Soluble cyclodextrin inclusion compound of Azelaic Acid

Appearance

White powder

Grade

Pharmaceutical grade

Standard

In‑house (enterprise) standard

Description

The inclusion complex is formed by encapsulating azelaic acid (AZA/AZE) molecules into the hydrophobic cavity of cyclodextrin (e.g., β-cyclodextrin or hydroxypropyl-β-cyclodextrin) via host–guest inclusion complexation. Azelaic acid is a naturally occurring saturated dicarboxylic acid with anti-inflammatory, antioxidant, antimicrobial, and keratolytic properties. It is widely used for treating acne vulgaris, rosacea, melasma, and post-inflammatory hyperpigmentation. However, its therapeutic potential is limited by extremely poor water solubility. Complexation with cyclodextrin significantly improves aqueous solubility, reduces skin irritation, and enhances skin penetration and bioavailability. The inclusion complex is typically formed at a 1:1 molar ratio.

CAS Number

Component CAS numbers: azelaic acid 123-99-9; β-cyclodextrin 7585-39-9; hydroxypropyl-β-cyclodextrin 128446-35-5.

Solubility

Significantly enhanced: >20.0 g/100 cm³ at 20°C (compared to ~0.24 g/100 cm³ for free azelaic acid). Some products report solubility up to 20% (25°C).

Storage

Store in tightly sealed containers, away from heat and direct light, in a cool, dry place

Applications

Widely used in pharmaceuticals and cosmetics for: treatment of acne vulgaris; treatment of papulopustular rosacea; treatment of melasma and post-inflammatory hyperpigmentation; anti-inflammatory and antimicrobial therapy; oil control and exfoliation; and as a skin-lightening agent.

Physical State

Solid powder.

Stability

Stable under recommended storage conditions. Encapsulation provides stabilization against oxidation, degradation, and photolytic cleavage. Short-term stability has been confirmed in hydrogel formulations