A Youthful Pursuit with Antioxidants

There’s a hunger within our society to stay young and beautiful. Many pursue eternal youth through exercise, healthy eating and the use of premium anti-aging beauty products. But in a rather contradictory fashion, some of the same consumers are willing to endure cosmetic procedures that involve injections and going under the knife for the sake of physical beauty. The quest to stay forever young has become so prevalent, even teenagers have adopted the obsession for taut skin and a radiant glow by using anti-aging products.

Cosmeceuticals have paved a way for those wanting to grow old gracefully (and naturally) by tapping into antioxidants, nature’s answer to the fountain of youth. Cosmeceuticals, as defined by Datamonitor, are personal care products containing at least one bio-active ingredient that not only enhances appearance, but also has a positive physiological effect at the cellular level. At the recent SupplySide West show, Julia McNamara, vice president consumer markets consulting, Datamonitor, discussed the trend toward antioxidant use for addressing specific conditions and body parts. She noted in a recent survey, 56.1 percent of consumers said solving specific beauty problems was their main reason for using cosmeceuticals.

Antioxidants have become the darlings for some of the most innovative and newest cosmeceutical products hitting store shelves, delivering results on specific conditions and concerns, and making a profitable dent in the personal care market.

According to Packaged Facts, a market research firm, new products making antioxidant claims escalated at a compound annual growth rate of 306 percent between 2002 and 2006. In its report “Antioxidants: Nature Meets Science for Anti-Aging Solutions,” the firm projected the retail cosmeceuticals market will be valued at more than $17.2 billion by 2010, reflecting a five-year gain of 29.4 percent, or $3.9 billion.

Adding an antioxidant into a cosmetic formula and marketing it to the masses is neither easy nor simple. Manufacturers are finding adding these cosmeceutical ingredients comes with behind-the-scenes research and ingredient evaluations, formulation obstacles and challenges, as well as the need to educate both themselves and the consumer.

A RADICAL CONCEPT

Antioxidants have a higher purpose in maintaining healthy, youthful skin. In order to comprehend how this relationship works, one begins at the atomic level, finitely combing and dissecting trillions of cells that compose the human body.

Cells are made of various types of molecules, which contain one or more atoms and elements. One of the most important features of an atom is its ability to determine the molecule’s chemical behavior based the number of electrons in its outer shell. An atom that has a full outer shell does not have chemical reactions; atoms are constantly seeking a state of stability by filling their outer shells by either gaining or losing electrons; or sharing electrons with other atoms, thus binding them together for maximum stability of the molecule. A shared atoms’ bond normally doesn’t break in a way that leaves a molecule with an odd, unpaired atom; however, a weak bond may split, creating free radicals, unstable compounds looking to capture the needed electron to gain stability. A free radical may steal an electron from the nearest stable molecule, which makes this attacked molecule unstable and a free radical. This cascading effect ultimately results in the disruption of a living cell.

A molecule can also relinquish one of its electrons, creating free radical damage, to another oxygen molecule such as carbon monoxide, hydrogen peroxide and superoxide, as well as ultraviolet (UV) radiation, cigarette smoke, ozone and other pollutants. These molecules are regarded as reactive oxygen species (ROS) and can cause even more damage. “An excess of ROS, e.g. induced by the exposure to solar UV-irradiation, can lead to a depletion of antioxidants in the skin resulting in premature cutaneous aging, carcinogenesis and hyper pigmentation,” noted Ulrich Issberner, M.D., senior marketing manager, personal care, Cognis Corp.

According to skin experts, free radical damage causes deterioration of the skin’s support structures, decreasing elasticity and resilience—in other words, all aspects of aging are caused by free radical damage taking place on the skin. Additionally, free radical damage activates an enzyme called metalloproteinase, which breaks down collagen—one of the major causes of wrinkles, added Ellen Kamhi, Ph.D., R.N., The Natural Nurse. ROS’s are now believed by most medical researchers to be the culprits behind acne, wrinkles, skin sagging, dryness, cellulite, tanning, age spots and skin cancer. In short, inflammation is the basis for the redness and swelling of sunburn, and “is the bottom line of aging,” noted Rebecca James Gadberry, president, YG Laboratories.

The connection between inflammation and many antioxidants is closely linked, according to growing research showing topically applied antioxidants can help protect against sun damage. Studies have shown a combination of antioxidants and sunscreen provide increased protection. When used in conjunction with sunscreen, vitamins C and E were found to offer photoprotective effects; vitamin E showing a boost in UVB protection and vitamin C offering stronger protection against UVA radiation (J Amer Acad Dermatol. 2003; 48:866-74). Vitamin A has also been shown to have photoprotective effects on radiation (J Invest Dermatol. 2003; 121:1163-7).

