Formula Anatomy Deciphered: Anti-wrinkle Skin Care

For consumers, antiaging has many definitions and is a marketing position for a variety of topical personal care products. Within the antiaging category are a number of consumer products claiming to prevent or treat facial wrinkling. As is generally known, wrinkles occur as skin ages and are associated with causes that are genetic and environmental. For example, changes such as a decrease in both the number of fibroblasts and biosynthetic changes of biomolecules, based on large extra-cellular matrix molecular weight, as well as dermis atrophy are accentuated in the dermis.

In addition, external assault especially from sun exposure accelerates facial wrinkling. Therefore, skin aging can be attributed to both physiological skin changes and photodegradation. Moisture and collagen content and the immune responsiveness of skin are the main factors causing wrinkle formation. This is based on a decrease in the diameter or decomposition of collagen and elastin, along with the expansion of blood vessels. In the end, the mechanical strength and viscoelastic properties of the dermis are compromised, allowing skin to stretch under the influence of its own weight.

To address to this change, consumers seek products that make them look younger by toning the skin or visually hiding negative attributes. To such an end, active cosmetic ingredients have been developed to fight the loss of skin tone by simultaneously lifting and smoothing the skin and improving its viscoelastic properties. However, anti-wrinkle products that inspire such physiological changes and tout such benefits raise questions as to whether they are truly cosmetics or are more pharmaceutical in nature.

It is unfortunately difficult to turn back the clock on the age-related deterioration of skin physiology but three topical approaches can impart antiaging effects via other means: by covering or filling in wrinkles for smoother looking and feeling skin; by tightening the skin via astringent effects; and by physiologically improving the skin’s own repair mechanisms. Current studies in the area of genomics and DNA and cellular repair support this latter approach, although it acts on drug-related mechanisms; such products are therefore labeled cosmeceuticals.

Key Components

Many ingredients claim to improve the appearance of or to treat and repair wrinkles. The current trend is to develop natural botanical ingredients and polypeptides that provide antiaging properties at low and effective levels. It would be difficult to list all the possible natural ingredients that claim some type of antiaging effect without missing some, so one may generalize by simply stating that crucial to an antiaging treatment is the delivery of a natural or synthetic ingredient that provides the following key properties: antioxidation to counteract free radical formation; anti-inflammation to calm the skin and reduce irritation; exfoliation through raw materials such as alpha hydroxyl acids (AHA); sun protection, specifically through sunscreen agents that absorb or block UVA; skin softening, to support the elasticity and/or firming of skin; and pore- and crease-filling capabilities, so that particles fit within skin crevices and appear as a part of the skin.

The past several months have seen various innovative patents issued in relation to the antiaging category. Highlighted here are but a few, including those based on hydration, skin rejuvenation, collagen maintenance, repair and skin tensing, as well as one describing anti-wrinkle testing.

Recent Antiaging Patents

Endogenous hydration and aging: This invention1 is based on the hypothesis of Wisser and Gallagher2 that there is a relationship between the oxidative processes in skin and its degree of hydration. The inventors postulated that they could increase the effectiveness of antioxidants by using the cell water and hydrating molecules present within the skin. This approach would theoretically curb the oxidative process, and by maintaining good hydration in the surface layers of the skin, epidermis and horny layer, potentially improve the effectiveness of endogenous antioxidant molecules, or of cosmetic agents exhibiting an antioxidant effect.

In a preferred embodiment of this invention, plant extracts that are rich in flavonoids, isoflavonoids and/or anthocyanins, rose extract in particular, were used to confer antioxidant properties to protect against reactive oxygen species (ROS), which are responsible for oxidative stress. This invention also relates to an antiaging composition including a combination of cosmetic active agents.

Three-step skin rejuvenation: This patent discloses a three-step skin rejuvenation system3 involving a) the application of a booster product to activate the skin area to be treated; b) an exfoliant; and c) a nano-additive product for enhancing the penetration of the booster product and exfoliating product inside the skin area. Both the booster and exfoliant contain the active ingredients ferulic acid and phloretin; in addition, the exfoliant is formulated with fruit acids or alpha hydroxy acids.

