In Vitro Skin Retention of Crisaborole after Topical Application

Area of Science:

• Pharmacology
• Dermatology
• Materials Science

Background:

• Crisaborole is a novel nonsteroidal phosphodiesterase 4 inhibitor for atopic dermatitis.
• It's the first nonsteroidal treatment approved in over a decade.
• Understanding its skin interaction is crucial for efficacy.

Purpose of the Study:

• To investigate the in vitro skin permeation and retention of crisaborole.
• To characterize crisaborole's physicochemical properties.
• To elucidate the role of the stratum corneum and formulation in drug disposition.

Main Methods:

• In vitro permeation studies using porcine skin.
• Characterization of crisaborole: thermal behavior, solubility, logP.
• Experiments on tape-stripped skin to assess stratum corneum effects.
• Comparison with a solution formulation.

Main Results:

• Crisaborole 2% ointment leads to considerable skin accumulation, favoring the dermis over the epidermis.
• Low affinity for the stratum corneum was observed.
• The formulation significantly influences crisaborole distribution within skin layers and the receptor compartment.

Conclusions:

• Topical crisaborole ointment results in substantial skin retention, with preferential accumulation in the dermis.
• Stratum corneum is not the primary barrier for crisaborole, suggesting follicular or sebaceous gland penetration.
• Formulation plays a key role in crisaborole's skin disposition and potential therapeutic outcomes.