Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement

Rong Lu,1 Shan Liu,1 Qilin Wang,1 Xia Li1,2 1School of Ocean, Shandong University, Weihai, 2School of Pharmaceutical Sciences, Shandong University, Jinan, People’s Republic of China Abstract: Oral administration remains a significant challenge in regards to drugs with serious solu...

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Autores principales: Lu R, Liu S, Wang Q, Li X
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Lenguaje:EN
Publicado: Dove Medical Press 2015
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Acceso en línea:https://doaj.org/article/f24256f143504c2587c7b84e93898fc7
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spelling oai:doaj.org-article:f24256f143504c2587c7b84e93898fc72021-12-02T02:42:32ZNanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement1178-2013https://doaj.org/article/f24256f143504c2587c7b84e93898fc72015-07-01T00:00:00Zhttp://www.dovepress.com/nanoemulsions-as-novel-oral-carriers-of-stiripentol-insights-into-the--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Rong Lu,1 Shan Liu,1 Qilin Wang,1 Xia Li1,2 1School of Ocean, Shandong University, Weihai, 2School of Pharmaceutical Sciences, Shandong University, Jinan, People’s Republic of China Abstract: Oral administration remains a significant challenge in regards to drugs with serious solubility and stability issues. This article aimed to investigate the suitability of nanoemulsions as oral carriers of stiripentol (STP), an acid-labile drug, for enhancement of stability and bioavailability. STP-loaded nanoemulsions (STP-NEs) were prepared by using a solvent-diffusion/ultrasonication technique. STP-NEs were characterized in a variety of ways such as by particle size, entrapment efficiency, in vitro drug release, and transmission electron microscopy. A bioavailability study was performed in rats after oral administration of either STP-NEs, or commercial formulation (Diacomit®). The resultant nanoemulsions were 146.6 nm in particle size with an entrapment efficiency of 99.47%. It was demonstrated that nanoemulsions significantly improved the biochemical stability and bioavailability of STP. The bioavailability of STP-NEs was up to 206.2% relative to Diacomit®. Nanoemulsions fabricated from poly(ethylene glycol) monooleate/medium-chain triglycerides exhibited excellent performance in drug stabilization and absorption enhancement. The results suggest that STP-NEs are a promising means to solve the problems associated with stability and solubility of STP. Keywords: stiripentol, nanoemulsions, stability, intestinal permeability, bioavailabilityLu RLiu SWang QLi XDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 4937-4946 (2015)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Lu R
Liu S
Wang Q
Li X
Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement
description Rong Lu,1 Shan Liu,1 Qilin Wang,1 Xia Li1,2 1School of Ocean, Shandong University, Weihai, 2School of Pharmaceutical Sciences, Shandong University, Jinan, People’s Republic of China Abstract: Oral administration remains a significant challenge in regards to drugs with serious solubility and stability issues. This article aimed to investigate the suitability of nanoemulsions as oral carriers of stiripentol (STP), an acid-labile drug, for enhancement of stability and bioavailability. STP-loaded nanoemulsions (STP-NEs) were prepared by using a solvent-diffusion/ultrasonication technique. STP-NEs were characterized in a variety of ways such as by particle size, entrapment efficiency, in vitro drug release, and transmission electron microscopy. A bioavailability study was performed in rats after oral administration of either STP-NEs, or commercial formulation (Diacomit®). The resultant nanoemulsions were 146.6 nm in particle size with an entrapment efficiency of 99.47%. It was demonstrated that nanoemulsions significantly improved the biochemical stability and bioavailability of STP. The bioavailability of STP-NEs was up to 206.2% relative to Diacomit®. Nanoemulsions fabricated from poly(ethylene glycol) monooleate/medium-chain triglycerides exhibited excellent performance in drug stabilization and absorption enhancement. The results suggest that STP-NEs are a promising means to solve the problems associated with stability and solubility of STP. Keywords: stiripentol, nanoemulsions, stability, intestinal permeability, bioavailability
format article
author Lu R
Liu S
Wang Q
Li X
author_facet Lu R
Liu S
Wang Q
Li X
author_sort Lu R
title Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement
title_short Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement
title_full Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement
title_fullStr Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement
title_full_unstemmed Nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement
title_sort nanoemulsions as novel oral carriers of stiripentol: insights into the protective effect and absorption enhancement
publisher Dove Medical Press
publishDate 2015
url https://doaj.org/article/f24256f143504c2587c7b84e93898fc7
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AT wangq nanoemulsionsasnoveloralcarriersofstiripentolinsightsintotheprotectiveeffectandabsorptionenhancement
AT lix nanoemulsionsasnoveloralcarriersofstiripentolinsightsintotheprotectiveeffectandabsorptionenhancement
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