<i>In Vitro</i> 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 <i>in vitro</i> from a 2% ointment using porcine s...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-05-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/12/6/491 |
| _version_ | 1797566792674050048 |
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| author | Adriana Fantini Anna Demurtas Sara Nicoli Cristina Padula Silvia Pescina Patrizia Santi |
| author_facet | Adriana Fantini Anna Demurtas Sara Nicoli Cristina Padula Silvia Pescina Patrizia Santi |
| author_sort | Adriana Fantini |
| collection | DOAJ |
| 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 <i>in vitro</i> 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. |
| first_indexed | 2024-03-10T19:32:00Z |
| format | Article |
| id | doaj.art-3b8c804822b14a168175bfcbf3c9eccb |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T19:32:00Z |
| publishDate | 2020-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-3b8c804822b14a168175bfcbf3c9eccb2023-11-20T02:02:44ZengMDPI AGPharmaceutics1999-49232020-05-0112649110.3390/pharmaceutics12060491<i>In Vitro</i> Skin Retention of Crisaborole after Topical ApplicationAdriana Fantini0Anna Demurtas1Sara Nicoli2Cristina Padula3Silvia Pescina4Patrizia Santi5Department of Food and Drug, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/a, 43124 Parma, ItalyCrisaborole, 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 <i>in vitro</i> 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.https://www.mdpi.com/1999-4923/12/6/491atopic dermatitiscrisaboroleskin retentiontape stripping |
| spellingShingle | Adriana Fantini Anna Demurtas Sara Nicoli Cristina Padula Silvia Pescina Patrizia Santi <i>In Vitro</i> Skin Retention of Crisaborole after Topical Application Pharmaceutics atopic dermatitis crisaborole skin retention tape stripping |
| title | <i>In Vitro</i> Skin Retention of Crisaborole after Topical Application |
| title_full | <i>In Vitro</i> Skin Retention of Crisaborole after Topical Application |
| title_fullStr | <i>In Vitro</i> Skin Retention of Crisaborole after Topical Application |
| title_full_unstemmed | <i>In Vitro</i> Skin Retention of Crisaborole after Topical Application |
| title_short | <i>In Vitro</i> Skin Retention of Crisaborole after Topical Application |
| title_sort | i in vitro i skin retention of crisaborole after topical application |
| topic | atopic dermatitis crisaborole skin retention tape stripping |
| url | https://www.mdpi.com/1999-4923/12/6/491 |
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