ASCORBYL TETRAISOPALMITATE - Vitamin C Derivative

Posted by Add Actives 21/05/2016 0 Comment(s) Know your actives,

 

Ascorbyl Tetraisopalmitate is stabilized (heat and oxygen stable), non acidic, oil soluble vitamin C derivative of Ascorbic and Isopalmitic Acid. It effectively converts into the free vitamin C in the skin.
Ascorbyl Tetraisopalmitate is known for its superior percutaneous absorption.
It’s an antioxidant with SOD (superoxide dismutase)-like activity, protects collagen from degradation, and also promotes its synthesis (anti-aging).
It’s one of the best ingredients to add to your skincare arsenal when treating hyperpigmentation, and skin changes associated with photoaging.
Ascorbyl Tetraisopalmitate is approved as a quasi-drug active in Japan at 3%. It is also registered in Korea as a functional ingredient for skin lightening at 2% concentration.
 

Why Ascorbyl Tetraisopalmitate? What About Pure Ascorbic Acid?

The skincare benefits of vitamin C are well-researched and well-known (1). But, there are a few problems with the use of pure vitamin C aka Ascorbic Acid: 

  • Vitamin C is an unstable molecule, undergoes rapid oxidation, and almost half of it gets degraded within 30 minutes (1) (2) (29). It can be stabilized to some degree by keeping it at low pH (below 3,5), and by adding other antioxidants to the formula (Vitamin E, Ferulic acid). 

  • When taken orally or applied to the skin, most of the vitamin C never makes it to the target site, that is, to the target body cells. Also, it is difficult to deliver Ascorbic Acid into the dermis in the optimum dosage (3). 

  • Ascorbic Acid requires low pH (acidic) environment to be able to penetrate the skin, and can cause peeling, stinging, irritation, and dryness of the skin.


Ascorbyl Tetraisopalmitate - A More Potent and Stable Vitamin C Derivative 

Despite its obvious benefits, the utility of vitamin C is limited. Therefore, researchers have come up with vitamin C derivatives that are more stable, more effective, and far more potent. One such derivative is Ascorbyl Tetraisopalmitate.
When compared to pure vitamin C (Ascorbic Acid), vitamin C derivatives are:

  • More stable, both in solution and topical forms (5) (29). 

  • Ascorbyl Tetraisopalmitate has three times better penetration than ascorbic acid (6) (7) (29). 

  • Ascorbyl Tetraisopalmitate is able to produce better results even when used in doses 25 times lower than ascorbic acid (6) (7). 


SKINCARE BENEFITS OF ASCORBYL TETRAISOPALMITATE

What benefits should you expect following the use of Ascorbyl Tetraisopalmitate? Here are some beauty benefits of this vitamin C derivative:

  1. It is a potent antioxidant and inhibits the peroxidation of lipids (8).

  2. It has anti-aging benefits (9). 

  3. Protects the skin against UV (Ultraviolet) radiations (10). 

  4. Improves skin brightening by reducing skin melanin production (10). 

  5. Gives your skin a youthful look by improving collagen production (11) and decreasing collagen breakdown (12). 
     

1.    Antioxidant Benefits of Ascorbyl Tetraisopalmitate

Your skin is the biggest yet the most sensitive organ of your body. The reactive oxygen species or ROS start to build up in your body as you age. The oxidative stress also increases with the exposure to environmental pollutants and UV radiations (13). Among other body organs, your skin has the highest load of ROS (14). 
An increase in oxidative stress wreaks havoc on your skin health. It increases melanin production, hinders the synthesis of collagen, and speeds up the breakdown of already present collagen. As a result, you have a skin full of wrinkles, age spots, and uneven pigmentation (15). 
Ascorbate and its derivate molecules are known to act at a cellular level to quench the ROS (16). When compared to simple Ascorbic Acid, Ascorbyl Tetraisopalmitate was able to exert free-radical scavenging effects for a longer duration (up to 40 hours). Ascorbic acid, on the other hand, caused maximum free radical elimination within 30 minutes and not after that (17). 

2.    Anti-Aging Properties of Ascorbyl Tetraisopalmitate

The signs of aging include wrinkles, uneven skin tone, roughness of the skin, and reduced skin brightness. The underlying mechanisms for skin aging include reduced collagen production, higher photo-damage, and a decline in skin hydration. These can be the result of poor nutrition, overexposure to the sun, environmental pollutants, and improper hydration (18). 
Ascorbic Acid and its derivatives help improve skin appearance and exert anti-aging benefits due to their ability to improve cell survival, skin hydration, and collagen synthesis (19) (20).
When treated with hydrogen peroxide (a chemical toxic to cells), the survival rate of cells subsequently treated with Ascorbyl Tetraisopalmitate was 100% compared to control (where the survival was less than 80%) (17). 
In a double-blinded, randomized control trial, researchers evaluated the efficacy of Ascorbyl Tetraisopalmitate based products in improving signs of aging. At the end of 12 weeks, almost all the participants noted a significant reduction in wrinkles, uneven skin tone, and experienced improved skin hydration and better skin complexion (21). 

