At BulkActives we have decided to discontinue selling Ellagic acid, because it does not dissolve well, and we do not want people to take crazy risks with sodium hydroxide.

Why sodium hydroxide?

Ellagic acid is NOT easy to dissolve.

It is ONLY soluble in s strong alkaline solvent such as sodium hydroxide (NaOH) also know as Lye.

Sodium hydroxide is very dangerous to work with, it is highly caustic and will degrade organic tissue.

Theoretically one could make an alkaline solution of sodium hydroxide, dissolve the Ellagic acid, mix it into a cream, and then bring the pH down to a neutral level, but…

Why even bother with Ellagic?

Already many customers are making their DIY products fresh every week, because they do not want to use preservatives. Other customers do not use certain ingredients because they only dissolve in propylene glycol. So why even consider putting a solution of sodium hydroxide on your face.

As for Ellagic acid, is it really such an important cosmeceutical??

Sure, it is very popular in Japan, where it is used as an alternative to hydroquinone (which is banned in Japan). There are also a couple of great animal studies that suggest it a highly effective for preventing and repairing sun damage.

However, there are other products that are just as effective AND they are much easier to work with.

What are the alternatives?

Well, for sun protection the most researched product is l-ascorbic acid and its derivatives, especially when combined with Vitamin E and Ferulic acid.

For lightning and brightening the combination of Niacinamide and Glucosamine is claimed to be highly effective. There is even a recent study that suggests that Niacinamide is nearly as effective as hydroquinone in the treatment of melsama.

There are many other when topically applied actives that, like Ellagic acid, may:

lighten and brighten skin (treat melsama/hyper pigmentation)

repair and treat sun damage

prevent or reduce UVA and UVB sun damage

increase skin elasticity

act as an anti oxidant

In conclusion!

I  know that we often believe that the one product we can’t use is the most effective. However, this is far from true with Ellagic acid. Ellagic acid is not a miracle product, and you will be better of using the above mentioned alternatives for DIY skin care.

Note to our wholesale customers:

we are still selling Ellagic acid  in amounts of 5kg +, just email us as per usual.

About Vitamin C (L-ascorbic acid)

Vitamin C (L-ascorbic acid) is one of the very few skin care ingredients that is supported by strong and reliable scientific research and evidence.

However, it is also one of the most difficult products to formulate with, because it is extremely unstable.

As soon as l-ascorbic acid is mixed with water it starts oxidizing. This makes the l-ascorbic acid ineffective and also dangerous, because oxidized L-ascorbic acid is a pro-oxidant which may increase the formation of free radicals.

So, the challenge has been to make stable L-ascorbic acid products, or to make l-ascorbic acid itself stable.

Currently there are three ways this has been done:

1. The Skinceuticals Vitamin C Plus Ferulic Acid + Vitamin E formulation: The Skinceuticals study and patent shows that Ferulic acid stabilizes L-ascorbic acid, and in a lab this is probably true. However, the reality is that by the time customers get their bottle of Skinceuticals C+E+Ferulic it has been sitting on the shelves for too long, and when they open their bottle the product has turned orange, which means the L-ascorbic has started oxidizing and has become pro-oxidant.

2. Anhydrous C: “Anyhydrous” means “without water,” and this is a great way to formulate with the unstable Vitamin C. Instead of dissolving the vitamin C powder in water, it is mixed and dispersed into a silicone gel. W hen the silicone is applied to the face it acts like a dermal patch. The l-ascorbic acid will slowly be dissolved by the natural moisture in the skin, and the L-ascorbic acid will then be absorbed into the skin.

3. Vitamin C derivatives: To improve the stability of vitamin C in skin care, scientists have been looking for alternative solutions. One of these has been to create Vitamin C derivatives. Usually these are made by combining ascorbic acid with other molecules. Examples of these are the water soluble Magnesium Ascorbyl Phosphate and the oil soluble Tetrahexyldecyl Ascorbate (which is also known as Ascorbyl Tetraisopalmitate)

Vitamin C derivatives

Magnesium Ascorbyl Phosphate (MAP)

Magnesium Ascorbyl Phosphate is a water-soluble vitamin C derivative. Magnesium Ascorbyl Phosphate is not acidic so it does not irritate the skin and it is more stable than vitamin C.

