Friday, September 14, 2012

Vitamin C: Derivatives and Anti Aging

DIY Vitamin C or pay exorbitant amounts for something which you can quite easily make yourself and treat your entire body to the benefits of a C serum? The Anti Aging arena is awash with "new" materials and profound promises to erase those fine lines, boost that collagen production and massage your stem cells into action.

 Lancome is promising : "Boosts the activity of genes and stimulates the production of youth proteins," and "A powerful combination of unique ingredients—Reconstruction Complex and Pro-Xylane™, a patented scientific innovation—has been shown to improve the condition around the stem cells and stimulate cell regeneration to reconstruct skin to a denser quality."

FDA said "Your products are not generally recognized among qualified experts as safe and effective for the above referenced uses and, therefore, the products are new drugs." The agency went on to say its letter is not exhaustive of all the violations associated with the company's products.

Sending Out An SOS: FDA's Warning Letter to Lancome
Alissa Marrapodi Copyright 2012 by Virgo Publishing.
http://cosmetics.supplysideinsights.com/

The "patented scientific innovation" without a shred of evidence to be found anywhere. There is no Fountain of Youth in a Cheap Plastic Bottle, but marketing would have us believe otherwise. Are there effective anti aging ingredients? Yes, however, one must check one's expectations against reality. There is not a cream/ serum on the market that is going to make a 60 year old look like s /he's 20. There is no subsititute for a life time of  regular exercise, healthy diet and the use of an effective SPF. Supplements, antioxidants, well formulated creams cannot change the chronological age, but minimum, one doesn't have to look it. There are always choices and thereby one can make a significant difference in the final outcome.

Due to the Baby boomers ongoing quest for effective products that may actually meet the claims, countless products are swamping the market. Endless types of treatments are made available, promoted via websites and beauty blogs. Invasive and potentially harmful treatements, Laser to botox,  you name it. Topical treatments, repleat with Apple stem cell extract, and if that wasn't bad enough, the latest, Green Tea Stem Cell extract. Let's not forget Lancome's foray into botanical stem cell science with the Absolue hilarity of Rose Stem cell extract. All of which are bunk. Let's not discuss the price for that either.

Vitamin C serums are almost synonymous with Anti aging. Where you see anti aging as a focus of skin care, invariably, Vitamin C or its derivatives come up  in discussion. That Vitamin C is an extremely useful active in skin care is proven. It is an effective anti oxidant, up regulates collagen synthesis, exfoliates and is a mild lightening agent. L ascorbic acid is an inexpensive ingredient and very easy to source. The question then becomes, why are cosmetic companies selling this extremely useful and cheap ingredient for over $100.00 for 30 ml? Relatively simple answer, it works and most people are unaware of the multiples in the profit margin. The main problem with LAA, is that due to its excellent  antioxidative effect in the skin, it oxidizes quite readily. It is fundamentally unstable. The effective use is limited by the pH requirement, generally under 3.2- 3.5. That low pH is problematic for many. Over time it may cause irritation and flaky skin due to over exfoliation. Not quite the "glowy" look one is going for. 

To better deal with the short shelf of LAA and irritation due to pH, several vitamin C derivatives have been developed. They are not LAA, however when applied to the skin and through enzymatic processess, ascorbic acid is released. Unfortunately not all Vitamin C derivatives are created equal, nor do they share the same capacity for positive dermal/ cosmetic effect.

MAP, VC-PMG, Magnesium Ascorbyl Phosphate is the more gentle version of Vitamin C. pH is closer to neutral and requires 7.2 in solution/ serum / cream at higher use levels to avoid hydrolyzing and giving off a potent stench. MAP was shown in clinical trial to have the same capacity as LAA with respect to collagen up regulation. This makes it quite a good substitute for LAA if that is the focus of the end user. As a lightening agent, is not as effective as LAA, however LAA is not particularly effective to begin with. It's been incorrectly labled as a tyrosinase inhibitor by some, it is not, it acts to  to reduce  o-dopaquinone to dopa, avoiding dopachrome and melanin formation. Quite different mechanism. MAP has also been shown to improve moisture content in the skin, where as LAA did not. One study suggests that MAP at 10% was useful for treatment of  melasma.

Tetra C, ATIP, VC-IP, Ascorbyl Tetra-Isopalmitate, Tetrahexadecyl Ascorbate. A lipophillic Vitamin C derivative. The majority of the data behind the use of Tetra C comes from the makers of the derivative. Another study promoting its use had 7% LAA in the vehicle from which they drew astoundingly glowing conclusions regarding its efficacy. To be fair, in other research it was shown to be more effective at protecting from UVA induced oxidative stress than LAA.  One may hypothesize that it may be due to the depot effect in the skin and the slow release. Whether that is the case invivo is not clear.

As far as antioxidative effect, LAA is more effective than either. MAP is more effective than TetraC in a water based formula, however that reverses in favor of TetraC in an oil base.

Ascorbyl Acid 2 Glucoside stacks up quite nicely next to MAP, if not better for it's ease of formulation and stability but also for it's effect on collagen synthesis. Slow release is also part of the stated mechanism for it's effect. Ascorbic Acid 2-glucoside has been shown to maintain prolonged biological activity of ascorbic acid longer than  SAP [sodium L-ascorbic acid 2-phosphate], another conventional ascorbic acid derivative .

