Anti-inflammatory skin cream with Vitamin E Phosphate

Otto Mills, PhD, Robert Wood Johnson Medical School, Doylestown, PA, United States; Robert Verdicchio, PhD, Verdi Enterprises, Succasunna, NJ, United States; Journal of American Academy of Dermatology. March 2005 (Vol. 52, Issue 3, Suppliment, Page P-85)

The deleterious effects of sun exposure relating to erythema and free radical induced aging are well documented. Moreover, recent studies have shown that brief exposure to UV rays during normal everyday routine activities can be cumulative and produce the above effects over time. Similarly, the overuse of cosmetics can cause sub clinical erythema, which can also be cumulative. The daily use of products that inhibit the above deleterious skin effects is needed for moisture balance, to mitigate free radical-induced premature skin aging, and to promote youthful healthy skin is a necessity for most all skin types. A cream containing 3% wt/wt vitamin E phosphate (disodium lauriminodipropionate tocopheryl phosphates), a new potent form of vitamin E, can readily be used to prevent erythema and restore skin as a before and after sun exposure product. For optimal coverage the formulation contains the above in a light elegant cosmetic base with INCI-registered esters to promote moisture balance and emolliency. In addition, the cream reduces redness due to acne. Skin studies have shown that in this base the vitamin E phosphate exhibits excellent distribution into the skin compared with an equivalent amount of vitamin E acetate. Clinical studies have shown that vitamin E phosphate at levels of 1% to 3% active is a more effective anti-inflammatory compared with aloe, vitamin E acetate, and a topical steroid. The results of a human repeat insult patch test (HRIPT) on humans show no cumulative irritation and/or sensitization, and the cream is well tolerated for frequent daily use on skin.

Vitamin E
Moisturising Lotion
Before After

Disodium Lauriminodipropionate Tocopheryl Phosphates: Potent New Anti-Inflammatory

By: Mark E. Rerek, International Speciality Products; Otto H. Mills, Robert Wood Johnson Medical School; Robert Verdicchio and Simon West, Vital Personal Care Specialties

The beneficial use of vitamins in general & specifically vitamin E, continues to be an active area in dermatology & cosmetic science. It is clear that vitamin E, especially in the form of -tocopherol, is a potent antioxidant and is widely used by the body to protect lipids in cell membranes from oxidative damage. However, the role of vitamin E in skin is much less clear, both in the understanding of its intrinsic role as well as clearly demonstrating its clinically relevant, in vivo benefits. -Tocopherol is stored in the liver & adipose tissue. In the liver it is bound and transferred by a specific cytosolic protein, -tocopherol transfer protein (?TTP). When circulated through plasma, tocopherol is transported by several forms of lipoproteins including very low density lipoproteins (VLDL) & high density lipoproteins (HDL). It is believed that most -tocopherol is delivered through HDLs to cells for use in the membrane or within the cell. It is not unreasonable to assume that when delivered topically, - tocopherol needs to associate with a transport protein to gain access to the dermis, especially the fibroblasts, unless some other delivery vehicle is provided in the formulation. Another significant formulation challenge is to keep tocopherol stable until use. The most common approach is to use the ester -tocopherol acetate. Although the ester is more stable than -tocopherol, it has a different efficacy profile. For instance, it has been shown that -TTP binds tocopherol to an extent more than 50 times greater than tocopherol acetate. A second approach to vitamin and drug stabilization is phosphorylation. Phosphorylation is the transformation of an alcohol to a phosphate ester through transfer of a phosphoryl group (-PO3H2). Adenosine triphosphate (ATP) is the most common endogenous phosphorylating agent. It has been shown that phosphorylated vitamin C is accumulated into cells as vitamin C. Work in our laboratories has begun to develop evidence for the presence of phosphorylated - tocopherol in the human body. For this reason, we believe that phosphorylation is a better route to formulation stabilization & that it allows a better opportunity for in vivo efficacy through an endogenous form that can be activated by phosphate ester cleavage.
UAS Pharmaceuticals Pty Ltd P.O. Box 802 Castle Hill, NSW 1765 Australia www.neutriderm.com.au

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