<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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Gespeichert in:

Autor*in:	Adriana Fantini [verfasserIn] Anna Demurtas [verfasserIn] Sara Nicoli [verfasserIn] Cristina Padula [verfasserIn] Silvia Pescina [verfasserIn] Patrizia Santi [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2020

Schlagwörter:	atopic dermatitis crisaborole skin retention tape stripping

Übergeordnetes Werk:	In: Pharmaceutics - MDPI AG, 2010, 12(2020), 6, p 491
Übergeordnetes Werk:	volume:12 ; year:2020 ; number:6, p 491

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/pharmaceutics12060491

Katalog-ID:	DOAJ022799435

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allfieldsSound	10.3390/pharmaceutics12060491 doi (DE-627)DOAJ022799435 (DE-599)DOAJ3b8c804822b14a168175bfcbf3c9eccb DE-627 ger DE-627 rakwb eng RS1-441 Adriana Fantini verfasserin aut <i<In Vitro</i< Skin Retention of Crisaborole after Topical Application 2020 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier 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. atopic dermatitis crisaborole skin retention tape stripping Pharmacy and materia medica Anna Demurtas verfasserin aut Sara Nicoli verfasserin aut Cristina Padula verfasserin aut Silvia Pescina verfasserin aut Patrizia Santi verfasserin aut In Pharmaceutics MDPI AG, 2010 12(2020), 6, p 491 (DE-627)614096529 (DE-600)2527217-2 19994923 nnns volume:12 year:2020 number:6, p 491 https://doi.org/10.3390/pharmaceutics12060491 kostenfrei https://doaj.org/article/3b8c804822b14a168175bfcbf3c9eccb kostenfrei https://www.mdpi.com/1999-4923/12/6/491 kostenfrei https://doaj.org/toc/1999-4923 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 12 2020 6, p 491
language	English
source	In Pharmaceutics 12(2020), 6, p 491 volume:12 year:2020 number:6, p 491
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topic_facet	atopic dermatitis crisaborole skin retention tape stripping Pharmacy and materia medica
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authorswithroles_txt_mv	Adriana Fantini @@aut@@ Anna Demurtas @@aut@@ Sara Nicoli @@aut@@ Cristina Padula @@aut@@ Silvia Pescina @@aut@@ Patrizia Santi @@aut@@
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callnumber-first	R - Medicine
author	Adriana Fantini
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topic_title	RS1-441 <i<In Vitro</i< Skin Retention of Crisaborole after Topical Application atopic dermatitis crisaborole skin retention tape stripping
topic	misc RS1-441 misc atopic dermatitis misc crisaborole misc skin retention misc tape stripping misc Pharmacy and materia medica
topic_unstemmed	misc RS1-441 misc atopic dermatitis misc crisaborole misc skin retention misc tape stripping misc Pharmacy and materia medica
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title	<i<In Vitro</i< Skin Retention of Crisaborole after Topical Application
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title_auth	<i<In Vitro</i< Skin Retention of Crisaborole after Topical Application
abstract	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.
abstractGer	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.
abstract_unstemmed	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.
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