Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects

Yixuan Wang, Sisi Cao, Kaiyue Yu, Fengdie Yang, Xiuming Yu, Yuanhao Zhai, Chuanbin Wu, Yuehong XuDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People’s Republic of ChinaBackground: Topical application of tacrolimus (FK506) was eff...

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Autores principales:	Wang Y, Cao S, Yu K, Yang F, Yu X, Zhai Y, Wu C, Xu Y
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Tacrolimus microemulsion menthol camphor eutectic atopic dermatitis percutaneous delivery Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/15375b15b31a4dd3a35b08731bec99b5
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spelling	oai:doaj.org-article:15375b15b31a4dd3a35b08731bec99b52021-12-02T09:15:27ZIntegrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects1178-2013https://doaj.org/article/15375b15b31a4dd3a35b08731bec99b52019-07-01T00:00:00Zhttps://www.dovepress.com/integrating-tacrolimus-into-eutectic-oil-based-microemulsion-for-atopi-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Yixuan Wang, Sisi Cao, Kaiyue Yu, Fengdie Yang, Xiuming Yu, Yuanhao Zhai, Chuanbin Wu, Yuehong XuDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People’s Republic of ChinaBackground: Topical application of tacrolimus (FK506) was effective in treating atopic dermatitis (AD); however, the therapeutic efficiency is hampered by its poor penetration into the skin and local side effects of transient irritation symptoms with a burning sensation, a feeling of warmth or heat. Menthol and camphor have been widely used in topical compound formulations for adjunctive pharmacotherapy for antipruritics and analgesics owing to their cool nature, and both present skin penetration enhancing effects. Moreover, they can form a liquid eutectic oil to solubilize hydrophobic drugs.Purpose: Taking advantages of menthol/camphor eutectic (MCE), this work aims to integrate FK506 into MCE to construct a microemulsion system, i.e., FK506 MCE ME, which simultaneously enhances the percutaneous delivery and treatment efficacy, while reduces the side effects of FK506.Methods: The formulation of FK506 MCE ME was optimized and characterized. Different formulations containing FK506 were topically administered to treat 1–chloro–2, 4–dinitrobenzene (DNCB)-induced murine AD.Results: MCE solubilized FK506. FK506 in MCE ME penetrated skin in vitro more than in the commercial ointment, and MCE predominantly exerted the enhancing effects in MCE ME. FK506 MCE ME or FK506 MCE ME gel had greater effects on clinical symptoms, histological analysis, and IgE than did commercial FK506. The anti-pruritic and down-regulation of substance P effects of MCE ME vehicle mitigated the side effects of FK506 application.Conclusion: MCE ME presented the excellent properties of simultaneously enhancing the percutaneous delivery and treatment efficacy, while reducing the side effects of FK506 for AD. Therefore, MCE ME is a promising nanoscale system for FK506 to effectively treating AD with low irritation and high medication adherence.Chemical compounds studied in this article: Tacrolimus (PubChem CID: 445643); menthol (PubChem CID: 1254); camphor (PubChem CID: 2537)Keywords: tacrolimus, microemulsion, menthol, camphor, eutectic, atopic dermatitis, percutaneous deliveryWang YCao SYu KYang FYu XZhai YWu CXu YDove Medical PressarticleTacrolimusmicroemulsionmentholcamphoreutecticatopic dermatitispercutaneous deliveryMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 5849-5863 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Tacrolimus microemulsion menthol camphor eutectic atopic dermatitis percutaneous delivery Medicine (General) R5-920
spellingShingle	Tacrolimus microemulsion menthol camphor eutectic atopic dermatitis percutaneous delivery Medicine (General) R5-920 Wang Y Cao S Yu K Yang F Yu X Zhai Y Wu C Xu Y Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects
description	Yixuan Wang, Sisi Cao, Kaiyue Yu, Fengdie Yang, Xiuming Yu, Yuanhao Zhai, Chuanbin Wu, Yuehong XuDepartment of Pharmaceutics, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, People’s Republic of ChinaBackground: Topical application of tacrolimus (FK506) was effective in treating atopic dermatitis (AD); however, the therapeutic efficiency is hampered by its poor penetration into the skin and local side effects of transient irritation symptoms with a burning sensation, a feeling of warmth or heat. Menthol and camphor have been widely used in topical compound formulations for adjunctive pharmacotherapy for antipruritics and analgesics owing to their cool nature, and both present skin penetration enhancing effects. Moreover, they can form a liquid eutectic oil to solubilize hydrophobic drugs.Purpose: Taking advantages of menthol/camphor eutectic (MCE), this work aims to integrate FK506 into MCE to construct a microemulsion system, i.e., FK506 MCE ME, which simultaneously enhances the percutaneous delivery and treatment efficacy, while reduces the side effects of FK506.Methods: The formulation of FK506 MCE ME was optimized and characterized. Different formulations containing FK506 were topically administered to treat 1–chloro–2, 4–dinitrobenzene (DNCB)-induced murine AD.Results: MCE solubilized FK506. FK506 in MCE ME penetrated skin in vitro more than in the commercial ointment, and MCE predominantly exerted the enhancing effects in MCE ME. FK506 MCE ME or FK506 MCE ME gel had greater effects on clinical symptoms, histological analysis, and IgE than did commercial FK506. The anti-pruritic and down-regulation of substance P effects of MCE ME vehicle mitigated the side effects of FK506 application.Conclusion: MCE ME presented the excellent properties of simultaneously enhancing the percutaneous delivery and treatment efficacy, while reducing the side effects of FK506 for AD. Therefore, MCE ME is a promising nanoscale system for FK506 to effectively treating AD with low irritation and high medication adherence.Chemical compounds studied in this article: Tacrolimus (PubChem CID: 445643); menthol (PubChem CID: 1254); camphor (PubChem CID: 2537)Keywords: tacrolimus, microemulsion, menthol, camphor, eutectic, atopic dermatitis, percutaneous delivery
format	article
author	Wang Y Cao S Yu K Yang F Yu X Zhai Y Wu C Xu Y
author_facet	Wang Y Cao S Yu K Yang F Yu X Zhai Y Wu C Xu Y
author_sort	Wang Y
title	Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects
title_short	Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects
title_full	Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects
title_fullStr	Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects
title_full_unstemmed	Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects
title_sort	integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/15375b15b31a4dd3a35b08731bec99b5
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Integrating tacrolimus into eutectic oil-based microemulsion for atopic dermatitis: simultaneously enhancing percutaneous delivery and treatment efficacy with relieving side effects

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