Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose

Kaiyue Yu, Yixuan Wang, Tao Wan, Yuanhao Zhai, Sisi Cao, Wenyi Ruan, Chuanbin Wu, Yuehong Xu School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, People’s Republic of China Background: Topical application of tacrolimus (FK506) was effective in the treatment of atopic der...

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Autores principales:	Yu K, Wang Y, Wan T, Zhai Y, Cao S, Ruan W, Wu C, Xu Y
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	tacrolimus chitosan nanoparticles nicotinamide atopic dermatitis percutaneous delivery reducing dose. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/2a9b6661cdec4da9ac63694d1756c93e
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spelling	oai:doaj.org-article:2a9b6661cdec4da9ac63694d1756c93e2021-12-02T02:48:32ZTacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose1178-2013https://doaj.org/article/2a9b6661cdec4da9ac63694d1756c93e2017-12-01T00:00:00Zhttps://www.dovepress.com/tacrolimus-nanoparticles-based-on-chitosan-combined-with-nicotinamide--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Kaiyue Yu, Yixuan Wang, Tao Wan, Yuanhao Zhai, Sisi Cao, Wenyi Ruan, Chuanbin Wu, Yuehong Xu School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, People’s Republic of China Background: Topical application of tacrolimus (FK506) was effective in the treatment of atopic dermatitis (AD); however, adverse effects frequently occurred with the increase of FK506 dose during long–term treatment.Objective: The objective of this project was to develop a hybrid skin targeting system encapsulating FK506 based on nicotinamide (NIC) and chitosan nanoparticles (CS–NPs), ie, FK506–NIC–CS–NPs, which took advantages of both of NIC and CS–NPs to obtain the synergetic effects of percutaneous delivery and treatment efficacy enhancement along with dose reduction.Methods: The formulation of FK506–NIC–CS–NPs was optimized and characterized. In vitro and in vivo skin permeation studies were performed. AD–like skin lesions were constructed with BALB/c mice by 1–chloro–2, 4–dinitrobenzene (DNCB)–induced, and FK506–NIC–CS–NPs containing different dose of FK506 were topically administered to treat AD–like skin lesions in comparison with Protopic.Results: NIC was found to significantly increase the FK506 EE to 92.2% by CS–NPs. In comparison with commercial FK506 ointment (Protopic), in vitro and in vivo skin permeation studies demonstrated that NIC–CS–NPs system significantly enhanced FK506 permeation through and into the skin, and deposited more FK506 into the skin. The treatment efficacy on clinical symptoms, histological analysis, and molecular biology of the AD–mice demonstrated that NIC–CS–NPs with ~1/3 dose of FK506 of Protopic was superior to that of Protopic, and NIC–CS–NPs vehicle exhibited the adjuvant therapy and moderate anti–AD effects.Conclusion: The system of NIC–CS–NPs enhances the permeability of FK506, plays an adjuvant role in anti-AD, reduces the dose of FK506 in treating AD, and is therefore a promising nanoscale system of FK506 for the effective treatment of AD. Keywords: tacrolimus, chitosan, nanoparticles, nicotinamide, atopic dermatitis, percutaneous delivery, reducing doseYu KWang YWan TZhai YCao SRuan WWu CXu YDove Medical Pressarticletacrolimuschitosannanoparticlesnicotinamideatopic dermatitispercutaneous deliveryreducing dose.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 129-142 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	tacrolimus chitosan nanoparticles nicotinamide atopic dermatitis percutaneous delivery reducing dose. Medicine (General) R5-920
spellingShingle	tacrolimus chitosan nanoparticles nicotinamide atopic dermatitis percutaneous delivery reducing dose. Medicine (General) R5-920 Yu K Wang Y Wan T Zhai Y Cao S Ruan W Wu C Xu Y Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose
description	Kaiyue Yu, Yixuan Wang, Tao Wan, Yuanhao Zhai, Sisi Cao, Wenyi Ruan, Chuanbin Wu, Yuehong Xu School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, People’s Republic of China Background: Topical application of tacrolimus (FK506) was effective in the treatment of atopic dermatitis (AD); however, adverse effects frequently occurred with the increase of FK506 dose during long–term treatment.Objective: The objective of this project was to develop a hybrid skin targeting system encapsulating FK506 based on nicotinamide (NIC) and chitosan nanoparticles (CS–NPs), ie, FK506–NIC–CS–NPs, which took advantages of both of NIC and CS–NPs to obtain the synergetic effects of percutaneous delivery and treatment efficacy enhancement along with dose reduction.Methods: The formulation of FK506–NIC–CS–NPs was optimized and characterized. In vitro and in vivo skin permeation studies were performed. AD–like skin lesions were constructed with BALB/c mice by 1–chloro–2, 4–dinitrobenzene (DNCB)–induced, and FK506–NIC–CS–NPs containing different dose of FK506 were topically administered to treat AD–like skin lesions in comparison with Protopic.Results: NIC was found to significantly increase the FK506 EE to 92.2% by CS–NPs. In comparison with commercial FK506 ointment (Protopic), in vitro and in vivo skin permeation studies demonstrated that NIC–CS–NPs system significantly enhanced FK506 permeation through and into the skin, and deposited more FK506 into the skin. The treatment efficacy on clinical symptoms, histological analysis, and molecular biology of the AD–mice demonstrated that NIC–CS–NPs with ~1/3 dose of FK506 of Protopic was superior to that of Protopic, and NIC–CS–NPs vehicle exhibited the adjuvant therapy and moderate anti–AD effects.Conclusion: The system of NIC–CS–NPs enhances the permeability of FK506, plays an adjuvant role in anti-AD, reduces the dose of FK506 in treating AD, and is therefore a promising nanoscale system of FK506 for the effective treatment of AD. Keywords: tacrolimus, chitosan, nanoparticles, nicotinamide, atopic dermatitis, percutaneous delivery, reducing dose
format	article
author	Yu K Wang Y Wan T Zhai Y Cao S Ruan W Wu C Xu Y
author_facet	Yu K Wang Y Wan T Zhai Y Cao S Ruan W Wu C Xu Y
author_sort	Yu K
title	Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose
title_short	Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose
title_full	Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose
title_fullStr	Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose
title_full_unstemmed	Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose
title_sort	tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/2a9b6661cdec4da9ac63694d1756c93e
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Tacrolimus nanoparticles based on chitosan combined with nicotinamide: enhancing percutaneous delivery and treatment efficacy for atopic dermatitis and reducing dose

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