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In Vitro Skin Retention of Crisaborole after Topical Application

Crisaborole, a nonsteroidal phosphodiesterase 4 inhibitor, represents the first nonsteroidal medication approved for the treatment of atopic dermatitis in over a decade. In this work, crisaborole skin permeation and retention was studied in vitro from a 2% ointment using porcine skin as barrier. Cri...

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Autores principales: Fantini, Adriana, Demurtas, Anna, Nicoli, Sara, Padula, Cristina, Pescina, Silvia, Santi, Patrizia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7355453/
https://www.ncbi.nlm.nih.gov/pubmed/32481663
http://dx.doi.org/10.3390/pharmaceutics12060491
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author Fantini, Adriana
Demurtas, Anna
Nicoli, Sara
Padula, Cristina
Pescina, Silvia
Santi, Patrizia
author_facet Fantini, Adriana
Demurtas, Anna
Nicoli, Sara
Padula, Cristina
Pescina, Silvia
Santi, Patrizia
author_sort Fantini, Adriana
collection PubMed
description Crisaborole, a nonsteroidal phosphodiesterase 4 inhibitor, represents the first nonsteroidal medication approved for the treatment of atopic dermatitis in over a decade. In this work, crisaborole skin permeation and retention was studied in vitro from a 2% ointment using porcine skin as barrier. Crisaborole was also characterized in terms of thermal behavior, solubility, and logP. Control experiments were performed also on tape stripped skin to clarify the role of stratum corneum in drug partitioning and permeation across the skin. The results obtained indicate that crisaborole accumulates into the skin in considerable amounts after application of a topical lipophilic ointment. Crisaborole shows more affinity for the dermis compared to the epidermis despite its relatively high value of partition coefficient; stratum corneum analysis revealed a low affinity of the drug for this skin layer. Skin penetration across hair follicles or sebaceous glands can be a reason for the high dermis retention and is worth further investigation. The comparison with data obtained from a solution in acetonitrile suggests that the formulation plays a certain role in determining the relative distribution of crisaborole in the skin layers and in the receptor compartment.
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spelling pubmed-73554532020-07-23 In Vitro Skin Retention of Crisaborole after Topical Application Fantini, Adriana Demurtas, Anna Nicoli, Sara Padula, Cristina Pescina, Silvia Santi, Patrizia Pharmaceutics Article Crisaborole, a nonsteroidal phosphodiesterase 4 inhibitor, represents the first nonsteroidal medication approved for the treatment of atopic dermatitis in over a decade. In this work, crisaborole skin permeation and retention was studied in vitro from a 2% ointment using porcine skin as barrier. Crisaborole was also characterized in terms of thermal behavior, solubility, and logP. Control experiments were performed also on tape stripped skin to clarify the role of stratum corneum in drug partitioning and permeation across the skin. The results obtained indicate that crisaborole accumulates into the skin in considerable amounts after application of a topical lipophilic ointment. Crisaborole shows more affinity for the dermis compared to the epidermis despite its relatively high value of partition coefficient; stratum corneum analysis revealed a low affinity of the drug for this skin layer. Skin penetration across hair follicles or sebaceous glands can be a reason for the high dermis retention and is worth further investigation. The comparison with data obtained from a solution in acetonitrile suggests that the formulation plays a certain role in determining the relative distribution of crisaborole in the skin layers and in the receptor compartment. MDPI 2020-05-28 /pmc/articles/PMC7355453/ /pubmed/32481663 http://dx.doi.org/10.3390/pharmaceutics12060491 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Fantini, Adriana
Demurtas, Anna
Nicoli, Sara
Padula, Cristina
Pescina, Silvia
Santi, Patrizia
In Vitro Skin Retention of Crisaborole after Topical Application
title In Vitro Skin Retention of Crisaborole after Topical Application
title_full In Vitro Skin Retention of Crisaborole after Topical Application
title_fullStr In Vitro Skin Retention of Crisaborole after Topical Application
title_full_unstemmed In Vitro Skin Retention of Crisaborole after Topical Application
title_short In Vitro Skin Retention of Crisaborole after Topical Application
title_sort in vitro skin retention of crisaborole after topical application
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7355453/
https://www.ncbi.nlm.nih.gov/pubmed/32481663
http://dx.doi.org/10.3390/pharmaceutics12060491
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