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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

Department of Food Biofunctionality, Institute of Nutritional Sciences, University of Hohenheim, 70599 Stuttgart, Germany
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Academic Editor: Volker Böhm
Antioxidants 2021, 10(11), 1826; https://doi.org/10.3390/antiox10111826
Received: 5 November 2021 / Revised: 15 November 2021 / Accepted: 15 November 2021 / Published: 17 November 2021
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. View Full-Text
Keywords: cellular uptake; curcuminoids; cyclodextrin complex; drug interactions; efflux transporter; intestinal cell line; multidrug resistance protein 1; polysorbate 80 micelles; turmeric oils cellular uptake; curcuminoids; cyclodextrin complex; drug interactions; efflux transporter; intestinal cell line; multidrug resistance protein 1; polysorbate 80 micelles; turmeric oils
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MDPI and ACS Style

Flory, S.; Männle, R.; Frank, J. The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation. Antioxidants 2021, 10, 1826. https://doi.org/10.3390/antiox10111826

AMA Style

Flory S, Männle R, Frank J. The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation. Antioxidants. 2021; 10(11):1826. https://doi.org/10.3390/antiox10111826

Chicago/Turabian Style

Flory, Sandra, Romina Männle, and Jan Frank. 2021. "The Inhibitory Activity of Curcumin on P-Glycoprotein and Its Uptake by and Efflux from LS180 Cells Is Not Affected by Its Galenic Formulation" Antioxidants 10, no. 11: 1826. https://doi.org/10.3390/antiox10111826

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