol protective antioxidants (e.g. BHT) could perhaps do it.
I’ve have the same issue, I want to optimize for long term stability and present a simple degradation curve to my customers so they know what they can expect when the product is stored out of sunlight at room temperature, even if it degrades more than 10% in a year. Some people might want to use it past the EXP date too, this way they’ll at least know how much bang remains.
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#zink best way would be to patent a stabilized form of retinol and its analogs ie retinyl palmitate for cosmetic use and avoid FDA completely.
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Or a stabilization system that’s not too obvious?
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Or simply use something like RetiStar Stabilized Retinol from BASF in combination with Retinyl Palmitate
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@MarkBroussard I’m using a similar combination already to help stabilize it, but the addition of .1% Sodium Ascrorbate is interesting.
Otherwise if you can do a OWO emulsion that can double shelf-life.
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