A ray of hope for sunscreens? The Florida Chapter's Sunscreen Symposium takes place just days after the FDA issues its Final Monograph on sunscreens.

TALK ABOUT PERFECT TIMING! Little more than a week after the U.S. Food and Drug Administration issued its Final Monograph on sunscreens, the Florida Chapter of the Society of Cosmetic Chemists held its semi-annual Sunscreen Symposium in Orlando, FL. And while FDA officials declined an invitation to speak at the symposium, plenty of attendees had a thought or two about the long-awaited FM. The good news for industry is that FDA is accepting comments on the new rule until Nov. 26, 2007.

While the Final Monograph was the topic of much of the conversation among the nearly 400 attendees, keynote speaker Daniel Yarosh, president, AGI Dermatics, urged the audience to look beyond sunburn when formulating products and toward DNA repair and photoaging. Dr. Yarosh explained that while sunscreens were originally developed to prevent sunburn, over the years, consumers have come to expect them to stop photoaging, reduce suppression of the immune system and even eliminate skin cancers. All three of these maladies are the result of DNA damage, which itself is caused directly by absorbing light and indirectly by reactive oxygen species generated by UV.

Dr. Yarosh then explained how delivery of OGGI enzymes via liposomes can actually repair this damage to DNA.

"Using a DNA-repair lotion that contains DNA repair enzymes, we can repair skin by adding more enzymes," explained Dr. Yarosh.

His company has applied for a New Drug Application (NDA) for the material, which has already been found to be effective in hairless mice. He urged the audience to consider pairing his DNA repair material with sunscreens, noting that the former is ideal for improving skin in ways that are impossible with the latter. In fact, after four weeks of use the material produced a 41% decrease in pigment spots and 74% decrease in wrinkles among women in their thirties.

New Pathways to Protection

Creating effective sunscreens is one thing. Testing their efficacy is another. That was apparent following the presentation by Craig Bonda of Hallstar. In his opening remarks, he raised two questions to the audience:

* Why does oxybenzone partially stablize avobenzone?

* Why doesn't octocrylene stabilize avobenzone in the presence of octinoxate?

He suggested that a formula containing 5% OMC, 2% avobenzone and 7% ethylhexyl methoxycrylene is stable. Moreover, the formula has a UVA Protection Factor of 13.79--well above the 12 level required by the Monograph.

"This formula qualifies for a four-star rating for UVA protection," noted Mr. Bonda.

He warned, however, that the delivery vehicle plays a key role in product efficacy, which is one reason why Hallstar has developed a photostabilizing silicone fluid.

On the inorganic front, Dr. Yun Shao of Kobo Products explained how formulators can use titanium dioxide and zinc oxide for balanced UV protection. He noted that alone, titanium dioxide does not provide balanced UV protection. Similarly zinc oxide cannot provide balanced protection unless its use level is 25%.

"(Moreover) titanium dioxide is often too whitening and zinc oxide is not an effective UVB agent," he added. The solution, then, is to combine the two to provide SPF and PFA protection. But to create a formula that will meet European standards, formulators must shoot for a ratio of 3:1 of SPF/PFA. Kobo researchers developed just such a formula based on 6% titanium dioxide and 12% zinc oxide.

"By combining these materials, balanced UV protection with SPF 30 or higher can be achieved," he concluded.

Experimental Design

The new FDA regulations and the possibility of new sunscreen approvals could lead many companies to reformulate their products. Unfortunately, trying to optimize every component of the formulation is too costly and time consuming, since it would require an extremely large number of experiments.

But Julian P. Hewitt of Croda explained how experimental design and statistical modeling techniques can shorten the process and lead to a more optimized formulation. According to Mr. Hewitt, these techniques allow multiple variables to be studied in a relatively small number of experiments and generate a predictive model to indicate the optimum value of each variable. Experimental design calls for all variables to be changed at once, and from this chaos, the data are analyzed using Analysis of Variance (ANOVA).

"What you get is the prediction profile, which lets you explore the effects of each variable, in order to find the optimum values of each variable," he explained.

All of this leads to significant cost savings for the higher SPFs, compared to the "one variable at a time approach."

UV Filter Update

While formulators eagerly await the sunscreen final monograph, Nadim A. Shaath, president of Alpha Research, noted that while there are 55 UV filters approved for use around the world, the U.S. has only approved 17 and really only uses 11. In contrast, South Africa has approved 48 filters. For a detailed look at UV filters, read Dr. Shaath's article, "The Photostability of Ultraviolet Filters," which starts on p. 77 in this issue.

Roundtable Discussion

The first day of the Sunscreen Symposium concluded with a roundtable discussion of key issues that was moderated by David Steinberg, Steinberg Associates. Panelists included: Gavin Greenoak, University of Sydney; Dennis Lott, Tanning Research Labs; Craig Weiss, Consumer Product Testing Co.; Mr. Bonda, Hallstar; Chris Vaughn, SPF Consulting; Dr. Shaath, Alpha Research and Mr. Hewitt, Croda.

