Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion

Yong-Tai Zhang, Ji-Hui Zhao, Su-Juan Zhang, Yang-Zi Zhong, Zhi Wang, Ying Liu, Feng Shi, Nian-Ping FengSchool of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People&rsquo;s Republic of ChinaObjective: The purpose of this study was to improve skin permeation of evo...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Zhong YT, Zhao JH, Zhang SJ, Zhong YZ, Wang Z, Liu Y, Shi F, Feng NP
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/8d2625c80f4e41158d93973f6dc70f67
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:8d2625c80f4e41158d93973f6dc70f67
record_format	dspace
spelling	oai:doaj.org-article:8d2625c80f4e41158d93973f6dc70f672021-12-02T09:08:47ZEnhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion1176-91141178-2013https://doaj.org/article/8d2625c80f4e41158d93973f6dc70f672011-10-01T00:00:00Zhttp://www.dovepress.com/enhanced-transdermal-delivery-of-evodiamine-and-rutaecarpine-using-mic-a8533https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Yong-Tai Zhang, Ji-Hui Zhao, Su-Juan Zhang, Yang-Zi Zhong, Zhi Wang, Ying Liu, Feng Shi, Nian-Ping FengSchool of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People&rsquo;s Republic of ChinaObjective: The purpose of this study was to improve skin permeation of evodiamine and rutaecarpine for transdermal delivery with microemulsion as vehicle and investigate real-time cutaneous absorption of the drugs via in vivo microdialysis.Methods: Pseudoternary phase diagrams were constructed to evaluate microemulsion regions with various surfactants and cosurfactants. Nine formulations of oil in water microemulsions were selected as vehicles for assessing skin permeation of evodiamine and rutaecarpine in ex vivo transdermal experiments. With a microdialysis hollow fiber membrane implanted in the skin beneath the site of topical drug administration, dialysis sampling was maintained for 10 hours and the samples were detected directly by high performance liquid chromatography. Real-time concentrations of the drugs in rat skin were investigated and compared with those of conventional formulations, such as ointment and tincture. Furthermore, the drugs were applied to various regions of the skin using microemulsion as vehicle.Results: In ex vivo transdermal experiments, cutaneous fluxes of evodiamine and rutaecarpine microemulsions were 2.55-fold to 11.36-fold and 1.17-fold to 6.33-fold higher, respectively, than those of aqueous suspensions. Different drug loadings, microemulsion water content, and transdermal enhancers markedly influenced the permeation of evodiamine and rutaecarpine. In microemulsion application with in vivo microdialysis, the maximum concentration of the drugs (evodiamine: 18.23 &plusmn; 1.54 ng/mL; rutaecarpine: 16.04 &plusmn; 0.69 ng/mL) were the highest, and the area under the curve0&ndash;t of evodiamine and rutaecarpine was 1.52-fold and 2.27-fold higher than ointment and 3.06-fold and 4.23-fold higher than tincture, respectively. A greater amount of drugs penetrated through and was absorbed by rat abdominal skin than shoulder and chest, and a reservoir in the skin was found to supply drugs even after the microemulsion was withdrawn.Conclusion: Compared to conventional formulations, higher cutaneous fluxes of evodiamine and rutaecarpine were achieved with microemulsion. Based on this novel transdermal delivery, the transdermal route was effective for the administration of the two active alkaloids.Keywords: microemulsion, evodiamine, rutaecarpine, transdermal delivery, microdialysisZhong YTZhao JHZhang SJZhong YZWang ZLiu YShi FFeng NPDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 2469-2482 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Zhong YT Zhao JH Zhang SJ Zhong YZ Wang Z Liu Y Shi F Feng NP Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion
description	Yong-Tai Zhang, Ji-Hui Zhao, Su-Juan Zhang, Yang-Zi Zhong, Zhi Wang, Ying Liu, Feng Shi, Nian-Ping FengSchool of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People&rsquo;s Republic of ChinaObjective: The purpose of this study was to improve skin permeation of evodiamine and rutaecarpine for transdermal delivery with microemulsion as vehicle and investigate real-time cutaneous absorption of the drugs via in vivo microdialysis.Methods: Pseudoternary phase diagrams were constructed to evaluate microemulsion regions with various surfactants and cosurfactants. Nine formulations of oil in water microemulsions were selected as vehicles for assessing skin permeation of evodiamine and rutaecarpine in ex vivo transdermal experiments. With a microdialysis hollow fiber membrane implanted in the skin beneath the site of topical drug administration, dialysis sampling was maintained for 10 hours and the samples were detected directly by high performance liquid chromatography. Real-time concentrations of the drugs in rat skin were investigated and compared with those of conventional formulations, such as ointment and tincture. Furthermore, the drugs were applied to various regions of the skin using microemulsion as vehicle.Results: In ex vivo transdermal experiments, cutaneous fluxes of evodiamine and rutaecarpine microemulsions were 2.55-fold to 11.36-fold and 1.17-fold to 6.33-fold higher, respectively, than those of aqueous suspensions. Different drug loadings, microemulsion water content, and transdermal enhancers markedly influenced the permeation of evodiamine and rutaecarpine. In microemulsion application with in vivo microdialysis, the maximum concentration of the drugs (evodiamine: 18.23 &plusmn; 1.54 ng/mL; rutaecarpine: 16.04 &plusmn; 0.69 ng/mL) were the highest, and the area under the curve0&ndash;t of evodiamine and rutaecarpine was 1.52-fold and 2.27-fold higher than ointment and 3.06-fold and 4.23-fold higher than tincture, respectively. A greater amount of drugs penetrated through and was absorbed by rat abdominal skin than shoulder and chest, and a reservoir in the skin was found to supply drugs even after the microemulsion was withdrawn.Conclusion: Compared to conventional formulations, higher cutaneous fluxes of evodiamine and rutaecarpine were achieved with microemulsion. Based on this novel transdermal delivery, the transdermal route was effective for the administration of the two active alkaloids.Keywords: microemulsion, evodiamine, rutaecarpine, transdermal delivery, microdialysis
format	article
author	Zhong YT Zhao JH Zhang SJ Zhong YZ Wang Z Liu Y Shi F Feng NP
author_facet	Zhong YT Zhao JH Zhang SJ Zhong YZ Wang Z Liu Y Shi F Feng NP
author_sort	Zhong YT
title	Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion
title_short	Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion
title_full	Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion
title_fullStr	Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion
title_full_unstemmed	Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion
title_sort	enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/8d2625c80f4e41158d93973f6dc70f67
work_keys_str_mv	AT zhongyt enhancedtransdermaldeliveryofevodiamineandrutaecarpineusingmicroemulsion AT zhaojh enhancedtransdermaldeliveryofevodiamineandrutaecarpineusingmicroemulsion AT zhangsj enhancedtransdermaldeliveryofevodiamineandrutaecarpineusingmicroemulsion AT zhongyz enhancedtransdermaldeliveryofevodiamineandrutaecarpineusingmicroemulsion AT wangz enhancedtransdermaldeliveryofevodiamineandrutaecarpineusingmicroemulsion AT liuy enhancedtransdermaldeliveryofevodiamineandrutaecarpineusingmicroemulsion AT shif enhancedtransdermaldeliveryofevodiamineandrutaecarpineusingmicroemulsion AT fengnp enhancedtransdermaldeliveryofevodiamineandrutaecarpineusingmicroemulsion
_version_	1718398256929570816

Enhanced transdermal delivery of evodiamine and rutaecarpine using microemulsion

Ejemplares similares