Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

Li-Na Shen,1 Yong-Tai Zhang,1 Qin Wang,2 Ling Xu,2 Nian-Ping Feng11Department of Pharmaceutical Sciences, 2Department of Oncology, Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of ChinaAbstract: The aims of the present study were to inv...

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Autores principales:	Shen LN, Zhang YT, Wang Q, Xu L, Feng NP
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/9335cb7a858d4d34952cb49420cf3277
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spelling	oai:doaj.org-article:9335cb7a858d4d34952cb49420cf32772021-12-02T03:58:33ZPreparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis1178-2013https://doaj.org/article/9335cb7a858d4d34952cb49420cf32772014-07-01T00:00:00Zhttp://www.dovepress.com/preparation-and-evaluation-of-microemulsion-based-transdermal-delivery-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Li-Na Shen,1 Yong-Tai Zhang,1 Qin Wang,2 Ling Xu,2 Nian-Ping Feng11Department of Pharmaceutical Sciences, 2Department of Oncology, Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of ChinaAbstract: The aims of the present study were to investigate the skin permeation and cellular uptake of a microemulsion (ME) containing total flavone of rhizoma arisaematis (TFRA), and to evaluate its effects on skin structure. Pseudo-ternary phase diagrams were constructed to evaluate ME regions with various surfactants and cosurfactants. Eight formulations of oil-in-water MEs were selected as vehicles, and in vitro skin-permeation experiments were performed to optimize the ME formulation and to evaluate its permeability, in comparison to that of an aqueous suspension. Laser scanning confocal microscopy and fluorescent-activated cell sorting were used to explore the cellular uptake of rhodamine 110-labeled ME in human epidermal keratinocytes (HaCaT) and human embryonic skin fibroblasts (CCC-ESF-1). The structure of stratum corneum treated with ME was observed using a scanning electron microscope. Furthermore, skin irritation was tested to evaluate the safety of ME. ME formulated with 4% ethyl oleate (weight/weight), 18% Cremophor EL® (weight/weight), and 18% Transcutol® P, with 1% Azone to enhance permeation, showed good skin permeability. ME-associated transdermal fluxes of schaftoside and isoschaftoside, two major effective constituents of TFRA, were 3.72-fold and 5.92-fold higher, respectively, than those achieved using aqueous suspensions. In contrast, in vitro studies revealed that uptake by HaCaT and CCC-ESF-1 cells was lower with ME than with an aqueous suspension. Stratum corneum loosening and shedding was observed in nude mouse skin treated with ME, although ME produced no observable skin irritation in rabbits. These findings indicated that ME enhanced transdermal TFRA delivery effectively and showed good biocompatibility with skin tissue.Keywords: microemulsion, transdermal, nanocarrier, cellular uptakeShen LNZhang YTWang QXu LFeng NPDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 3453-3464 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Shen LN Zhang YT Wang Q Xu L Feng NP Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis
description	Li-Na Shen,1 Yong-Tai Zhang,1 Qin Wang,2 Ling Xu,2 Nian-Ping Feng11Department of Pharmaceutical Sciences, 2Department of Oncology, Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of ChinaAbstract: The aims of the present study were to investigate the skin permeation and cellular uptake of a microemulsion (ME) containing total flavone of rhizoma arisaematis (TFRA), and to evaluate its effects on skin structure. Pseudo-ternary phase diagrams were constructed to evaluate ME regions with various surfactants and cosurfactants. Eight formulations of oil-in-water MEs were selected as vehicles, and in vitro skin-permeation experiments were performed to optimize the ME formulation and to evaluate its permeability, in comparison to that of an aqueous suspension. Laser scanning confocal microscopy and fluorescent-activated cell sorting were used to explore the cellular uptake of rhodamine 110-labeled ME in human epidermal keratinocytes (HaCaT) and human embryonic skin fibroblasts (CCC-ESF-1). The structure of stratum corneum treated with ME was observed using a scanning electron microscope. Furthermore, skin irritation was tested to evaluate the safety of ME. ME formulated with 4% ethyl oleate (weight/weight), 18% Cremophor EL® (weight/weight), and 18% Transcutol® P, with 1% Azone to enhance permeation, showed good skin permeability. ME-associated transdermal fluxes of schaftoside and isoschaftoside, two major effective constituents of TFRA, were 3.72-fold and 5.92-fold higher, respectively, than those achieved using aqueous suspensions. In contrast, in vitro studies revealed that uptake by HaCaT and CCC-ESF-1 cells was lower with ME than with an aqueous suspension. Stratum corneum loosening and shedding was observed in nude mouse skin treated with ME, although ME produced no observable skin irritation in rabbits. These findings indicated that ME enhanced transdermal TFRA delivery effectively and showed good biocompatibility with skin tissue.Keywords: microemulsion, transdermal, nanocarrier, cellular uptake
format	article
author	Shen LN Zhang YT Wang Q Xu L Feng NP
author_facet	Shen LN Zhang YT Wang Q Xu L Feng NP
author_sort	Shen LN
title	Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis
title_short	Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis
title_full	Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis
title_fullStr	Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis
title_full_unstemmed	Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis
title_sort	preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/9335cb7a858d4d34952cb49420cf3277
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Preparation and evaluation of microemulsion-based transdermal delivery of total flavone of rhizoma arisaematis

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