The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation

The biological activities of curcumin in humans, including its antioxidative and anti-inflammatory functions, are limited by its naturally low bioavailability. Different formulation strategies have been developed, but the uptake of curcumin from these galenic formulations into and efflux from intest...

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Autores principales:	Sandra Flory, Romina Männle, Jan Frank
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	cellular uptake curcuminoids cyclodextrin complex drug interactions efflux transporter intestinal cell line Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/9b59b5d958a942fb8b64a7833c65a9c4
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spelling	oai:doaj.org-article:9b59b5d958a942fb8b64a7833c65a9c42021-11-25T16:29:10ZThe Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation10.3390/antiox101118262076-3921https://doaj.org/article/9b59b5d958a942fb8b64a7833c65a9c42021-11-01T00:00:00Zhttps://www.mdpi.com/2076-3921/10/11/1826https://doaj.org/toc/2076-3921The biological activities of curcumin in humans, including its antioxidative and anti-inflammatory functions, are limited by its naturally low bioavailability. Different formulation strategies have been developed, but the uptake of curcumin from these galenic formulations into and efflux from intestinal cells, which may be critical processes limiting bioavailability, have not been directly compared. Furthermore, little is known about their effect on P-glycoprotein activity, an important determinant of the pharmacokinetics of potentially co-administered drugs. P-glycoprotein activity was determined in LS180 cells, incubated with 30 or 60 µmol/L of curcumin in the form of seven different formulations or native curcuma extract for 1 h. All formulations inhibited P-glycoprotein activity at both concentrations. Curcumin uptake, after 1 h incubation of LS180 cells with the formulations (60 µmol/L), showed significant variability but no consistent effects. After 1 h pre-treatment with the formulations and further 8 h with curcumin-free medium, curcumin in cell culture supernatants, reflecting the efflux, differed between individual formulations, again without a clear effect. In conclusion, curcumin inhibits P-glycoprotein activity independently of its formulation. Its uptake by and efflux from intestinal cells was not significantly different between formulations, indicating that these processes are not important regulatory points for its bioavailability.Sandra FloryRomina MännleJan FrankMDPI AGarticlecellular uptakecurcuminoidscyclodextrin complexdrug interactionsefflux transporterintestinal cell lineTherapeutics. PharmacologyRM1-950ENAntioxidants, Vol 10, Iss 1826, p 1826 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	cellular uptake curcuminoids cyclodextrin complex drug interactions efflux transporter intestinal cell line Therapeutics. Pharmacology RM1-950
spellingShingle	cellular uptake curcuminoids cyclodextrin complex drug interactions efflux transporter intestinal cell line Therapeutics. Pharmacology RM1-950 Sandra Flory Romina Männle Jan Frank The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation
description	The biological activities of curcumin in humans, including its antioxidative and anti-inflammatory functions, are limited by its naturally low bioavailability. Different formulation strategies have been developed, but the uptake of curcumin from these galenic formulations into and efflux from intestinal cells, which may be critical processes limiting bioavailability, have not been directly compared. Furthermore, little is known about their effect on P-glycoprotein activity, an important determinant of the pharmacokinetics of potentially co-administered drugs. P-glycoprotein activity was determined in LS180 cells, incubated with 30 or 60 µmol/L of curcumin in the form of seven different formulations or native curcuma extract for 1 h. All formulations inhibited P-glycoprotein activity at both concentrations. Curcumin uptake, after 1 h incubation of LS180 cells with the formulations (60 µmol/L), showed significant variability but no consistent effects. After 1 h pre-treatment with the formulations and further 8 h with curcumin-free medium, curcumin in cell culture supernatants, reflecting the efflux, differed between individual formulations, again without a clear effect. In conclusion, curcumin inhibits P-glycoprotein activity independently of its formulation. Its uptake by and efflux from intestinal cells was not significantly different between formulations, indicating that these processes are not important regulatory points for its bioavailability.
format	article
author	Sandra Flory Romina Männle Jan Frank
author_facet	Sandra Flory Romina Männle Jan Frank
author_sort	Sandra Flory
title	The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation
title_short	The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation
title_full	The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation
title_fullStr	The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation
title_full_unstemmed	The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation
title_sort	inhibitory activity of curcumin on p-glycoprotein and its uptake by and efflux from ls180 cells is not affected by its galenic formulation
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/9b59b5d958a942fb8b64a7833c65a9c4
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The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation

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