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  • Writer's pictureSolomon Matzner

Azelaic Acid for Hyperpigmentation

Azelaic acid is highly regarded for its effectiveness in treating various forms of hyperpigmentation, including melasma, post-inflammatory hyperpigmentation (PIH), and other pigment disorders. Its efficacy stems from its ability to address the key mechanisms of hyperpigmentation through multiple pathways. Here's a detailed exploration of how azelaic acid works, supported by scientific evidence, along with information on how it's formulated and used in treatments for hyperpigmentation.

1. Tyrosinase Inhibition

The primary mechanism by which azelaic acid combats hyperpigmentation is through the inhibition of tyrosinase, an enzyme crucial for melanin production.

  • Mechanism: Azelaic acid interferes with the synthesis of melanin by inhibiting tyrosinase. It is particularly effective because it selectively targets hyperactive melanocytes (the cells that produce melanin) without affecting normally functioning cells. This selective inhibition helps reduce the formation of unwanted pigment without lightening surrounding normal skin.

  • Scientific Evidence: Studies, including one by Katsambas et al., have shown that azelaic acid is as effective as hydroquinone, a standard treatment for hyperpigmentation, in reducing the pigmentation in melasma patients, attributing this effect to its tyrosinase-inhibiting properties.

Reference: Katsambas, A., et al. (1998). Azelaic acid for the treatment of hyperpigmentation disorders. Archives of Dermatology.

2. Antioxidant Properties

Azelaic acid also possesses antioxidant properties that contribute to its effectiveness in treating hyperpigmentation.

  • Mechanism: It reduces oxidative stress in the skin, which can trigger melanin production. By neutralizing free radicals, azelaic acid helps prevent the activation of pathways that lead to excess pigment production.

  • Impact: This antioxidant activity is particularly beneficial in managing melanin synthesis triggered by environmental factors like UV radiation and pollution.

3. Anti-inflammatory Effects

Inflammation is a significant trigger for melanin production, particularly in conditions like PIH, where an inflammatory event leads to increased pigment production.

  • Mechanism: Azelaic acid reduces inflammation by modulating several inflammatory pathways and decreasing the migration of leukocytes, thereby reducing cytokine release in the affected area. By controlling inflammation, azelaic acid helps prevent the overproduction of melanin that often follows dermatological injuries or acne.

  • Scientific Evidence: Research indicates that azelaic acid’s anti-inflammatory properties contribute significantly to its ability to reduce PIH and other inflammation-induced pigmentation issues.

How Azelaic Acid Is Used in Formulations for Hyperpigmentation

Azelaic acid is incorporated into various dermatological products designed to treat hyperpigmentation, including creams, gels, and serums.

  • Concentration: It is commonly formulated at concentrations of 10% to 20%. These concentrations have been found effective in reducing pigmentation without causing significant irritation.

  • Application: Products are typically applied to clean skin once or twice daily, depending on the formulation's strength and the dermatologist's advice. For best results, azelaic acid should be used regularly over several months.

Usage Guidelines: Consistent use of azelaic acid is crucial for reducing hyperpigmentation. Improvement can generally be observed within a few weeks, with more significant results appearing with continued use. Azelaic acid is often used in combination with other treatments like sunscreen, which helps prevent further pigmentation from UV exposure.


Azelaic acid’s multifaceted approach—combining tyrosinase inhibition, antioxidant properties, and anti-inflammatory effects—makes it an effective treatment for various types of hyperpigmentation. This comprehensive mode of action allows it to address both the symptoms and underlying causes of excess pigment production, improving skin tone and reducing the appearance of dark spots.

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