Enhanced bioavailability of silymarin by self-microemulsifying drug delivery system

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 63, Issue 3, 2006, Pages 288-294

  Wu, Wei ^a   Wang, Yang ^a   Que, Li ^a  

^a FUDAN UNIVERSITY   (China)

Author keywords

Bioavailability; In vitro release; Pharmacokinetics; Self microemulsifying drug delivery system; Silybin; Silymarin

Indexed keywords

ALCOHOL; LINOLEIC ACID ETHYL ESTER; LIPID; MACROGOL 400; POLYSORBATE 80; SILIBININ; SILYMARIN;

ANIMAL EXPERIMENT; AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DIALYSIS; DILUTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUTION; ENTEROHEPATIC CIRCULATION; FEEDING; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; MALE; MAXIMUM ALLOWABLE CONCENTRATION; MICROEMULSION; NONHUMAN; PARTICLE SIZE; SUSPENSION; ULTRAFILTRATION;

ANIMALS; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DRUG DELIVERY SYSTEMS; EMULSIONS; MALE; PARTICLE SIZE; RABBITS; SILYMARIN; SOLUBILITY;

EID: 33646854907     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2005.12.005     Document Type: Article

References (33)

1. Pepping J. Milk thistle: Silybum marianum. Am. J. Health-System Pharm. 56 (1999) 1195-1197
2. Flora K., Hahn M., Rosen H., and Benner K. Milk thistle (Silybum marianum) for the therapy of liver disease. Am. J. Gastroenterol. 93 (1998) 139-143
3. Luper S. A review of plants used in the treatment of liver disease: part 1. Altern. Med. Rev. 3 (1998) 410-421
4. O'Hara M.A., Kiefer D., Farrell K., and Kemper K. A review of 12 commonly used medicinal herbs. Arch. Fam. Med. 7 (1998) 523-536
5. Zi X., Feyes D.K., and Agarwal R. Anticarcinogenic effect of a flavonoid antioxidant, silymarin, in human breast cancer cells MDA-MB 468: induction of G1 arrest through an increase in Cip1/p21 concomitant with a decrease in kinase activity of cyclin-dependent kinases and associated cyclins. Clin. Cancer Res. 4 (1998) 1055-1064
6. Zi X., Grasso A.W., Kung H.J., and Agarwal R. A flavonoid antioxidant, silymarin, inhibits activation of erbB1 signaling and induces cyclin-dependent kinase inhibitors, G1 arrest, and anticarcinogenic effects in human prostate carcinoma DU145 cells. Cancer Res. 58 (1998) 1920-1929
7. Lahiri-Chatterjee M., Katiyar S.K., Mohan R.R., and Agarwal R. A flavonoid antioxidant, silymarin, affords exceptionally high protection against tumor promotion in the SENCAR mouse skin tumorigenesis model. Cancer Res. 59 (1999) 622-632
8. Morazzoni P., Montalbetti A., Malandrino S., and Pifferi G. Comparative pharmacokinetics of silipide and silymarin in rats. Eur. J. Drug Metab. Pharmacokinet. 18 (1993) 289-297
9. Lorenz D., Lucker P.W., Mennicke W.H., and Wetzelsberger N. Pharmacokinetic studies with silymarin in human serum and bile. Methods Find. Exp. Clin. Pharmacol. 6 (1984) 655-661
10. Barzaghi N., Crema F., Gatti G., Pifferi G., and Perucca E. Pharmacokinetic studies on IdB 1016, a silybin-phosphatidylcholine complex, in healthy human subjects. Eur. J. Drug Metab. Pharmacokinet. 15 (1990) 333-338
11. Schandalik R., Gatti G., and Perucca E. Pharmacokinetics of silybin in bile following administration of silipide and silymarin in cholecystectomy patients. Arzneimittelforschung 42 (1992) 964-968
12. Chen W., Xia H., and Wu W. Optimized preparation of silymarin dripping pills by a central composite design-response surface method. Chin. Trad. Herb. Drug. 36 (2005) 679-683
