Skin permeation and penetration of Crisaborole when coapplie
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Atopic dermatitis (AD), a chronic inflammatory skin disease characterized by eczematous lesions and pruritus, is prevalent worldwide. Crisaborole ointment 2% is a nonsteroidal phosphodiesterase 4 inhibitor for the treatment of mild to moderate AD. The objective of this study was to assess the effect of over-the-counter (OTC) cream and ointment moisturizers on the permeation and penetration of crisaborole.

Crisaborole was applied (10 mg/cm2) to ex vivo healthy abdominal human skin (3 donors, 4 replicates, sliced to a thickness of 500 ± 50 micrometre with a dermatome) either alone, 15 minutes before, immediately after, or 15 minutes after application of OTC cream or OTC ointment. The skin was mounted in a flow-through diffusion cell, and the receptor solution (phosphate-buffered saline) was collected at 2-hour intervals up to 24 hours. The amount of crisaborole delivered into the skin and through the skin into the receptor solution was determined by liquid chromatography–tandem mass spectrometry.

When crisaborole was applied 15 minutes before either OTC cream or ointment, there were no statistical differences in the concentration of crisaborole in the receptor solution or the dermis. However, when crisaborole was applied immediately after OTC cream, the concentration was significantly decreased by approximately 3-fold in the receptor solution and 2-fold in the dermis compared with crisaborole alone. Similar results were observed for the epidermis.

Application of crisaborole 15 minutes after OTC cream resulted in no statistical difference in the concentration of crisaborole in the receptor solution or in the epidermis and dermis. When crisaborole was applied immediately after OTC ointment, there was no statistical difference in the concentration of crisaborole in the receptor solution or in the epidermis and dermis. However, when crisaborole was applied 15 minutes after OTC ointment, the concentration of crisaborole decreased by approximately 2-fold in both the receptor solution and the epidermis.

There are limited data regarding the effect of coapplication of moisturizers and topical treatments. It is shown that using an ex vivo model, the time between applications can affect drug penetration and permeation. The current findings in an ex vivo model suggests that crisaborole should be applied at least 15 minutes before OTC ointments and creams to minimize the impact on dermal absorption of crisaborole.

source: https://www.jaad.org/article/S0190-9622(20)30541-7/fulltext?rss=yes
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