Studies have shown that Magnesium Ascorbyl Phosphate is JUST as effective at boosting skin collagen synthesis as L-ascorbic acid.

Magnesium Ascorbyl Phosphate has proven to be an effective skin lightener, reducing hyperpigemnetation in some test subject.

Finally, studies have shown that Magnesium Ascorbyl Phosphate protects against UVB induced skin damage, such as inflammation and free radical formation, both duuring and after exposure to sunlight.

Even Magnesium Ascorbyl Phosphate is a lot more stable than L-ascorbic acid, it still degrades slowly when exposed to light and air.

Tetrahexyldecyl Ascorbate ( Ascorbyl Tetraisopalmitate)

Tetrahexyldecyl Ascorbate is the latest development in Vitamin C derivatives.

Tetrahexyldecyl Ascorbate is oil soluble, just like your skin, which means that it easily penetrates into the skin. It is not acidic and it does not require a low pH to get it to penetrate the skin so it does not sting. It is also stable in air and water for up to 18 months, which means it will work as an anti-oxidant long after you start using it.

Studies have shown that Tetrahexyldecyl Ascorbate is an effective skin care product. It effectively suppresses UVB-induced skin pigmentation, possibly through its anti-oxidative activity.

Tetrahexyldecyl Ascorbate also prevented UVA induced oxidative stress, and it boosted collagen synthesis.

Magnesium Ascorbyl Phosphate (MAP) References

Kameyama K, Sakai C, Kondoh S, Yonemoto K, Nishiyama S, Tagawa M, Murata T, Ohnuma T, Quigley J, Dorsky A, Bucks D, Blanock K. Inhibitory effect of magnesium L-ascorbyl-2-phosphate (VC-PMG) on melanogenesis in vitro and in vivo.

Geesin JC, Gordon JS, Berg RA. Regulation of collagen synthesis in human dermal fibroblasts by the sodium and magnesium salts of ascorbyl-2-phosphate.

Austria R, Semenzato A, Bettero A., Stability of vitamin C derivatives in solution and topical formulations.

Kobayashi S, Takehana M, Kanke M, Itoh S, Ogata E. Postadministration protective effect of magnesium-L-ascorbyl-phosphate on the development of UVB-induced cutaneous damage in mice.

Kobayashi S, Takehana M, Itoh S, Ogata E. Protective effect of magnesium-L-ascorbyl-2 phosphate against skin damage induced by UVB irradiation.

Tetrahexyldecyl Ascorbate ( Ascorbyl Tetraisopalmitate References

Xiao L, Kaneyasu K, Saitoh Y, Terashima Y, Kowata Y, Miwa N. Cytoprotective effects of the lipoidic-liquiform pro-vitamin C tetra-isopalmitoyl-ascorbate (VC-IP) against ultraviolet-A ray-induced injuries in human skin cells together with collagen retention, MMP inhibition and p53 gene repression.

Ochiai Y, Kaburagi S, Obayashi K, Ujiie N, Hashimoto S, Okano Y, Masaki H, Ichihashi M, Sakurai H. A new lipophilic pro-vitamin C, tetra-isopalmitoyl ascorbic acid (VC-IP), prevents UV-induced skin pigmentation through its anti-oxidative properties.

Fitzpatrick RE, Rostan EF. Double-blind, half-face study comparing topical vitamin C and vehicle for rejuvenation of photodamage.

Without a doubt the most popular skin care products are those which use Vitamin C, also known as L-ascorbic acid.

In this post I will write about Cellex C and Skinceuticals C E Ferulic, two popular anti aging skin care products that use Vitamin C as their main active ingredients.

