Bioavailability of silymarin flavonolignans: drug formulations and biotransformation

0428336 - MBÚ 2015 RIV NL eng J - Článek v odborném periodiku
Theodosiou, E. - Purchartová, Kateřina - Stamatis, H. - Kolisis, F. - Křen, Vladimír
Bioavailability of silymarin flavonolignans: drug formulations and biotransformation.
Phytochemistry Reviews. Roč. 13, č. 1 (2014), s. 1-18. ISSN 1568-7767. E-ISSN 1572-980X
Grant CEP: GA ČR(CZ) GAP301/11/0662; GA MŠMT(CZ) LD11051; GA MŠMT(CZ) ME10027
Institucionální podpora: RVO:61388971
Klíčová slova: Silymarin * Silybin * Silibinin
Kód oboru RIV: CE - Biochemie
Impakt faktor: 2.407, rok: 2014

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, chemo-enzymatic 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, i.e., liposomes, phytosomes, self-microemulsifying drug delivery systems, solid dispersions systems, dripping pills, nanosuspensions, floating tablets, and micronization, are reviewed. Silybin (semi)synthetic derivatives prepared by chemical or enzymatic methods, such as fatty acid conjugates, silybin bishemisuccinate, silybin glycosides, silybin sulfates, silybinic acid, and 2,3-dehydrosilybin, 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
Trvalý link: http://hdl.handle.net/11104/0233696