COSMECEUTICAL DARLIN’S

While the term antioxidant applies to molecules reacting with oxygen or protecting molecules from free radicals, it also defines an enzyme or other organic molecule that counteracts the damaging effects of oxygen in tissues or other substances prone to oxidation. Antioxidants work by intervening in the chain-reaction, electron theft process by grabbing the unstable molecule and nullifying it, thereby slowing or inhibiting the problematic free radical progression. Mark Sysler, vice president of sales, Bio-Botanica, added that in addition to inhibiting free radical production, antioxidants also provide cellular and DNA protection from UV damage. “The environment can severely damage our skin by oxidizing and deteriorating our cells, in the form of free radicals. Antioxidants fight free radicals and prevent much of this damage,” he said.

Additionally, antioxidants play a role in detoxifying and repairing cell constituents, connective fibers and the lipid barrier of the skin. “For [repairing] the lipid barrier, fat-soluble antioxidants are required: vitamin E and the carotenoids especially,” said Frank Schonlau, Ph.D., director of scientific communication, Horphag Research. “These are crucial when skin is exposed to sunlight as this leads to enormous oxidative stress, which may lead to death of skin cells, which subsequently triggers inflammation (sunburn).”

Antioxidants include ingredients such as vitamins A, C and E; superoxide dismutase (SOD); beta-carotene; glutathione; and the minerals selenium and zinc, which act as co-factors for endogenous antioxidant activity. Many plant-sourced antioxidants can be categorized as carotenoids or flavonoids. Carotenoids offer protection for the fat-containing skin layers. Carotenoids also enhance the activity of other fat-soluble antioxidants, such as vitamins A and E and coenzyme Q10 (CoQ10). Some of the best-known carotenoids are lycopene, beta-carotene and lutein.

Flavonoids are water-soluble compounds—such as the bioflavonoids in Pycnogenol® French maritime pine bark extract, epigallocatechin (EGC) from green tea, and polyphenols, the chemical substances found in plants characterized by the presence of more than one phenol per molecule, which can offer significant antioxidant action. Additionally, “polyphenols are subdivided into hydrolysable tannins, which are gallic acid esters of glucose and other sugars; and phenylpropanoids, such as lignins, flavonoids and condensed tannins,” Issberner noted.

Antioxidants can be separated into two categories: direct antioxidants and indirect antioxidants. Direct antioxidants, such as vitamins C and E and beta-carotene, eliminate ROS by neutralizing the unstable molecules; indirect antioxidants, such as various minerals and their derivatives—manganese, copper, zinc, selenium, an extract of malachite (Malakite) and oligominerals, act to increase the overall antioxidant capacity of cells, Gadberry noted. “The benefit of indirect antioxidants persists long after they have left the body because they serve to boost the sophisticated, natural antioxidant defense system,” she added. Additionally, they promote the production of a variety of protective enzymes, including superoxide dismutase, catalase and glutathione peroxidase, which provides greater protection against more types of damage compared with the action of a single, direct antioxidant.

“Antioxidants are useful active ingredients for cosmetics,” said Sysler, noting a dual benefit for the consumer and the product itself. “They prevent degradation of the natural ingredients in a cosmetic product (lipids, proteins and sugars); and they also protect skin cells from being damaged and help to slow down the aging process.”

THE GREATER CHALLENGE

While antioxidants may have positive effects on skin, there are challenges to getting these benefits delivered effectively and to the right location. Antioxidants are much like a double-sided coin—on one side, some are fragile and must be stabilized in formulations due to their self-reducing activity; on the other side, they are key ingredients in preventing product deterioration by inhibiting lipid peroxidation that leads to rancidity. “Antioxidants are added to preserve the integrity of formulations,” said Lakshimi Prakash, Ph.D., Sabinsa Corp. “Although synthetic antioxidants are conventionally used as preservatives, natural actives are used for functionality in protecting the skin.”

In the skin, many antioxidants have been found to soothe irritation, control sensitivity, firm skin, reduce signs of wrinkles, lighten age spots or uneven pigmentation, moisturize and soften rough skin, fight signs of acne, and smooth signs of cellulite. But not just one antioxidant delivers these wonders; instead, a combination of antioxidants may offer a handful of benefits.

Manufacturers are asked to use more natural ingredients and make the products without synthetic preservatives. This is a challenge many formulators are facing, in addition to obtaining proper and stable natural extracts in mediums that work with the formulation. In fact, adding antioxidants to a product line can mean a complete overhaul, from reformatting marketing strategies to reformulating product specifications, which equals more studies. “A change of specifications may require appropriate clinical studies for safety and efficacy. Also, costs and marketing will be affected,” said Ryungza Lee Fletcher, marketing executive, Toyo Bio-Pharma. Thus, personal care companies should take advantage of the resources and the clinical studies conducted by ingredient suppliers, as well as their knowledge of how their ingredients can be incorporated into finished products. “We not only provide the ingredients but can show prospective companies finished products using our ingredients and provide valuable services in product development and marketing strategies,” Fletcher said.

