Novel technology produces 3-in-1 whitening ingredient

The global market for skin whitening products (also called brighteners, according to the geographical areas) amounts to US$ 13 billion and is a rapidly growing segment in the personal care industry.

According to Euromonitor, it will grow at about 13% per year in Asia Pacific during the next 5 years. Skin lightening has been quite popular in Japan for a considerable time but the whole Asian market is actively following the trend. The whitening cosmetic market is growing rapidly in China (33% of the Chinese population use lightening cosmetics daily or weekly). Asian women are using these products to lighten their naturally dark skin colour. However, European and American women are using ‘brightening’ products to reduce age spots, acne scars and freckles, for instance. There is a continuous demand for innovative and efficient products, able to act both instantaneously and in the long term.

Actives for a long-term brightening effect

To address problems presented by skin hyperpigmentation, hydroquinone and hydroxyanisole have been used in the past as traditional active ingredients. Kojic acid has also been a popular one. However, all these ingredients have raised safety concerns and have been questioned by various reports demonstrating their adverse effects. As a consequence, the cosmetic market has been looking into alternatives and whenever possible for natural ones. The first step was to find natural products with similar lightening properties as hydroquinone or hydroxyanisole. Active compounds isolated from plants, such as arbutin, aloesin, flavonoids, liquorice and polyphenols, are able to inhibit melanogenesis. Arbutin which is derived from the leaves of bearberry, cranberry, mulberry or blueberry shrubs possesses melanin inhibiting properties and has shown efficacy as a depigmenting agent. Arbutin actually exists in two conformations, alpha and beta. The alpha conformation, obtained through synthesis, offers higher stability over the beta conformation and is the preferred form for skin lightening indications. Alpha arbutin will not liberate hydroquinone in the tested pH range from 3.5 to 6.5 including the pH range of the skin. Both have been tested as tyrosinase inhibitors, but alpha arbutin inhibits the activity of tyrosinase much more effectively than its beta version due to its perfect affinity to the active site of tyrosinase. The inhibitory effect of alpha arbutin on melanin synthesis is not due to the action of hydroquinone released. Liquorice extract is also a reference in the market of whitening ingredients. The main component of the hydrophobic fraction of liquorice is glabridin. This substance which is safe for global applications has been used to prevent UVB-induced pigmentation and to inhibit tyrosinase. Glabridin also exhibits antiinflammatory properties and a study on glabridin reported that it inhibited tyrosinase activity of melanocytes without cytotoxicity, at a topical application of 0.5%. All these substances have the property to inhibit the tyrosinase activity and thus to block epidermal melanin biosynthesis. The effect of all these active ingredients is not immediate and results can be seen only after the tyrosinase inhibition and melanin formation is stopped.

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