I will also discuss the problems with using Vitamin C in anti ageing skin care products and some other the alternatives that are available in the form of Vitamin C derivatives.

In the next post I will be giving some examples on how we can make our own DIY Cellex C and DIY Skinceuticals C E Ferulic products.

Vitamin C and anti-aging skin care

Vitamin C is one of the most popular ingredients in anti aging skin care products. Vitamin C can benefit the skin in two ways. First it can increase collagen production, and second as an antioxidant it can reduce and prevent skin damage caused by free radicals.

Vitamin C is also one of the most studied active ingredients in anti aging skin care. These studies examined the various ways in which Vitamin C increases collagen synthesis, and the way in which vitamin C prevents free radical damage, as well as UVB damage.

For more details about these studies, please look at this list of abstracts.

Cellex C

Commercial skin care products with vitamin C started with Cellex C. Developed by Lorraine Meisner , who is a cell biologist at UW-Madison, Cellex-C was quite revolutionary. There is an interesting article about her here.

From a DIY skin care point of view Cellex C is not very practical.  The three main ingredients are: L-ascorbic acid, the mineral zinc and the amino acid tyrosin.

Tyrosin has poor solubility in water and alcohol, and requires the use of some very professional (and dangerous) solvents.

Also, L-ascorbic acid is unstable, and this is what the main problem is.

Unstable L-ascorbic Acid

It is well known that L ascorbic acid is unstable.  It reacts with water and air, and will easily oxidize. Oxidized Vitamin C is not good for the skin, instead of an antioxidant, it becomes a pro-oxidant. This means that it will increase the formation of free radicals, instead of doing what it is supped to do and decrease free radicals in the skin.

Vitamin C derivatives

Many efforts have been made to use Vitamin C in skin care products. Most of these efforts have involved developing Vitamin C derivatives. For example, products such as: Ascorbyl palmitate, Magnesium ascorbyl phosphate, and Ascorbyl Tetraisopalmitate (also known as Tetrahexyldecyl Ascorbate).

Magnesium ascorbyl phosphate and Ascorbyl Tetraisopalmitate / Tetrahexyldecyl Ascorbate, have shown to increase collagen production, and they are good stable alternatives to L-ascorbic acid. However, it would be nice if we could still use the real deal.

Stable L-ascorbic acid in skin care products

Two other solutions have been developed. One is the L-ascorbic acid in silicone. I blogged about this recently, and you can read all about it here.

The other solution was offered by Pinnel and others in their paper “Ferulic Acid Stabilizes a Solution of Vitamins C and E and Doubles its Photoprotection of Skin”.

L-ascorbic acid with Ferulic acid

The Pinnell paper proposes that:

“Ferulic acid is a potent ubiquitous plant antioxidant. Its incorporation into a topical solution of 15% L-ascorbic acid and 1% tocopherol improved chemical stability of the vitamins (C+E) and doubled photoprotection to solar-simulated irradiation of skin from 4-fold to approximately 8-fold as measured by both erythema and sunburn cell formation. Inhibition of apoptosis was associated with reduced induction of caspase-3 and caspase-7. This antioxidant formulation efficiently reduced thymine dimer formation. This combination of pure natural low molecular weight antioxidants provides meaningful synergistic protection against oxidative stress in skin and should be useful for protection against photoaging and skin cancer.”

This study (and the patent) led to the Skinceuticals C E + Ferulic product. The Skinceuticals skin care product is certainly very popular and many people swear by it.

However, is it really stable?

This sentence “Ferulic acid is a potent ubiquitous plant antioxidant. Its incorporation into a topical solution of 15% L-ascorbic acid and 1% tocopherol improved chemical stability of the vitamins (C+E)” would suggest it is.

However, some forum members have commented that their product is colored orange, and an orange product with L-ascorbic acid means that the asacorbic acid has oxidized.

Did the Pinnell study also look at for how long Ferulic acid can stabilize a solution of Vitamin C and Vitamin E?

