Journal Info

Title: Jurnal Medical Aradean (Arad Medical Journal)
Abbreviated title: J. Med. Ar.
Publisher: "Vasile Goldis" University Press
Owner: Western University "Vasile Goldis" Arad, Romania
ISSN: 1224-3744
e-ISSN: 2067-7790

Ranking and Indexing

Rank: CNCSIS C (code 292) since 2010

International Database: Index Copernicus Journal Master List Value (2010): 4.66

Who's Online

We have 13 guests online

Index Databases

Solubility increasing experiments of sylimarin with cyclodextrins PDF Print E-mail
Written by Fenyvesi F., Petervari M., Nagy L., Keki S., Zsuga M., Bacskay I., Kiss T., Varadi J., Feher P., Ujhelyi Z., Reti-Nagy K., Vecsernyes M.   
Read full article
Article Title: Solubility increasing experiments of sylimarin with cyclodextrins
Authors: Ferenc Fenyvesi1, Mátyás Pétervári 1, Lajos Nagy2, Sándor Kéki2, Miklós Zsuga2, Ildikó
Bácskay1, Tímea Kiss1, Judit Váradi1, Pálma Fehér1, Zoltán Ujhelyi1, Katalin Réti-Nagy1,
Miklós Vecsernyés1*
Affiliation: 1Department of Pharmaceutical Technology, University of Debrecen, Debrecen, Hungary
2Department of Applied Chemistry, University of Debrecen, Debrecen, Hungary
Abstract: Silymarin formulations with high bioavailability are required for the treatment hepatic disorders.
Silymarin, the dry extract of Silybum Marianum is water insoluble and its oral bioavailability is limited.
Cyclodextrins are widely used solubility and absorption enhancers therefore we applied the cyclodextrin
nano-encapsulation for the improvement of silymarin solubility. Hydroxylpropyl-β-cyclodextrin (HPBCD),
randomly methylated β-cyclodextrin (RAMEB), 2,6-di-O-methyl β-cyclodextrin (DIMEB) and Quaternary amino
β-cyclodextrin polymer (QABCDP) were used as host molecules. Sylimarin-cyclodextrin complexes were
prepared in 1:20 mass ratio and we found that each cyclodextrin was able to increase the water solubility
of silymarin. The solutions were stable, thus we can conclude that these cyclodextrins are suitable for the
formulations of sylimarin with increased bioavailability.
Keywords: silymarin, cyclodextrins, solubility, mass spectrometry, HPLC
References: Blumenthal M, Goldberg A, Brinckmann J. Herbal
medicine. Expanded commission E monographs:
integrative medicine communications; 2000.
Carducci R, Armellino MF, Volpe C, Basile G, Caso N,
Apicella A, et al. Silibinin and acute poisoning with
Amanita phalloides. Minerva Anestesiol 62 (1996)
pp. 187-93.
Cserháti T, Forgács E. Inclusion complex formation
of steroidal drugs with hydroxypropyl-betacyclodextrin
studied by charge-transfer
chromatography. J Pharm Biomed Anal. 18 (1-2)
(1998) pp. 179-85.
Dehmlow C, Erhard J, de Groot H. Inhibition of
Kupffer cell functions as an explanation for the
hepatoprotective properties of silibinin. Hepatology
23 (1996) pp. 749–54.
D. Voinovich, B. Perissutti, L. Magarotto, D. Ceschia,
P. Guiotto, A. Bilia Solid state mechanochemical
simultaneous activation of the constituents of the
Silybum marianum phytocomplex with crosslinked
polymers J Pharm Sci, 98 (2009), pp. 215–228
Favari L, Perez-Alvarez V. Comparative effects of
colchicines and silymarin on CCl4 chronic liver
damage in rats. Arch Med Res 28 (1997) pp. 11-7.
Fenyvesi F, Kiss T, Fenyvesi E, Szente L, Veszelka S,
Deli MA, Váradi J, Fehér P, Ujhelyi Z, Tósaki A,
Vecsernyés M, Bácskay I. Randomly methylated
