Climbazole (CAS 38083-17-9)

Climbazole – Synthetic Imidazole Antifungal for Dandruff and Seborrheic Dermatitis Treatment

Basic Information

• CAS Number: 38083-17-9

• Molecular Formula: C₁₅H₁₇ClN₂O₂

• Molecular Weight: 292.76 g/mol

• Synonyms: Climbazole, 1-(4-Chlorophenoxy)-1-imidazol-1-yl-3,3-dimethylbutan-2-one

• Appearance: White to off‑white crystalline powder

• Solubility: Lipophilic, poorly soluble in water; soluble in organic solvents and surfactants

• Storage: Store in a cool, dry place, protected from light and moisture

Overview
Climbazole is a synthetic imidazole derivative with potent antifungal activity. It is specifically designed to inhibit the growth of Malassezia species, the primary fungal pathogens responsible for dandruff and seborrheic dermatitis. Its efficacy, combined with a favourable safety profile, has made it a popular active ingredient in cosmetic and dermatological formulations, particularly in anti‑dandruff shampoos, scalp lotions, and leave‑on treatments.

Mechanism of Action
Climbazole acts by inhibiting the synthesis of ergosterol, an essential component of fungal cell membranes. It targets the enzyme lanosterol 14α‑demethylase (CYP51), disrupting membrane integrity and leading to fungal cell death. This mechanism ensures effective control of fungal colonization on the scalp, reducing flaking, itching, and inflammation associated with seborrheic dermatitis.

Physicochemical Properties

• Lipophilic nature: Enhances penetration into the stratum corneum and hair follicles, where Malassezia resides.

• High stability: Resistant to thermal and chemical degradation, allowing incorporation into various formulation types (shampoos, conditioners, creams, lotions).

• Low irritation: Non‑irritating to skin and scalp at recommended concentrations (0.5–2.0%).

• Substantivity: Adheres to skin and hair, providing prolonged antifungal activity even after rinsing.

Applications

• Anti‑dandruff shampoos: Used as a primary active ingredient at concentrations of 0.5–1.5% for daily or weekly use.

• Scalp lotions and tonics: Formulated for leave‑on application to manage chronic seborrheic dermatitis.

• Conditioners and hair masks: Combined with other conditioning agents to maintain scalp health and reduce recurrence.

• Cosmetic emulsions: Incorporated into creams and ointments for topical treatment of facial and body fungal infections.

• Synergistic formulations: Often combined with zinc pyrithione, piroctone olamine, or salicylic acid for enhanced efficacy and broader spectrum.

Key Benefits

• Highly effective against Malassezia yeasts, the main cause of dandruff and seborrheic dermatitis.

• Safe and well‑tolerated with low potential for skin irritation and sensitization.

• Long‑lasting activity due to good substantivity on skin and hair.

• Stable and compatible with a wide range of cosmetic ingredients and surfactants.

• Suitable for both rinse‑off and leave‑on products.

• Approved for use in cosmetics in many regions (EU, US, Asia) with established safety limits.

Recommended Use
Typical usage levels: 0.5–2.0% in shampoos and rinse‑off products; 0.5–1.0% in leave‑on formulations. For optimal efficacy, incorporate into the surfactant or oil phase during manufacturing. Pre‑dissolving in a suitable solvent (e.g., glycols, ethanol) may improve dispersion in aqueous systems.

Safety and Handling

• Climbazole is generally recognized as safe for topical use at recommended concentrations.

• Avoid contact with eyes; in case of contact, rinse thoroughly with water.

• May cause mild skin irritation in sensitive individuals; perform a patch test before use in leave‑on products.

• Store in a cool, dry place, away from direct sunlight and moisture.

• Use appropriate personal protective equipment (gloves, safety goggles) when handling raw material.

• Shelf life: typically 24–36 months under recommended storage conditions.

Quality Assurance
Each batch is tested for purity (by HPLC), melting point, and heavy metal content to ensure compliance with cosmetic and pharmaceutical standards.