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Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats

Although linarin possesses diverse pharmacological activities, its poor oral bioavailability has been a concern for further development. The present study aimed to demonstrate the feasibility of improving the oral absorption of linarin in rats with a bioenhancer‒piperine. First, the intestinal perme...

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Autores principales: Feng, Xinchi, Liu, Youping, Wang, Xin, Di, Xin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271293/
https://www.ncbi.nlm.nih.gov/pubmed/24786847
http://dx.doi.org/10.3390/molecules19055624
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author Feng, Xinchi
Liu, Youping
Wang, Xin
Di, Xin
author_facet Feng, Xinchi
Liu, Youping
Wang, Xin
Di, Xin
author_sort Feng, Xinchi
collection PubMed
description Although linarin possesses diverse pharmacological activities, its poor oral bioavailability has been a concern for further development. The present study aimed to demonstrate the feasibility of improving the oral absorption of linarin in rats with a bioenhancer‒piperine. First, the intestinal permeability of linarin in the presence and absence of verapamil or piperine was investigated using an in situ single-pass rat intestinal perfusion method. A significant increase in the P(eff) when co-perfused with verapamil or piperine indicated that piperine effectively inhibited P-glycoprotein mediated efflux of linarin. Then, the pharmacokinetic profiles of linarin in rats after oral administration of linarin (50 mg/kg) alone and in combination with piperine (20 mg/kg) were determined using a validated LC–MS/MS method. The results showed that piperine increased the plasma exposure (AUC) of linarin by 381% along with an increase in the C(max) by 346% and the T(max) from 0.05 h to 0.2 h. The present study revealed that piperine significantly enhanced the oral absorption of linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of linarin.
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spelling pubmed-62712932018-12-21 Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats Feng, Xinchi Liu, Youping Wang, Xin Di, Xin Molecules Article Although linarin possesses diverse pharmacological activities, its poor oral bioavailability has been a concern for further development. The present study aimed to demonstrate the feasibility of improving the oral absorption of linarin in rats with a bioenhancer‒piperine. First, the intestinal permeability of linarin in the presence and absence of verapamil or piperine was investigated using an in situ single-pass rat intestinal perfusion method. A significant increase in the P(eff) when co-perfused with verapamil or piperine indicated that piperine effectively inhibited P-glycoprotein mediated efflux of linarin. Then, the pharmacokinetic profiles of linarin in rats after oral administration of linarin (50 mg/kg) alone and in combination with piperine (20 mg/kg) were determined using a validated LC–MS/MS method. The results showed that piperine increased the plasma exposure (AUC) of linarin by 381% along with an increase in the C(max) by 346% and the T(max) from 0.05 h to 0.2 h. The present study revealed that piperine significantly enhanced the oral absorption of linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of linarin. MDPI 2014-04-30 /pmc/articles/PMC6271293/ /pubmed/24786847 http://dx.doi.org/10.3390/molecules19055624 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Feng, Xinchi
Liu, Youping
Wang, Xin
Di, Xin
Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats
title Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats
title_full Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats
title_fullStr Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats
title_full_unstemmed Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats
title_short Effects of Piperine on the Intestinal Permeability and Pharmacokinetics of Linarin in Rats
title_sort effects of piperine on the intestinal permeability and pharmacokinetics of linarin in rats
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271293/
https://www.ncbi.nlm.nih.gov/pubmed/24786847
http://dx.doi.org/10.3390/molecules19055624
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