In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion

Yong-Tai Zhang, Zhe-Bin Huang, Su-Juan Zhang, Ji-Hui Zhao, Zhi Wang, Ying Liu, Nian-Ping FengDepartment of Pharmaceutics, Shanghai University of Traditional Chinese Medicine, Shanghai, The People&#39;s Republic of ChinaObjective: To investigate the cellular uptake of evodiamine and rutaecarp...

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Autores principales:	Zhang YT, Huang ZB, Zhang SJ, Zhao JH, Wang Z, Liu Y, Feng NP
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7dc1f3db99fd4098989f3ba24fa5d4e0
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spelling	oai:doaj.org-article:7dc1f3db99fd4098989f3ba24fa5d4e02021-12-02T02:27:10ZIn vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion1176-91141178-2013https://doaj.org/article/7dc1f3db99fd4098989f3ba24fa5d4e02012-05-01T00:00:00Zhttp://www.dovepress.com/in-vitro-cellular-uptake-of-evodiamine-and-rutaecarpine-using-a-microe-a9921https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Yong-Tai Zhang, Zhe-Bin Huang, Su-Juan Zhang, Ji-Hui Zhao, Zhi Wang, Ying Liu, Nian-Ping FengDepartment of Pharmaceutics, Shanghai University of Traditional Chinese Medicine, Shanghai, The People&#39;s Republic of ChinaObjective: To investigate the cellular uptake of evodiamine and rutaecarpine in a microemulsion in comparison with aqueous suspensions and tinctures.Materials and methods: A microemulsion was prepared using the dropwise addition method. Mouse skin fibroblasts were cultured in vitro to investigate the optimal conditions for evodiamine and rutaecarpine uptake with different drug concentrations and administration times. Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions. Rhodamine B labeling and laser scanning confocal microscopy (LSCM) were used to explore the distribution of fluorochrome transferred with the microemulsion in fibroblasts. Cellular morphology was also investigated, using optical microscopy to evaluate microemulsion-induced cellular toxicity.Results: The maximum cellular drug uptake amounts were obtained with a 20% concentration (v/v) of microemulsion and an 8 hour administration time. Drug uptake by mouse skin fibroblasts was lowest when the drugs were loaded in microemulsion. After incubation with rhodamine B-labeled microemulsion for 8 hours, the highest fluorescence intensity was achieved, and the fluorochrome was primarily distributed in the cytochylema. No obvious cellular morphologic changes were observed with the administration of either the microemulsion or the aqueous suspension; for the tincture group, however, massive cellular necrocytosis was observed.Conclusion: The lower cellular uptake with microemulsion may be due to the fact that most of the drug loaded in the microemulsion vehicle was transported via the intercellular space, while a small quantity of free drug (released from the vehicle) was ingested through transmembrane transport. Mouse skin fibroblasts rarely endocytosed evodiamine and rutaecarpine with a microemulsion as the vehicle. The microemulsion had no obvious effect on cellular morphology, suggesting there is little or no cellular toxicity associated with the administration of microemulsion on mouse skin fibroblasts.Keywords: mouse skin fibroblasts, evodiamine, rutaecarpine, microemulsion, cellular uptake, in vitroZhang YTHuang ZBZhang SJZhao JHWang ZLiu YFeng NPDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 2465-2472 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Zhang YT Huang ZB Zhang SJ Zhao JH Wang Z Liu Y Feng NP In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
description	Yong-Tai Zhang, Zhe-Bin Huang, Su-Juan Zhang, Ji-Hui Zhao, Zhi Wang, Ying Liu, Nian-Ping FengDepartment of Pharmaceutics, Shanghai University of Traditional Chinese Medicine, Shanghai, The People&#39;s Republic of ChinaObjective: To investigate the cellular uptake of evodiamine and rutaecarpine in a microemulsion in comparison with aqueous suspensions and tinctures.Materials and methods: A microemulsion was prepared using the dropwise addition method. Mouse skin fibroblasts were cultured in vitro to investigate the optimal conditions for evodiamine and rutaecarpine uptake with different drug concentrations and administration times. Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions. Rhodamine B labeling and laser scanning confocal microscopy (LSCM) were used to explore the distribution of fluorochrome transferred with the microemulsion in fibroblasts. Cellular morphology was also investigated, using optical microscopy to evaluate microemulsion-induced cellular toxicity.Results: The maximum cellular drug uptake amounts were obtained with a 20% concentration (v/v) of microemulsion and an 8 hour administration time. Drug uptake by mouse skin fibroblasts was lowest when the drugs were loaded in microemulsion. After incubation with rhodamine B-labeled microemulsion for 8 hours, the highest fluorescence intensity was achieved, and the fluorochrome was primarily distributed in the cytochylema. No obvious cellular morphologic changes were observed with the administration of either the microemulsion or the aqueous suspension; for the tincture group, however, massive cellular necrocytosis was observed.Conclusion: The lower cellular uptake with microemulsion may be due to the fact that most of the drug loaded in the microemulsion vehicle was transported via the intercellular space, while a small quantity of free drug (released from the vehicle) was ingested through transmembrane transport. Mouse skin fibroblasts rarely endocytosed evodiamine and rutaecarpine with a microemulsion as the vehicle. The microemulsion had no obvious effect on cellular morphology, suggesting there is little or no cellular toxicity associated with the administration of microemulsion on mouse skin fibroblasts.Keywords: mouse skin fibroblasts, evodiamine, rutaecarpine, microemulsion, cellular uptake, in vitro
format	article
author	Zhang YT Huang ZB Zhang SJ Zhao JH Wang Z Liu Y Feng NP
author_facet	Zhang YT Huang ZB Zhang SJ Zhao JH Wang Z Liu Y Feng NP
author_sort	Zhang YT
title	In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_short	In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_full	In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_fullStr	In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_full_unstemmed	In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_sort	in vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/7dc1f3db99fd4098989f3ba24fa5d4e0
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In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion

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