SAP, Asc 2-P, Sodium Ascorbyl Phosphate, this one doesn't stack up too well. It's sold as being equal to MAP, but it is 1/10 as effective as MAP or LAA at its ability to stimulate collagen synthesis. It is stable by comparison to LAA. Non irritating, and  not particularly effective at increasing collagen synthesis when compare to MAP or LAA.

AP, Ascorbyl Palmitate,  ascorbic acid-6-palmitate , is unfortunately not the solution to the problem either. It may be stable, however when applied to the skin and exposed to UVB, which occurs every day, AP was found to strongly promote ultraviolet-B-induced lipid peroxidation, c-Jun N-terminal kinase activation, and cytotoxicity. Not a good choice as, despite the selling point being that it is lipid soluble, it is  the lipid component of ascorbic acid-6-palmitate that contributes to the generation of oxidized lipid metabolites that are toxic to epidermal cells.The data suggested that, despite its antioxidant properties, ascorbic acid-6-palmitate may intensify skin damage following physiologic doses of ultraviolet radiation. It may be convenient to work with, however it is certainly not worth using.



Clearly there are differences in the concept of what consititutes an effective choice even for a simple C serum. Who wants to waste their time or money on the wrong ingredients? Wrinkles don't 'go away' with wishful thinking. Defying the hands of time requires proven modalities. Fighting the effects of aging , cumulative sun damage, years of free radicals, it helps to choose the correct products. Whether one is looking to prevent or to reverse the signs of aging, a Vitamin C serum is a good place to start. It's something anyone is able to DIY and incorporate into their current skin care system. Beautiful skin is not a brand, it's not a right either, it's something one must work at to maintain.

Due to the marketing stories and the plethora of new ingredients, it can be very confusing for the vast majority. Is SAP better than MAP? No. Is Tetra C better than MAP? No. Is LAA better than MAP? No, but if your skin can not tolerate LAA, than the answer is Yes. Same answer for Tetra C, but personally, I wouldn't bother as the data on AA2G is more compelling.  Which is the most effective lightener? None of them. There are other actives that are more effective. Used in conjunction, it won't hurt and may help. When it comes to purchasing  skin care, it's  caveat emptor. When it comes to DIYing it, you increase the odds several fold.

Long story short with regards to the efficacy of the C derivatives.
LAA  ≥MAP  ≥ AA2G> TetracC >SAP>; AP 

If one is hoping to remove wrinkles, that most probably isn't going to happen. Reduction in fine lines, is a reasonable possibility. Damaged skin took many years to accumulate. To suggest that any topical product is going to undo years of damage is more than a leap of faith. It is an out right lie. Marketing takes no prisoners. There are many useful functional ingredients available. They are the boring, non patented type without the fanfare, but have a great deal in the way of solid clinical trials to suggest that their use may be of some benefit. Each is responsible for their choices in skin care whether to DIY or purchase. Hopefully over time, the average baby boomer skin care consumer will take the initiative to become more selective and demanding of the products they purchase.

1.Campos PM, Gon├žalves GM, Gaspar LR. In vitro antioxidant activity and in vivo efficacy of topical formulations containing vitamin C and its derivatives studied by non-invasive methods.Skin Res Technol. 2008 Aug;14(3):376-80.
2. Hitoshi Mitsuzumi. Properties of a Novel Vitamin C Supplement, L-Ascorbic Acid 2-Glucoside, and Its Uses in the Field of Foods. Foods Food Ingredients J. Jpn., Vol. 211, No.5, 2006
3. 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. J. Am. Acad. Dermatol. 1996, 34, 29-33.
4. Kumano, Y.; Sakamoto, T.; Egawa, M.; Iwai, I.; Tanaka, M.; Yamamoto, I. In vitro and in vivo prolonged biological activities of novel vitamin C derivative, 2-O- -D-glucopyranosyl-L-ascorbic acid (AA-2G), in cosmetic fields. J. Nutr. Sci. Vitaminol. 1998, 44, 345-359.
5. Kunikazu Moribe,Waree Limwikrant, Kenjirou Higashi, and Keiji Yamamoto. Drug Nanoparticle Formulation Using Ascorbic Acid Derivatives. Journal of Drug Delivery Volume 2011, Article ID 138929, 9 pages
6. Lee SC, Yuk HG, Lee DH, Lee KE, Hwang YI, Ludescher RD.Vitamin C derivative ascorbyl palmitate promotes ultraviolet-B-induced lipid peroxidation and cytotoxicity in keratinocytes.J Invest Dermatol. 2002 Nov;119(5):1103-8.
7. Miyai E.; Yanagida M. ; Akiyama J.-I. ; Yamamoto I. ; Ascorbic acid 2-O-╬▒-glucoside-induced redox modulation in human keratinocyte cell line, SCC : Mechanisms of photoprotective effect against ultraviolet light B. Biological & pharmaceutical bulletin ,1997, vol. 20, no6, pp. 632-636 (36 ref.)
8. 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. J Cell Biochem. 2009 Mar 1;106(4):589-98.