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Molecules 2017, 22(11), 1921;

Natural Deep Eutectic Solvents (NADES) to Enhance Berberine Absorption: An In Vivo Pharmacokinetic Study

Department of Pharmaceutical and Pharmacological Sciences University of Padova, via Marzolo 5, 35121 Padova, Italy
Unir&d, Nutraceutical lab, via Tommaseo, 35100 Padova, Italy
Department of Molecular Medicine University of Padova, via Gabelli, 35121 Padova, Italy
Faculty of Pharmacy, University of Ljubljana, Askerceva Cesta 7, SI-1000 Ljubljana, Slovenia
Department of Chemical and Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy
School of Pharmacy, University of Camerino, Via Sant’Agostino 1, I-62032 Camerino, Italy
Author to whom correspondence should be addressed.
Received: 12 October 2017 / Revised: 3 November 2017 / Accepted: 4 November 2017 / Published: 8 November 2017
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In the present study results related to the in vivo administration of Natural Deep Eutectic Solvents (NADES)-solubilized berberine are reported for the first time. NADES are mixtures of small natural compounds having a melting point significantly lower than that of any individual component. Such solvents have gained much attention of the scientific community in the green chemistry area, being considered useful alternatives to common organic solvents. NADES can be used also as administration vehicles, and this can be attractive for nutraceutical products when eutectics are formed with food grade ingredients. In this work, different NADES were prepared using mainly food grade constituents and were tested as solvents for the alkaloid berberine. Three selected NADES/berberine solutions and an aqueous suspension were orally administered to mice with in dose of 50 mg/Kg. Blood levels of berberine were measured by a LC-MS/MS method. The pharmacokinetic analysis revealed a 2–20 fold increase in blood concentration of NADES/berberine with significant changes in pharmacokinetic profile. Natural Deep Eutectic Solvents may thus be considered attractive solubilizing agents and may also play a role in the increase of absorption of poorly bioavailable natural products such as berberine. View Full-Text
Keywords: berberine; NADES; HPLC-MS/MS; pharmacokinetic; in vivo berberine; NADES; HPLC-MS/MS; pharmacokinetic; in vivo

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Sut, S.; Faggian, M.; Baldan, V.; Poloniato, G.; Castagliuolo, I.; Grabnar, I.; Perissutti, B.; Brun, P.; Maggi, F.; Voinovich, D.; Peron, G.; Dall’Acqua, S. Natural Deep Eutectic Solvents (NADES) to Enhance Berberine Absorption: An In Vivo Pharmacokinetic Study. Molecules 2017, 22, 1921.

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