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MoisturisingLotion

Vitamin E

The deleterious effects of sun exposure relating to erythema and freeradical 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 anecessity 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 promotemoisture 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.

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

Anti-inflammatory skin creamwith Vitamin E Phosphate

AfterBefore

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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

lowdensity 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 efficacyprofile. 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 phosphorylatingagent. 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 LtdP.O. Box 802 Castle Hill, NSW 1765 Australiawww.neutriderm.com.au AUS TRALI ANMADE & OWNED

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

Disodium Lauriminodipropionate Tocopheryl Phosphates:

Potent New Anti-Inflammatory