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. 2019 Jun 7;24(11):2155.
doi: 10.3390/molecules24112155.

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

Free PMC article

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

Alfonso Di Costanzo et al. Molecules. .
Free PMC article


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.

Keywords: enhanced bioavailability; liposome; nanoemulsion; nanostructured lipid carriers; polymeric particles; self-emulsifying delivery systems; silybin; silymarin; solid lipid nanoparticles.

Conflict of interest statement

The authors declare no conflict of interest.


Figure 1
Figure 1
Molecular structure of silybin A.
Figure 2
Figure 2
Relevant formulation strategies currently available to improve the bioavailability of silymarin.

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