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Formulation Strategies for Enhancing the Bioavailability of Silymarin: The State of the Art

1
Centre for Research and Training in Medicine for Aging, Department of Medicine and Health Sciences “Vincenzo Tiberio”, University of Molise, I-86100 Campobasso, Italy
2
Department of Agriculture, Environmental and Food Sciences (DIAAA), University of Molise, I-86100 Campobasso, Italy
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Molecules 2019, 24(11), 2155; https://doi.org/10.3390/molecules24112155
Received: 12 April 2019 / Revised: 2 June 2019 / Accepted: 6 June 2019 / Published: 7 June 2019
(This article belongs to the Special Issue Silymarin and Derivatives: From Biosynthesis to Health Benefits)
Silymarin, a mixture of flavonolignan and flavonoid polyphenolic compounds extractable from milk thistle (Silybum marianum) seeds, has anti-oxidant, anti-inflammatory, anti-cancer and anti-viral activities potentially useful in the treatment of several liver disorders, such as chronic liver diseases, cirrhosis and hepatocellular carcinoma. Equally promising are the effects of silymarin in protecting the brain from the inflammatory and oxidative stress effects by which metabolic syndrome contributes to neurodegenerative diseases. However, although clinical trials have proved that silymarin is safe at high doses (>1500 mg/day) in humans, it suffers limiting factors such as low solubility in water (<50 μg/mL), low bioavailability and poor intestinal absorption. To improve its bioavailability and provide a prolonged silymarin release at the site of absorption, the use of nanotechnological strategies appears to be a promising method to potentiate the therapeutic action and promote sustained release of the active herbal extract. The purpose of this study is to review the different nanostructured systems available in literature as delivery strategies to improve the absorption and bioavailability of silymarin. View Full-Text
Keywords: silymarin; silybin; nanoemulsion; solid lipid nanoparticles; nanostructured lipid carriers; liposome; polymeric particles; self-emulsifying delivery systems; enhanced bioavailability silymarin; silybin; nanoemulsion; solid lipid nanoparticles; nanostructured lipid carriers; liposome; polymeric particles; self-emulsifying delivery systems; enhanced bioavailability
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Di Costanzo, A.; Angelico, R. Formulation Strategies for Enhancing the Bioavailability of Silymarin: The State of the Art. Molecules 2019, 24, 2155.

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