Matrine and oxymatrine antiaging: This invention relates to a composition comprising the active ingredients matrine and oxymatrine for improving skin conditions such as wrinkles, skin pigmentation and hair loss.4 These materials reportedly have lower cytotoxicity than retinol as anti-wrinkle agents, and they inhibit collagenase activity and promote collagen biosynthesis at the molecular level, contributing to their efficacy in the improvement of skin wrinkles. In addition, both matrine and oxymatrine have been found to: exhibit an inhibitory effect on melanin production by inhibiting intracellular tyrosinase activity, improve the effects of UV-induced skin damage, promote skin growth and prevent hair loss.

Antiaging hyaluronic acid cream: The present invention relates to a topical anti-wrinkle and antiaging moisturizing cream designed to repair and restore human adult skin to a more youthful state.5 The moisturizer is a water-based blend of high molecular weight (HMW) hyaluronic acid (HA), 0.5–2.0 million Daltons, and low molecular weight HA oligosaccharides, i.e., small HA fragments less than 12,000 Daltons. An equal mixture of HMW HA and HA oligosaccharides at concentrations of 0.1–0.2% was found to provide the moisturizer with the ability to repair and rejuvenate adult human skin.

Anti-wrinkle oat polysaccharides: This invention relates to a method for obtaining an active ingredient that imparts an immediate anti-wrinkle and skin-tensing effect, characterized by extracting and purifying HMW polysaccharides from oat bran fibers or grains and stabilizing the polysaccharides in water.6 The method comprises at least two essential stages: a stage for solubilization of oat bran, fibers or seeds in a basic solution, and a stage of successive or simultaneous enzymatic hydrolysis(es) of polysaccharides that are contained in the oat bran, fibers or seeds, so as to facilitate their solubilization without disrupting their molecular structure. The invention also relates to the product obtained, to its uses, and to cosmetic compositions containing it.

Anti-wrinkle testing using ADAM: It is well-known that a group of membrane metalloproteases called A disintegrin and metalloprotease (ADAM), as well as matrix metalloprotease (MMP), cut various growth factors including heparin-binding epidermal growth factor (HB-EGF) and tumor necrosis factor (TNF), cytokines and many other membrane proteins from the cell surface and release them from the cell, resulting in the proliferation and differentiation of cells by those growth factors.7 Further, expression/release from the cell membrane of growth factors HB-EGF, TNF-alpha and cytokines are promoted by different stimuli, including UV light, oxidization and osmotic pressure. Signals for proliferation, differentiation, etc., are transmitted to the cells by the autocrine and paracrine mechanisms, leading to skin proliferation and thickening.

The present inventors have established a method whereby a test substance is applied to the skin, skin tissue or human cell; the enzymatic activity of the ADAM or gene expression level is detected; and the anti-wrinkle effect of the substance is assessed using the generation of the ADAM enzyme or gene expression as an index. Also described is an anti-wrinkle agent for ameliorating the particularly fine wrinkles developed when the skin’s barrier function is decreased by dryness. In addition, an anti-wrinkle agent or ADAM inhibitor is disclosed comprising an alkyl glucoside, wherein the alkyl group is represented by a linear or branched alkyl group with 1 to 18 carbon atoms.

Featured Ingredient: Antioxidants

Antioxidants are a popular anti-wrinkle treatment category. They can be derived from natural sources or synthetically manufactured. Their key performance criterion is to counteract free radicals that can mutate skin cells. Sources of these free radicals are environmental, such as smoke, sun exposure or diet. Use of antioxidants can mitigate skin damage to allow for healing, as well as stimulate new collagen production.

Antioxidants can be delivered as water-soluble or oil-soluble ingredients, although oil- or lipid-soluble derivatives can absorb more effectively into the stratum corneum. Antioxidants can assist in several capacities, including: reducing fine lines and wrinkles, supporting cell regeneration, evening out skin pigmentation, mitigating psoriasis effects, supporting a healthy immune system and stimulating collagen production.