β-cyclodextrin derivatives enhance taxol
permeability through human intestinal epithelial
Caco-2 cell monolayer. J Pharm Sci. 100(11) (2011)
pp. 4734-44.
J. He, S. Hou, W. Lu, L. Zhu, J. Feng Preparation,
pharmacokinetics and body distribution of
silymarin-loaded solid lipid nanoparticles after oral
administration J. Biomed. Nanotech. 3 (2007), pp.
J.S. Woo, T.S. Kim, J.H. Park, S.C. Chi Formulation and
biopharmaceutical evaluation of silymarin using
SMEDDS Arch. Pharm. Res., 30 (2007), pp. 82–89
Kiss T, Fenyvesi F, Bácskay I, Váradi J, Fenyvesi E, Iványi
R, Szente L, Tósaki A, Vecsernyés M. Evaluation
of the cytotoxicity of beta-cyclodextrin derivatives:
evidence for the role of cholesterol extraction. Eur J
Pharm Sci. 40(4) (2010) pp. 376-80
M. Arcari, A. Brambilla, A. Brandt, R. Caponi, G. Corsi,
M. Di Rella, F. Solinas, W.P. Wachter A new inclusion
complex of silibinin and beta-cyclodextrins: in
vitro dissolution kinetics and in vivo absorption
in comparison with traditional formulations Boll.
Chim. Farm., 131 (1992), pp. 205–209
Renganathan A. Pharmaco dynamic properties of
andrographolide in experimental animals. M.D.
thesis. Pharmacology. Pondicherry: Jawaharlal
Institute of Postgraduate Medical Education &
Research (JIPMER), Pondicherry University; 1999.
Saller R, Meier R, Brignoli R. The use of silymarin in
the treatment of liver diseases. Drugs 61 (2001) pp.
S.C. Pradhan & C. Girish Hepatoprotective herbal drug,
silymarin from experimental pharmacology to
clinical medicine Indian J Med Res 124 (2006) pp
Shamama Javed, PhD; Kanchan Kohli; Mushir Ali
Reassessing Bioavailability of Silymarin Altern
Med Rev 16(3) (2011) pp. 239-249
Vogel G, Tuchweber B, Trost W. Protection by silibinin
against Amanita phalloides intoxication in beagles.
Toxicol Appl Pharmacol 73 (1984) pp. 355-62.
W. Chen, H. Xia, W. Wu Optimized preparation of
silymarin dripping pills by a central composite
design–response surface method Chin. Trad. Herb.
Drug, 36 (2005), pp. 679–683
Wachter W, Zaeske H. Process for the manufacture of
flavanolignan preparation with improved release
and absorbability, compositions obtainable thereby
and their use for the preparation of pharmaceuticals.
US Patent 6020, 384; 2000.
Wang M, Grange LL, Tao J. Hepatoprotective properties
of Silybum marianum herbal preparation on
ethanolinduced liver damage. Fitoterapia 67 (1996)
pp. 167-71.
Wellington K, Jarvis B. Silymarin: a review of its clinical
properties in the management of hepatic disorders.
BioDrugs 15 (2001) pp. 465–89.
Wu JW, Lin LC, Tsai TH. Drug-drug interactions of
silymarin on the perspective of pharmacokinetics. J
Ethnopharmacol 121 (2009), pp.185-193.
W. Wei, W. Yang, Q. Li Enhanced bioavailability of
silymarin by self-microemulsifying drug delivery
system Eur. J. Pharm. Biopharm., 63 (2006), pp.
X. Yanyu, S. Yunmei, C. Zhipeng, P. Qineng The
preparation of silybin-phospholipid complex and
the study on its pharmacokinetics in rats Int. J.
Pharm., 307 (2006), pp. 77–82
*Correspondence: Miklós Vecsernyés, University of Debrecen, Debrecen, Faculty of Pharmacy, Department of Pharmaceutical
Technology, Egyetem square 1. 4010. Po. Box.: 78. Debrecen, Hungary. +36-30-512-900/22630. E-mail: This e-mail address is being protected from spambots. You need JavaScript enabled to view it