I don’t know, and it really does not matter, because this product is something that we can DIY ourselves.

The advantage of making your own version of Skinceuticals C+E+Ferulic is that it can be made fresh every week, so it will never oxidize.

In my next post I will discuss various DIY recipes for the SkinCeuticals product.  In the meantime there are already some recipes available on our website:  ce ferulic 1 and ce ferulic 2

Active ingredients for DIY Skinceuticals CE + Ferulic

http://www.bulkactives.com/ascorbicacid.htm

http://www.bulkactives.com/ferulicacidnatural.htm

http://www.bulkactives.com/dpanthenol.htm

http://www.bulkactives.com/nah.htm

There has been some confusion about the difference between Ascorbyl Tretaisopalmitate and Tetrahexyldecyl Ascorbate.

There is no difference!

Ascorbyl Tretaisopalmitate and Tetrahexyldecyl Ascorbate are the same product with a different name.

Tetrahexyldecyl Ascorbate is a colorless to pale yellow liquid.  Its CAS number is 183476-82-6 (CAS# 183476-82-6). Its INCI name is Tetrahexyldecyl Ascorbate (INCI: Tetrahexyldecyl Ascorbate) and its chemical name is Ascorbyl Tetraisopalmitate (Chem. Name: Ascorbyl Tetraisopalmitate).

What is Tetrahexyldecyl Ascorbate?

Tetrahexyldecyl Ascorbate is a very stable, oil-soluble Vitamin C ester which has anti-oxidant activity, inhibiting lipid peroxidation. Topical use can mitigate the damaging effects of UV exposure. Studies have shown it to stimulate collagen production as well as clarifying and brightening the skin by inhibiting melanogenesis (the production of pigment) thereby promoting a more even skin tone. Unlike ascorbic acid, it will not exfoliate or irritate skin.

How do I use Tetrahexyldecyl Ascorbate?

Tetrahexyldecyl Ascorbate is one of the easiest skin care actives to use in DIY skin care.  It can be added to any cream or lotion, and it is also the key ingredient in an Anhydrous C product.  I wrote a previous post about Anhydrous C  ( l-ascorbic acid and Tetrahexyldecyl Ascorbate in a silicone base) here: http://bulkactives.com/blog/index.php/2009/11/anhydrous-c-for-skin-care-absorption-of-l-ascorbic-in-a-silicone-base/

Recent posts on various DIY skin care forums have discussed the issue of the penetration of L-ascorbic acid suspended in a silicone base into the skin.

More precisely, a few posters have started promoting the idea that L-ascorbic acid cannot penetrate into the skin, because silicone forms a barrier on the skin.

I would like to address this issue in more detail.

Background: Stable L-ascorbic acid products for skin care

The DIY skin care community has long struggled with the formulation of a stable L-ascorbic acid skin care product. In fact, professional skin care companies and formulators have also struggled with the same problem.

Some attempts have been made by professionals to develop a stable vitamin C skin care product.  The best example of this is the Skinceuticals C+E+Ferulic product.  This is based on the 2006 study “Ferulic acid stabilizes a solution of vitamins C and E and doubles its photoprotection of skin” by Pinnel and others.

This study claimed that

“Ferulic acid is a potent ubiquitous plant antioxidant. Its incorporation into a topical solution of 15% L-ascorbic acid and 1% tocopherol improved chemical stability of the vitamins (C+E) and doubled photoprotection to solar-simulated irradiation of skin from 4-fold to approximately 8-fold as measured by both erythema and sunburn cell formation.” http://www.nature.com/jid/journal/v125/n4/full/5603565a.html

However, consumers have found that skinceuticals C E ferulic product is often orange tinted.  This color usually indicates that the L ascorbic acid has oxidized, thus making it pro-oxidant.  So, even though Ferulic acid may stabilize l ascorbic acid in the lab, in practicality there appear to be some serious issues that have not been addressed.

