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Patent Pick: Indolyl for Smarter Skin Whitening

Contact Author Rachel Grabenhofer
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Aging, and therefore anti-aging, takes many forms. In some skin types, youth gradually wrinkles; in others, skin spots appear before our very eyes. Most times, we eventually see both.

To minimize age spots, the general approach has been to regulate pigment production or dispersion in melanocytes. However, the current agents used either lack efficacy or cause skin irritation.

Thus, the present work describes efforts toward the continued need for new skin lightening agents with improved overall effectiveness. This need appears to be met using specific indolyl compounds.

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Compounds for reducing cellular melanin content
WIPO Patent Application WO/2018/046243 
Publication date: March 15, 2018
Assignee: Unilever

As stated, consumers desire an even-toned complexion, free from hyperpigmentation and age spots. One solution is to use biological actives that reduce the activity of melanocytes. These cells produce the dark-colored pigment melanin and export it to the neighboring keratinocytes. Thus, compounds that reduce melanin synthesis when topically applied will reduce skin darkness over time and can generate a more even skin tone.

Tyrosinase is one popular target for the regulation of melanocyte production. However, some inhibitors of tyrosinase are accompanied by safety issues; for example, permanent depigmentation, irritation and allergic reactions. Often, effective inhibitors such as hydroquinone can even kill melanocytes.

Other skin-lightening compositions are based on agents designed to control the dispersion of melanin or to inhibit tyrosinase. These include niacinamide, carboxylic acids such as azelaic acid and kojic acid, plant extracts and the aforementioned hydroquinone.

Indole-type compounds also have been reported impart cosmetic benefits; more specifically, indolyl compounds that contain a core indole group carrying other chemical groups. However, these have not been described for reducing melanin content in human skin. 

Surprisingly, these researchers found that specific indolyl compounds, such as 2-chloroethyl [2-(1 H-indol-3-yl)-1-methylethyl] carbamate, can reduce the cellular melanin content of melanocytes in human cell living skin equivalents containing keratinocytes and melanocytes. Thus, disclosed in this patent application is the use of said compounds for skin-whitening benefits.

Patent application accessed on March 19, 2018.

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