Transdermal delivery of nobiletin using ionic liquids

Abstract Nobiletin (NOB), a flavonoid, has extremely low water solubility and low oral bioavailability; however, despite these problems, various physiological effects have been investigated in vitro. In the present study, we investigated the transdermal delivery of NOB using choline and geranic acid...

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Autores principales:	Tadashi Hattori, Hiroki Tagawa, Makoto Inai, Toshiyuki Kan, Shin-ichiro Kimura, Shigeru Itai, Samir Mitragotri, Yasunori Iwao
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2019
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/63fa0dea7c1444fd9daa6d6a0abd59dc
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spelling	oai:doaj.org-article:63fa0dea7c1444fd9daa6d6a0abd59dc2021-12-02T13:35:11ZTransdermal delivery of nobiletin using ionic liquids10.1038/s41598-019-56731-12045-2322https://doaj.org/article/63fa0dea7c1444fd9daa6d6a0abd59dc2019-12-01T00:00:00Zhttps://doi.org/10.1038/s41598-019-56731-1https://doaj.org/toc/2045-2322Abstract Nobiletin (NOB), a flavonoid, has extremely low water solubility and low oral bioavailability; however, despite these problems, various physiological effects have been investigated in vitro. In the present study, we investigated the transdermal delivery of NOB using choline and geranic acid (CAGE), which is a biocompatible material that has been reported to be a promising transdermal delivery approach. The feasibility was evaluated by a set of in vitro and in vivo tests. A solubility evaluation demonstrated that CAGE induced excellent solubility of NOB induced by multipoint hydrogen bonding between NOB and CAGE. In vitro transdermal tests using a Franz diffusion cell showed that CAGE was effective in enhancing transdermal absorption of NOB, compared to other penetration enhancers. Subsequent in vivo tests demonstrated that CAGE significantly improved area under the concentration-time curve of NOB in vivo and NOB/CAGE sample showed 20-times higher bioavailability than oral administration of NOB crystal. Furthermore, NOB/CAGE sample also showed significant drops of the blood glucose level in rats derived from hypoglycemic activity of NOB. Thus, transdermal administration of NOB using CAGE was shown to be feasible, which indicates that the use of CAGE may be adapted for other flavonoids that also show both low water solubility and low permeability.Tadashi HattoriHiroki TagawaMakoto InaiToshiyuki KanShin-ichiro KimuraShigeru ItaiSamir MitragotriYasunori IwaoNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 9, Iss 1, Pp 1-11 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Tadashi Hattori Hiroki Tagawa Makoto Inai Toshiyuki Kan Shin-ichiro Kimura Shigeru Itai Samir Mitragotri Yasunori Iwao Transdermal delivery of nobiletin using ionic liquids
description	Abstract Nobiletin (NOB), a flavonoid, has extremely low water solubility and low oral bioavailability; however, despite these problems, various physiological effects have been investigated in vitro. In the present study, we investigated the transdermal delivery of NOB using choline and geranic acid (CAGE), which is a biocompatible material that has been reported to be a promising transdermal delivery approach. The feasibility was evaluated by a set of in vitro and in vivo tests. A solubility evaluation demonstrated that CAGE induced excellent solubility of NOB induced by multipoint hydrogen bonding between NOB and CAGE. In vitro transdermal tests using a Franz diffusion cell showed that CAGE was effective in enhancing transdermal absorption of NOB, compared to other penetration enhancers. Subsequent in vivo tests demonstrated that CAGE significantly improved area under the concentration-time curve of NOB in vivo and NOB/CAGE sample showed 20-times higher bioavailability than oral administration of NOB crystal. Furthermore, NOB/CAGE sample also showed significant drops of the blood glucose level in rats derived from hypoglycemic activity of NOB. Thus, transdermal administration of NOB using CAGE was shown to be feasible, which indicates that the use of CAGE may be adapted for other flavonoids that also show both low water solubility and low permeability.
format	article
author	Tadashi Hattori Hiroki Tagawa Makoto Inai Toshiyuki Kan Shin-ichiro Kimura Shigeru Itai Samir Mitragotri Yasunori Iwao
author_facet	Tadashi Hattori Hiroki Tagawa Makoto Inai Toshiyuki Kan Shin-ichiro Kimura Shigeru Itai Samir Mitragotri Yasunori Iwao
author_sort	Tadashi Hattori
title	Transdermal delivery of nobiletin using ionic liquids
title_short	Transdermal delivery of nobiletin using ionic liquids
title_full	Transdermal delivery of nobiletin using ionic liquids
title_fullStr	Transdermal delivery of nobiletin using ionic liquids
title_full_unstemmed	Transdermal delivery of nobiletin using ionic liquids
title_sort	transdermal delivery of nobiletin using ionic liquids
publisher	Nature Portfolio
publishDate	2019
url	https://doaj.org/article/63fa0dea7c1444fd9daa6d6a0abd59dc
work_keys_str_mv	AT tadashihattori transdermaldeliveryofnobiletinusingionicliquids AT hirokitagawa transdermaldeliveryofnobiletinusingionicliquids AT makotoinai transdermaldeliveryofnobiletinusingionicliquids AT toshiyukikan transdermaldeliveryofnobiletinusingionicliquids AT shinichirokimura transdermaldeliveryofnobiletinusingionicliquids AT shigeruitai transdermaldeliveryofnobiletinusingionicliquids AT samirmitragotri transdermaldeliveryofnobiletinusingionicliquids AT yasunoriiwao transdermaldeliveryofnobiletinusingionicliquids
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Transdermal delivery of nobiletin using ionic liquids

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