3.    UV Protection Offered By Ascorbyl Tetraisopalmitate


Exposure to UV radiations - either natural or due to tanning- can result in a number of skin complications. UV exposure increases inflammation in the superficial layers of your skin (epidermis and dermis). It damages the very core (DNA) of the skin keratinocytes (skin cells) and makes them die out quickly following a process called apoptosis. Moreover, UV rays increase your skin thickness and increase skin melanin production as well. What you are left with is a skin that is thick, coarse, full of wrinkles, and hyper-pigmented (22). 
Ascorbyl Tetraisopalmitate achieves an excellent penetration within the skin keratinocytes and helps them fight against the harmful effects of UV radiation. Cells treated with Ascorbyl Tetraisopalmitate have a 30% better survival rate compared to pure vitamin C.
p53 is a cellular protein that makes your body cells commit suicide (apoptosis). When treated with Ascorbyl Tetraisopalmitate, the UV-exposed cells have a less than 20% expression of p53 compared to control (17). 

4.     Ascorbyl Tetraisopalmitate Inhibits Melanogenesis 

Your skin contains a variety of cells and one of them is melanocytes. Melanocytes produce a skin pigment called melanin. Melanin is a black-colored pigment that saves your skin from the UV damage (23). But a lot of this pigment can result in a dark skin complexion and uneven skin tone. 
The production of melanin is a multi-stage process and is facilitated by a number of enzymes. Most of the whitening skin ingredients have a melanin lowering effect mainly due to their ability to reduce the activity of tyrosinase- an enzyme critical for melanin synthesis. Ascorbic acid has no tyrosinase inhibiting activity. Instead, it reduces melanin production by strengthening the intrinsic anti-oxidant mechanisms of the body which offer protection against melanin production secondary to UV exposure (24).
But the problem with usual vitamin C preparations is that they have a weak melanogenesis suppressing effect (25). In comparison, the results of laboratory testing have shown that treatment of skin cells with Ascorbyl Tetraisopalmitate can reduce melanogenesis by 80% (17). 
This fact has been backed by a number of clinical studies as well where the use of Ascorbyl Tetraisopalmitate based products resulted in significant skin brightening and a reduction in melanogenesis (7) (9) (10) (26) (27). 

5.    Ascorbyl Tetraisopalmitate Boosts Skin Collagen

Collagen is one of the most important proteins in your skin. It is responsible for maintaining the basic skin architecture and gives the skin a supple and youthful look. With age and due to the exposure to environmental toxins and pollutants, your skin starts to lose its collagen reserves. One of the several culprits for increased collagen breakdown is Matrix Metalloproteinase (MMP). This enzyme causes a rapid breakdown of skin collagen (28). 
Treatment of skin cells with ascorbate-based products can cause up to 8-folds increase in collagen synthesis (11). When compared to simple ascorbic acid, Ascorbyl Tetraisopalmitate caused a 50% increase in the skin collagen synthesis. Moreover, it also causes a substantial decline in the activity of collagen-degrading enzymes (17). 

To conclude, Ascorbyl Tetraisopalmitate is a potent anti-aging, antioxidant, melanin suppressing, and collagen boosting skincare ingredient with an impressive safety profile. It is more effective, safe, and potent than the usual vitamin C preparations. 


References:
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3.    Duconge J et al. Pharmacokinetics of vitamin C: insights into the oral and intravenous administration of ascorbate.P R Health Sci J. 2008 Mar;27(1):7-19.
4.    Karin Ried et al. The acute effect of high-dose intravenous vitamin C and other nutrients on blood pressure: a cohort study. Blood Press Monit. 2016 Jun; 21(3): 160–167.
5.    R. Austria et al. Stability of vitamin C derivatives in solution and topical formulations. Volume 15, Issue 6, March 1997, Pages 795-801
6.    Barnet Products Corp. Stable forms of vitamin C. Technical bulletin. Englewood Cliffs, NJ: Barnet Products Corp., 2001
7.    Fitzpatrick RE, Rostan EF. Double-blind, half-face study comparing topical vitamin C and vehicle for rejuvenation of photodamage. Dermatol Surg. 2002;28:231–236. 
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25.    Lee SA et al. Ascorbic acid increases the activity and synthesis of tyrosinase in B16F10 cells through activation of p38 mitogen-activated protein kinase. Arch Dermatol Res. 2011 Nov;303(9):669-78
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