Bioavailability of silymarin flavonolignans drug

Authors: Eleni Theodosiou Kateřina Purchartová Haralambos Stamatis Fragiskos Kolisis Vladimír Křen

Publish Date: 2013/04/06

Volume: 13, Issue: 1, Pages: 1-18

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Abstract

Over the past years great advances have been made on the development of novel delivery systems for bioactive natural compounds in parallel to their structural modification via chemical chemoenzymatic and enzymatic methodologies These approaches give rise to novel formulations and derivatives that often display advantages over the parental molecule such as enhanced bioavailability and pharmacological activity due to improved dissolution and stability Silymarin components suffer from poor solubility in water and lipid media and their resorption in the intestine is rather limited Moreover silybin undergoes intensive Phase II metabolism and is rapidly excreted in bile and urine leading to low therapeutic efficacy This work aims to present the current status of available silymarin formulations and to highlight successful efforts for the biotransformation of its constituent flavonolignans towards the synthesis of novel derivatives Herein various pharmaceutical formulations that aim at the bioavailability improvement of these fascinating phytochemicals ie liposomes phytosomes selfmicroemulsifying drug delivery systems solid dispersions systems dripping pills nanosuspensions floating tablets and micronization are reviewed Silybin semisynthetic derivatives prepared by chemical or enzymatic methods such as fatty acid conjugates silybin bishemisuccinate silybin glycosides silybin sulfates silybinic acid and 23dehydrosilybin are also discussed in detail Additionally this work attempts to direct the attention towards the pharmacological implications of optically pure silybin A and silybin B and their biotransformation reactions both Phase I and II in relation to bioavailability

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