One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine

Jing-Wen Luo, Zhi-Rong Zhang, Tao Gong, Yao Fu Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, People’s Republic of China Abstract: Our study aimed to develop a self-assembled nanomice...

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Autores principales:	Luo JW, Zhang ZR, Gong T, Fu Y
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Nanomicelles Self-assembly Nimodipine Oral bioavailability Transport mechanism Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/24122edfb3354ad5955e1f0ce82921e0
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spelling	oai:doaj.org-article:24122edfb3354ad5955e1f0ce82921e02021-12-02T02:29:09ZOne-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine1178-2013https://doaj.org/article/24122edfb3354ad5955e1f0ce82921e02016-03-01T00:00:00Zhttps://www.dovepress.com/one-step-self-assembled-nanomicelles-for-improving-the-oral-bioavailab-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Jing-Wen Luo, Zhi-Rong Zhang, Tao Gong, Yao Fu Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, People’s Republic of China Abstract: Our study aimed to develop a self-assembled nanomicelle for oral administration of nimodipine (NIM) with poor water solubility. Using Solutol® HS15, the NIM-loaded self-assembled nanomicelles displayed a near-spherical morphology with a narrow size distribution of 12.57±0.21 nm (polydispersity index =0.071±0.011). Compared with Nimotop® (NIM tablets), the intestinal absorption of NIM from NIM nanomicelle in rats was improved by 3.13- and 2.25-fold in duodenum and jejunum at 1 hour after oral administration. The cellular transport of NIM nanomicelle in Caco-2 cell monolayers was significantly enhanced compared to that of Nimotop®. Regarding the transport pathways, clathrin, lipid raft/caveolae, and macropinocytosis mediated the cell uptake of NIM nanomicelles, while P-glycoprotein and endoplasmic reticulum/Golgi complex (ER/Golgi) pathways were involved in exocytosis. Pharmacokinetic studies in our research laboratory have showed that the area under the plasma concentration–time curve (AUC0–∞) of NIM nanomicelles was 3.72-fold that of Nimotop® via oral administration in rats. Moreover, the NIM concentration in the brain from NIM nanomicelles was dramatically improved. Therefore, Solutol® HS15-based self-assembled nanomicelles represent a promising delivery system to enhance the oral bioavailability of NIM. Keywords: nanomicelles, stability, nimodipine, oral bioavailability, transport mechanism Luo JWZhang ZRGong TFu YDove Medical PressarticleNanomicellesSelf-assemblyNimodipineOral bioavailabilityTransport mechanismMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 1051-1065 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Nanomicelles Self-assembly Nimodipine Oral bioavailability Transport mechanism Medicine (General) R5-920
spellingShingle	Nanomicelles Self-assembly Nimodipine Oral bioavailability Transport mechanism Medicine (General) R5-920 Luo JW Zhang ZR Gong T Fu Y One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine
description	Jing-Wen Luo, Zhi-Rong Zhang, Tao Gong, Yao Fu Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, People’s Republic of China Abstract: Our study aimed to develop a self-assembled nanomicelle for oral administration of nimodipine (NIM) with poor water solubility. Using Solutol® HS15, the NIM-loaded self-assembled nanomicelles displayed a near-spherical morphology with a narrow size distribution of 12.57±0.21 nm (polydispersity index =0.071±0.011). Compared with Nimotop® (NIM tablets), the intestinal absorption of NIM from NIM nanomicelle in rats was improved by 3.13- and 2.25-fold in duodenum and jejunum at 1 hour after oral administration. The cellular transport of NIM nanomicelle in Caco-2 cell monolayers was significantly enhanced compared to that of Nimotop®. Regarding the transport pathways, clathrin, lipid raft/caveolae, and macropinocytosis mediated the cell uptake of NIM nanomicelles, while P-glycoprotein and endoplasmic reticulum/Golgi complex (ER/Golgi) pathways were involved in exocytosis. Pharmacokinetic studies in our research laboratory have showed that the area under the plasma concentration–time curve (AUC0–∞) of NIM nanomicelles was 3.72-fold that of Nimotop® via oral administration in rats. Moreover, the NIM concentration in the brain from NIM nanomicelles was dramatically improved. Therefore, Solutol® HS15-based self-assembled nanomicelles represent a promising delivery system to enhance the oral bioavailability of NIM. Keywords: nanomicelles, stability, nimodipine, oral bioavailability, transport mechanism
format	article
author	Luo JW Zhang ZR Gong T Fu Y
author_facet	Luo JW Zhang ZR Gong T Fu Y
author_sort	Luo JW
title	One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine
title_short	One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine
title_full	One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine
title_fullStr	One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine
title_full_unstemmed	One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine
title_sort	one-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/24122edfb3354ad5955e1f0ce82921e0
work_keys_str_mv	AT luojw onestepselfassemblednanomicellesforimprovingtheoralbioavailabilityofnimodipine AT zhangzr onestepselfassemblednanomicellesforimprovingtheoralbioavailabilityofnimodipine AT gongt onestepselfassemblednanomicellesforimprovingtheoralbioavailabilityofnimodipine AT fuy onestepselfassemblednanomicellesforimprovingtheoralbioavailabilityofnimodipine
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One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine

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