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Formulation Strategies for Enhancing the Bioavailability of Silymarin: The State of the Art
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Metabolism, Transport and Drug–Drug Interactions of Silymarin

School of Pharmacy, Macau University of Science and Technology, Taipa, Macao 999078, China
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Molecules 2019, 24(20), 3693; https://doi.org/10.3390/molecules24203693
Received: 27 September 2019 / Revised: 11 October 2019 / Accepted: 14 October 2019 / Published: 14 October 2019
(This article belongs to the Special Issue Silymarin and Derivatives: From Biosynthesis to Health Benefits)
Silymarin, the extract of milk thistle, and its major active flavonolignan silybin, are common products widely used in the phytotherapy of liver diseases. They also have promising effects in protecting the pancreas, kidney, myocardium, and the central nervous system. However, inconsistent results are noted in the different clinical studies due to the low bioavailability of silymarin. Extensive studies were conducted to explore the metabolism and transport of silymarin/silybin as well as the impact of its consumption on the pharmacokinetics of other clinical drugs. Here, we aimed to summarize and highlight the current knowledge of the metabolism and transport of silymarin. It was concluded that the major efflux transporters of silybin are multidrug resistance-associated protein (MRP2) and breast cancer resistance protein (BCRP) based on results from the transporter-overexpressing cell lines and MRP2-deficient (TR) rats. Nevertheless, compounds that inhibit the efflux transporters MRP2 and BCRP can enhance the absorption and activity of silybin. Although silymarin does inhibit certain drug-metabolizing enzymes and drug transporters, such effects are unlikely to manifest in clinical settings. Overall, silymarin is a safe and well-tolerated phytomedicine. View Full-Text
Keywords: silybin/silymarin; metabolism; efflux transporters; drug–drug interaction (DDI) silybin/silymarin; metabolism; efflux transporters; drug–drug interaction (DDI)
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Xie, Y.; Zhang, D.; Zhang, J.; Yuan, J. Metabolism, Transport and Drug–Drug Interactions of Silymarin. Molecules 2019, 24, 3693.

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