Antioxidants can include vitamins such as retinol and esters, ascorbic acid and esters, tocopherol and esters and cholecalcipherol, amino acids/peptides such as acetyl hexapeptide-22 and decapeptide-6, botanical extracts, and carboxylic acids among a multitude of others (see Antioxidants on Page 84). An extended antioxidant list can be found in the Personal Care Product Council’s Infobase.8

Finished Antiaging Products

There are many current anti-wrinkle products on the market. The following three are featured to demonstrate claim positioning as well as how specific ingredients are incorporated to support these claims. The information presented is taken from publicly available sources and is included for illustrative purposes only. The estimated ingredient ranges are provided as a starting point from which formulators can build their own unique formulas.

Bottega Verde Mielexpertise Intense Antiaging Eye Contour Cream: The cream shown in Figure 1 and Table 1 on Page 86 is described as an intensive, fast-absorbing, antiaging eye contour cream featuring a re-densifying, anti-wrinkle formula enriched with the company’s patented ingredients Cuore di Miele (honey essence) and Pluridefence, which are claimed to have revitalizing, antioxidant and firming effects to leave skin soft and radiant and protect against pollution.

Garnier Nutritioniste Ultra-Lift Anti-Wrinkle Firming Eye Cream: This eye cream (see Figure 2 and Table 2) is formulated with a blend of natural linoleic acid from safflower with retinyl acetate to lift the look of wrinkles; rice protein to fortify skin’s structure; and argan extract to make skin look firmer. According to the manufacturer, the cream instantly smooths and softens the delicate eye area, firming fine lines and lifting wrinkles.

Reviva Labs Collagen-Fibre Eye Pads with Myoxinol: These eye pads (see Figure 3 and Table 3) are said to contain 100% pure, freeze- dried collagen, which is reported to impart quick, Botox-like benefits to skin; instantly hydrate to help diminish wrinkles, bags, puffiness or dark circles; and relax the under-eye tissue to aid anti-wrinkle action. Myoxinol extracted from the hibiscus flower is said to relax facial wrinkles while the collagen plumps and smoothes the skin.

Formulator Beware

Anti-wrinkle skin products are a complex group with strong claims to “turn back the clock” on skin damage and sagging skin. The key to their success lies in the daily moisturization and hydration of skin. It is therefore important to understand how to formulate an aesthetically pleasing product that conveys moisture or the feeling of moisture to skin, while tightening and hiding fine lines. Regarding anti-wrinkle biological actives, it is difficult to say if they are incorporated in sufficient amounts to work on the cellular level and are bio-available for transport to the critical sites within skin’s physiology. Formulators must ask themselves: Is the plant part being used the right plant part? Are the critical functional ingredients in the plant being delivered in sufficient quantities to provide physiological effects? Also, is enough of the botanical incorporated into the finished formula to actually work, or is the botanical present merely for claim purposes—or for consumer “reason-to-believe” expectations?

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1. US Pat Appl 20100303872, Use of a polyphenol-rich plant extract as antioxidant in combination with a hydrating or humectant agent, M Dumas et al, assigned to LVMH Recherche (Dec 2, 2010)
2. M Visser and D Gallagher, Age-related change in body water and hydration in old age, in Hydration Throughout Life, MJ Arnaud, ed, Montrouge, France: John Libbey Eurotext (1998) pp 117–125
3. US Pat Appl 20100255079, Systems and methods for skin rejuvenation, GS Sanmiguel et al, assigned to Sesvalia USA, LLC (Oct 7, 2010)
4. US Pat Appl 20100099698, Compositions for improving skin conditions comprising matrine or its oxidized derivatives, DH Park et al, assigned to Biospectrum Inc. (Apr 22, 2010)
5. US Pat Appl 20100098794, Topical anti-wrinkle and antiaging moisturizing cream, G Armand (Apr 22, 2010)
6. US Patent Application 20100029583, Process for obtaining an active ingredient with an immediate tensor effect on the skin, J Paufique, assigned to Silab (Feb 4, 2010)
7. US Pat Appl 20100035831, Anti-wrinkle agent and ADAM inhibitor, Y Matsunaga et al, assigned to Shiseido Company, Ltd. (Feb 11, 2010)
8. Infobase, Personal Care Products Council, 60&IngredInfoList=14&ingred=true (accessed Dec 6, 2010)

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