NATURALS
The many functions of azelaic acid in cosmetics
Lisanne Brouns – Azeco Cosmeceuticals ABSTRACT
In Ayurvedic alternative medicine, the grains of wheat, barley and rye have been used since old time for the treatment of topical hyperpigmentation. Only about 3,000 years later it was found that this property was due to the inhibition of tyrosinase, the enzyme involved in the melanin formation process, by azelaic acid. Yet azelaic acid, a saturated
dicarboxylic acid, is not only a whitening agent, it exhibits also bactericidal and anti-inflammatory properties and this has resulted in the application of it for the treatment of acne vulgaris and rosacea. It also shows other interesting properties and synergies with other active ingredients, such as for example some ones useful in hair regrowth products. A commercial production of
Azelaic acid is a naturally occurring 9-carbon straight-chained saturated dicarboxylic acid (isolated from cultures of Pityrosporum Ovale) naturally present in rye, wheat, and barley. A single mechanism of action has not been identified to explain the several beneficial effects of azelaic acid on the skin. From the results of several accurate
experimental scientific works, it is known that topical azelaic acid has anti-inflammatory and antibacterial properties, in addition to comedolytic action. It also competitively inhibits tyrosinase, an enzyme involved in the conversion of tyrosine to melanin, and may than successfully used to reduce epidermal hyperkeratinization. So this active ingredient, an efficient
antibacterial and anti-proliferative agent, can find its natural application in the formulation of skincare cosmetics. According to the high number of scientific published data, it is the ideal active to treat skin to inhibit the pigment producing enzyme tyrosinase,1
it has comedolytic properties, and
may reduce epidermal hyperkeratinization. It has been shown to be effective in the treatment of hyperpigmentary disorders such as chloasma and lentigo maligna, and to have a cytotoxic effect on the human malignant melanocyte.2
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While treating cases of chloasma with topical application of an azelaic acid cream, it was observed, and confirmed by patients, that lesions of acne within the areas being treated showed significant improvement. This acid is then used to treat bacterial-
related acne breakouts by attacking the infected pores to help in reducing inflammation and lowering the production of keratin which creates clumps of dead skin cells that trap sebum in skin pores causing more breakouts. With that said, as azelaic acid was more commonly used to treat acne related problems, doctors noticed it had side effects to it which were related to skin lightening. In 1978, the tyrosinase-inhibiting activity of certain lipid fractions, mainly C9–C11 dicarboxylic acids, was demonstrated for the first time in vitro. The interest in azelaic acid, which is a C9-dicarboxylic acid, for treating pigmented lesions thus ensued.3 It is known in the art that Inhibition
of 5-α-reductase type 1 is an answer to androgenic alopecia, Azelaic acid is a very potent 5-α-reductase inhibitor. The powerful combination (azelaic acid + zinc sulphate + vitamin B6) for the treatment of androgenic alopecia is cosmetically suitable contrary to the steroidal and non-steroidal pharmaceutical
azelaic acid from botanical resources (wheat, barley and rye for example) is commercially not feasible, but today a natural derived azelaic grade (from high oleic sunflower oil) is present on the market, with a chemical structure identical to one observed in nature. This grade of azelaic acid is characterized by a very high purity, the highest in the market (> 99% by weight), very important feature to have a product characterized by the absence of collateral effects together a great effectiveness.
preparations present on the market for the treatment of this kind of disease. Today there is unanimous agreement
regarding efficacy of azelaic acid together absence of undesirable effects of note. Azelaic acid may be, then, used in the personal care products, in medical devices and in pharmaceutical products of many countries without concentration limitations. It shows no significant side effects, it has no cytotoxic properties and does not exhibit CMR (carcinogenic, mutagenic and reprotoxic) properties. Today several grades of azelaic acid are
available. Azeco Cosmeceuticals has developed and placed on the market an ultra-pure, micronised cosmetic grade of azelaic acid with vegetable origin, COSMOS approved. This grade of azelaic acid is the ideal active ingredient for a
October 2023 PERSONAL CARE
85
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