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Each took turns answering questions on the efficacy of sunscreens, waterproofing, application, claim regulation and UVA testing. Mr. Greenoak, for instance, noted that the UV spectrum provides a symphony of light and therefore protection should be directed at the entire spectrum and not just a single note.

While some groups have questioned the efficacy of sun care products, all the panelists agreed that sunscreen must be applied correctly and frequently in order to provide the proper level of protection. But Mr. Steinberg warned that UV damage will never be reduced as long as pop culture equates beauty with a tan.

"The incidence of sunburn won't go down until Hollywood backs off," insisted Mr. Steinberg. "We need an education program like Australia's 'Slip-Slap-Slop' campaign."

Investigating Ingredients

Day 2 of the Sunscreen Symposium was moderated by Gary Agisim of Wyeth Consumer Healthcare. Helena Gonzalez, a dermatologist based in Finland, provided insight into the percutaneous absorption of benzophenone-3 and the photostability of sunscreens. She noted that previous studies have shown that 0.5-2% benzophenone-3 (BZ-3) is excreted in the urine after topical application. In her study, which also measured the amount excreted of the major metabolite, 2,4-dihydroxybenzophenone (DHB), 25 subjects applied a commercially-available sunscreen containing 4% BZ-3 morning and night for five days.

According to Dr. Gonzalez, the mean value of excreted BZ-3 was 3.7%. BZ-3 and DHB were extensively conjugated and only a smaller part was excreted in the non-conjugated form, mean value 5.9% and 8.8%, respectively. Armed with these results, she cautioned formulators not to incorporate benzophenone-3 in products intended for children under 2 years of age.

During her presentation, Dr. Gonzalez took time out to ridicule the amount of sunscreen that the industry uses to test its products: 2mg/[cm.sup.2].

"All of our volunteers thought that was too much," she told the audience. "Nobody uses that amount, it's ridiculous!"

Patricia Alkens, BASF, reported on the anti-inflammatory, anti-photoaging and anti-oxidative effects of UVA filters. The study involved three active combinations:

* Ethylhexyl triazone (EHT), a UVB block;

* Diethylamino hydroxybenzoyl hexyl benzoate (DHHB) and EHT; and

* Zinc oxide and UHT.

Three biomarkers were studied: Matrix metalloproteinase (MMP-1), Heme oxygenase-1 (HO-1) and ICAM-1, an intercellular adhesion molecule.

According to Dr. Aikens, the presence of the two UVA filters in the formula reduced the specific m-RNA biomarkers compared to the UVB-only formula.

Christine Mendrok-Edinger, DSM Nutritional Products Ltd., provided conference attendees with test results that will enable formulators to choose the correct TiO2, when formulating products. The tests include:

* Catalytic activity in the presence of ascorbyl palmitate;

* Photostability under exposure of daylight;

* Photo reactivity in the presence of isopropanol;

* Compatibility with polyacrylic acid thickeners; and

* Compatibility with butyl methoxydibenzoyl methane.

Ms. Mendrok-Edinger noted that there are many types of TiO2, based on particle size, crystal structure and coating. She pointed out that rutile is good for UV and recommended that it be coated in silica, A1203 and stearic acid, before a final coating of dimethicone and simethicone.

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Coating is critical to the efficacy of the TiO2, she noted, as a perfect coating prevents photodegradation of the TiO2. Furthermore, a comprehensive coating dramatically reduces the risk of photoreactivity.

Diane Bilodeau, Atrium Biotechnologies, explained how biomimetic peptides derived from proopiomelanocortin (PMC) may be used to modulate neurogenic inflammation in the skin. A specific peptide, RE-053 (palmitoyl4tripeptide-3), reduced IL-8 production and had a soothing effect on skin.

A Look at Patents

Intellectual property is considered one of the most important weapons in today's highly competitive environment. Louis C. Paul, a principal with Cosmetics Intellectual Property Group, LLC, explained what's patentable and what's not. He noted that all patents must have three elements: useful, novel and not obvious.

New ingredients and new combinations of ingredients are both patentable, such as L'Oreal's avobenzone and octocrylene and ScheringPlough's avobenzone, zinc oxide and ensulizole. But Mr. Paul reminded the audience that patent protection is extended to the party that is first to invent, not patent. While many consider patents as a way companies try to dominate a sector, Mr. Paul suggested that there is a win-win scenario when the marketer patents the combination and the supplier patents the raw material.

The Impact of REACH

These days, no conference would be complete without a presentation on REACH, that far-reaching EU regulation that threatens to change the way cosmetic formulators create new products. But David Steinberg, Steinberg Associates, wasn't all doom and gloom during his presentation. He urged companies to pre-register their products as the process could buy them as much as 10 years in the entire registration process. Also, he doesn't expect extracts to feel the effects of REACH since so many of them fall below the one-ton limit. Taking a closer look at sunscreens, Mr. Steinberg said he expects most filters will be safe--of course, they'll cost more, but will remain on the market. Most interestingly, Mr. Steinberg said REACH might actually implode due to the overwhelming amount of work involved. Like so many other government agencies, the REACH staff is overextended, he noted. And when all pre-registrations show up at the pre-registration deadline (November 2008), regulators will be overwhelmed.

Tom Branna

Editorial Director