Many antioxidants are highly reactive with light and oxygen; therefore, antioxidant-rich products must be protected in both the formulation and its container. Once a product turns brown, oxidation has occurred. “Antioxidants neutralize ROS, and tend to do this already in the jar or flask even before they are administered to the skin,” Schonlau noted. “It represents a significant challenge for formulators to prevent the antioxidants in the formulations from getting oxidized either by addition of suitable protective agents, or using airless containers (tubes and the currently popular airless flasks with a pump).”

From invisible microcapsules and liposomes that release the antioxidant at the time of application, ingredient suppliers are offering strategic delivery mechanisms and methods to help personal care manufacturers overcome the hurdles of adding antioxidants. Toyo Bio-Pharma, for example, offers a NouriMask delivery system for deep dermal penetration; and Cognis has found encapsulating lipophilic vitamins such as retinol and polymers made by a chitosan coacervation technique are effective solutions. Sabinsa Corp. uses a natural patented spice extract called Tetrahydropiperine, derived from black pepper, to enhance the uptake of bioactive compounds when included in very small amounts in formulations. Other companies such as Bio-Botanica can offer alternatives to working with synthetic preservatives; its patented extraction method, Bio-Chelation®, provides a stable botanical compound while other patents cover natural preservatives made from extracts that are as effective as parabens.

The idea of beauty from the inside out is also emerging as a promising new delivery system. “Supplementation for skin health and beauty is an alternative to the harsh treatments and chemicals currently applied on the skin,” said Yasuko Kuroda, vice president, Fuji Health Science.

Ron Udell, president, Soft Gel Technologies, added: “Soft Gel Technologies places more emphasis on an anti-aging program from the inside out; shifting the focus of consumers to repairing the skin from within as well as supporting the rest of the body’s organs and systems.”

Ultimately, the goal is delivering a product that works. While an ingredient supplier can provide studies on individual ingredients, a variety of delivery systems and options, and even assistance in formulation, it is up to manufacturers to conduct performance tests on the finished product to confirm that the results will be delivered. Keep in mind, the biggest obstacle may be re-educating a consumer who is used to immediate results by reminding them the product may take longer to achieve noticeable effects. This can be achieved by backing the product with science, literature and a product that works.

The days of antioxidants being used strictly as novelty ingredients in upscale stores and spas are numbered, as more accessible and innovative cosmeceutical products emerge. “Antioxidants from botanicals and the combination of antioxidants will become more popular and will enable new claims in all kinds of different applications,” said Issberner. “Current modern and future applications will cover lotions and creams with antioxidants for all body areas, including scalp, legs, décolleté, feet and hair.”

But, the hottest buzz in the industry is the concept of achieving beauty both internally and externally. This trend is bound to continue through the new year, as research uncovers benefits afforded with topical and internal use of these specialty compounds. “Antioxidants are big business with companies today incorporating natural ingredients,” Sysler said. “With the increased popularity of cosmetic procedures such as botox and tucks, consumers will continue to search for more natural, less invasive alternatives.” 

The Rule of Four S’s

This system of evaluation for manufacturers and formulators looking to add plant-derived cosmetic ingredients to their personal care products was created by Rebecca James Gadberry, president, YG Laboratories, and is an excellent tool for manufacturers to consider when adding antioxidants or blends into a personal care line.

Standardization. The chemical composition of a plant may vary depending upon the nutrients in the soil, the climate, the age of the plant, and time of harvest. Companies perform tests to measure the presence of phytochemicals (which perform the results delivered by the plant to the skin). Known as chemical standardization, ingredient suppliers may compare new ingredient batches with a pre-existing standard that contains the desired mix and levels of phytochemicals. Since this is a controversial practice that leaves room for the “topping off” of standardized extracts with synthetic versions to meet specifications, some companies may prefer using whole plant extracts. Chemically standardized plants are more likely to contain known levels of phytochemicals, while whole plant extracts may vary from batch to batch, and some important phytochemicals may not be present at all.

Solubility. Ingredients tend to be either oil- or water-soluble and often contain only one group of soluble chemicals. When reviewing a study or learning about a plant’s phytochemical makeup, compare the phytochemical’s solubility to the form the ingredient takes in your product. Call the ingredient supplier to clarify if you are unsure of the solubility.

Studies. Not all studies on a specific plant ingredient apply to other ingredients with the same name. Keep in mind, studies on individual ingredients point the way to incorporating an ingredient into a formula but do not confirm that the endproduct will produce the same results. The best tests are the ones performed on the finished product.

Stability. Extracts rich in antioxidant flavonoids can be fragile in the presence of light and air, reducing their potency and causing browning. They can also be completely destroyed in hot temperatures. Check with your supplier on how they protect the activity of these phytochemicals.

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