DIY skin care formulators are able to work around this.  By making a CE Ferulic product at home, it is possible to have a fresh supply every week, thus reducing (but not eliminating) the amount of vitamin C oxidization.

Solution: The Fitzpatrick study

Another study of interest is the 2002 “Double-blind, half-face study comparing topical vitamin C and vehicle for rejuvenation of photodamage” by Fitzpatrick.

Even though this study predates the CE+Ferulic study, it did not start getting discussed on the DIY skin care forums until quite recently.

Fitzpatrick’s method was as follows:

“Ten patients having facial photodamage were recruited for a double-blind pilot study of a newly formulated vitamin C complex having 10% ascorbic acid, a water soluble acid, and 7% tetrahexyldecyl ascorbate, a lipid soluble analog.

Both of these are combined in an anhydrous polysilicone gel base, which acts as a ‘dermal patch,’ releasing the water soluble acid slowly and the lipid soluble analog rapidly. The active vitamin C complex was applied to one side of the face and the inactive placebo base was applied to the opposite side of the face once a day.” http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list_uids=11896774&query_hl=7&itool=pubmed_ExternalLink

Now, this is where a very few posters start having some issues.  The base used is an anhydrous silicone gel, and the doubt seems to be in the fact that a very few posters believe that silicone forms a barrier and therefore hinders the absorption of active ingredients.

However, let’s look at the next part of Fitzpatrick’s study:

“Biopsies showed increased Grenz zone collagen, as well as increased staining for mRNA for type I collagen. This formulation of vitamin C results in clinically visible and statistically significant improvement in wrinkling when used topically for 12 weeks. This clinical improvement correlates with biopsy evidence of new collagen formation.”

Now, if silicone prevents the absorption of active ingredients, than there would not have been an increase collagen.

So, this should put to rest the claims that using silicone as a base prevents the absorption of active ingredients.

Flawed study

There is one troubling aspect about the Fitzpatrick study.  The study did not test the use of each key ingredient separately.

The two key ingredients in the anhydrous C product are L-ascorbic acid (which is water soluble), and Ascorbyl Tetraisopalmitate (also known as Tetrahexyldecyl Ascorbate ) which is oil soluble.

So, even though the study shows that the combination the two active ingredients in a silicone base led to an increase of collagen, we do not know if this was caused by the Tetrahexyldecyl Ascorbate, the Vitamin C, or the combination of the two.

This brings us back full circle to the original problem! We do not know which active is responsible for the increase in collagen. So it is possible to claim that the L-ascorbic acid is in fact not absorbed by the skin, and that the increase of collagen is cause by the Tetrahexyldecyl Ascorbate.

The blame for this confusion can be put purely with Fitzpatrick. It seems a simple matter to have tested the activity of both l-ascorbic and Tetrahexyldecyl Ascorbate in anhydrous silicone, separately. However, he chose not to do this.

So, we remain with his original statement.

“Both of these are combined in an anhydrous polysilicone gel base, which acts as a ‘dermal patch,’ releasing the water soluble acid slowly and the lipid soluble analog rapidly.”

To me the dermal patch idea makes sense, and I personally put more trust in this than the doubt caused by a very few (but very ‘vocal’) posters on skin care forums.

In the end the choice is yours.

I will continue to use the anhydrous C product as my number one weapon in anti aging skin care.  Why? Because no matter which active did the job, somehow this product has improved my skin and that is ultimately what I want.

http://www.bulkactives.com/siliconegel.htm

http://www.bulkactives.com/ascorbicacid.htm

http://www.bulkactives.com/ascorbyltetraisopalmitate.htm

I sometimes get asked how L-ascorbic acid, also know as Vitamin C, ( CAS# 50-81-7) is made and, more often, what the source material is in the manufacturing and production of  l-ascorbic acid.

Here is the process, as I understand it.

First,  cornstarch is used to make Glucose.

Then, using a multi-step method called ‘The Reichstein process‘ , L-ascorbic acid is produced.

Short and sweet, L-ascorbic acid is made from corn.