Grand Azelaic

Grand Azelaic, is an organic compound with the chemical formula HOOC(CH2)7COOH.
This saturated dicarboxylic acid, initially identified in rancid fats, is also present in dietary sources like w h o l egrains. Industrially, azelaic acid is produced through the ozonolysis of oleic acid, yielding nonanoic acid as a byproduct. It is also naturally synthesized by Malassezia furfur (formerly Pityrosporum ovale), a yeast commonly found on healthy skin.

INCI name: Azeleic Acid

CAS: 123-99-9
Appearance: White crystal powder

Azelaic acid is a naturally occurring dicarboxylic acid found in grains such as barley, wheat, and rye. It is a versatile and effective ingredient in cosmetic and pharmaceutical formulations due to its anti-inflammatory, antimicrobial, and exfoliating properties.


Mechanism of Action:

  1. Antimicrobial Activity:
    Azelaic acid has strong antimicrobial properties, particularly against Propionibacterium acnes (P. acnes), the bacteria responsible for acne. It also has activity against other skin pathogens, including Staphylococcus epidermidis. This antimicrobial effect helps reduce the development of acne lesions and control infection on the skin.

  2. Anti-Inflammatory:
    Azelaic acid reduces inflammation, making it effective in treating inflammatory skin conditions like acne and rosacea. It works by inhibiting the production of reactive oxygen species (ROS) that lead to inflammation and by modulating the immune response to calm irritation and redness.

  3. Keratolytic (Exfoliating):
    Azelaic acid has a mild keratolytic effect, which means it promotes the shedding of dead skin cells and prevents the clogging of pores. By encouraging cell turnover, it helps improve skin texture, unclog pores, and treat hyperpigmentation, including post-inflammatory hyperpigmentation (PIH) that often results from acne.

  4. Inhibition of Melanin Production:
    Azelaic acid inhibits tyrosinase, an enzyme involved in the production of melanin. This makes it effective in treating hyperpigmentation, such as dark spots and melasma, by lightening the skin over time. This action also contributes to its use in treating post-acne pigmentation.

  5. Regulation of Keratinocytes:
    Azelaic acid regulates keratinocyte function, helping to normalize skin cell turnover. This leads to smoother, clearer skin, as it reduces the formation of comedones (clogged pores) and helps with conditions like acne.


Applications in Cosmetic and Pharmaceutical Formulations:

  1. Acne Treatment:

    • Topical Creams and Gels: Azelaic acid is commonly found in acne treatment products due to its ability to kill acne-causing bacteria, reduce inflammation, and exfoliate the skin. It is effective in both treating active acne and preventing future breakouts.
    • Prescription Acne Medications: It is available in prescription-strength formulations (typically 15% to 20%) for treating acne vulgaris, often as an alternative to other treatments like benzoyl peroxide or retinoids.
  2. Rosacea Treatment:

    • Topical Creams: Azelaic acid is used in rosacea treatments due to its anti-inflammatory and antimicrobial properties. It helps reduce the redness and swelling associated with rosacea by controlling the underlying inflammatory process.
  3. Hyperpigmentation and Skin Brightening:

    • Brightening Serums and Creams: Azelaic acid helps fade dark spots and hyperpigmentation caused by acne, melasma, and sun damage. Its inhibitory effect on melanin production makes it a popular choice in products targeting uneven skin tone and dark spots.
    • Post-Acne Scarring: It is effective in treating post-inflammatory hyperpigmentation (PIH) left behind after acne lesions heal, providing a more even skin tone.
  4. Anti-Aging and Skin Texture:

    • Exfoliating Masks and Serums: Due to its mild exfoliating properties, azelaic acid is often incorporated into products designed to improve skin texture and reduce fine lines. It enhances cell turnover and can help improve the overall appearance of the skin, making it look smoother and more youthful.
  5. Sensitive Skin Care:

    • Gentle Exfoliation: Azelaic acid is less irritating than many other exfoliants (such as AHAs or BHAs) and can be used on sensitive or reactive skin. It is often found in formulations for individuals with sensitive skin or conditions like eczema or rosacea.

Formulation Considerations:

  1. Stability:
    Azelaic acid is relatively stable when stored under proper conditions (in sealed containers, away from excessive light and heat). However, its solubility in water is limited, so it is often incorporated into products with oil-based or aqueous-alcoholic systems to enhance skin absorption.

  2. Concentration:

    • In over-the-counter (OTC) formulations, azelaic acid concentrations typically range from 10% to 15%.
    • Prescription-strength formulations may contain 15% to 20% azelaic acid. These formulations are often used to treat acne and rosacea more aggressively.
    • Concentration considerations: The concentration used in a product will depend on the skin concern being addressed and the patient’s skin tolerance.
  3. pH Compatibility:
    Azelaic acid works best in formulations with a slightly acidic to neutral pH, typically in the range of pH 4-6. It is important to adjust the pH of the product to ensure its effectiveness and stability.

  4. Compatibility with Other Ingredients:

    • Compatible Ingredients: Azelaic acid is generally compatible with most ingredients commonly used in skincare products, including antioxidants, peptides, and moisturizers. It can be combined with products containing niacinamide, hyaluronic acid, and vitamin C for enhanced brightening effects.
    • Incompatible Ingredients: While generally safe to use with most actives, azelaic acid may cause irritation when combined with other strong exfoliating agents like AHAs, BHAs, or retinoids in high concentrations. Care should be taken when formulating such combinations.

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