13. Weyhenmeyer R., Mascher H., and Birkmayer J. Study on dose-linearity of the pharmacokinetics of silibinin diastereomers using a new stereospecific assay. Int. J. Clin. Pharmacol. Ther. Toxicol. 30 (1992) 134-138
14. Schulz H.U., Schurer M., Krumbiegel G., Wachter W., Weyhenmeyer R., and Seidel G. The solubility and bioequivalence of silymarin preparations. Arzneimittelforschung 45 (1995) 61-64
15. Lawrence M.J., and Rees G.D. Microemulsion-based media as novel drug delivery systems. Adv. Drug Deliv. Rev. 45 (2000) 89-121
16. Humberstone A.J., and Charman W.N. Lipid-based vehicles for the oral delivery of poorly water soluble drugs. Adv. Drug Deliv. Rev. 25 (1997) 103-128
17. Constantinides P.P. Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects. Pharm. Res. 12 (1995) 1561-1572
18. Pouton C.W. Lipid formulation for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems. Eur. J. Pharm. Sci. 11 (2000) S93-S98
19. Gershanik T., and Benita S. Self-dispersing lipid formulations for improving oral absorption of lipophilic drugs. Eur. J. Pharm. Biopharm. 50 (2000) 179-188
20. Pouton C.W. Formulation of self-emulsifying drug delivery systems. Adv. Drug Deliv. Rev. 25 (1997) 47-58
21. O'Driscoll C.M. Lipid-based formulations for intestinal lymphatic delivery. Eur. J. Pharm. Sci. 15 (2002) 405-415
22. Swenson E.S., and Curatolo W.J. Means to enhance penetration. Adv. Drug Deliv. Rev. 8 (1992) 39-42
23. Haus D.J., Mehta S.C., and Radebaugh G.W. Targeting lymphatic transport and modified systemic distribution of CI-976, a lipophilic lipid-regulator drug, via a formulation approach. Int. J. Pharm. 108 (1994) 85-93
24. Holm R., Porter C.J.H., Edwards G.A., Müllertz A., Kristensen H.G., and Charman W.N. Examination of oral absorption and lymphatic transport of halofantrine in triple-cannulated canine model after administration in self-microemulsifying drug delivery systems (SMEDDS) containing structured triglycerides. Eur. J. Pharm Sci. 20 (2003) 91-97
25. Kang B.K., Lee J.S., Chon S.K., Jeong S.Y., Yuk S.H., Khang G., Lee H.B., and Cho S.H. Development of self-microemulsifying drug delivery systems (SMEDDS) for oral bioavailability enhancement of simvastatin in beagle dogs. Int. J. Pharm. 274 (2004) 65-73
26. Khoo S.M., Humberstone A.J., Porter C.J.H., Edwards G.A., and Charman W.N. Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine. Int. J. Pharm. 167 (1998) 155-164
27. Itoh K., Matsui S., Tozuka Y., Oguchi T., and Yamamoto K. Improvement of physicochemical properties of N-4472 Part II: characterization of N-4472 microemulsion and the enhanced oral absorption. Int. J. Pharm. 246 (2002) 75-83
28. Kommuru T.R., Gurley B., Khan M.A., and Reddy I.K. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment. Int. J. Pharm. 212 (2001) 233-246
29. Wang Y., Wu W., and Que L. Investigation on oil/Tween80/alcohol/water system pseudo-ternary phase diagrams and self-microemulsifying drug delivery system. Chin. J. Pharm. 36 (2005) 345-348
30. Mascher H., Kikuta C., and Weyhenmeyer R. Diastereomeric separation of free and conjugated silibinin in plasma by reversed phase HPLC after specific extraction. J. Liquid Chromatogr. 16 (1993) 2777-2789
31. Morazzoni P., Magistretti M.J., Giachetti C., and Zanolo G. Comparative bioavailability of Silipide, a new flavanolignan complex in rats. Eur. J. Drug Metab. Pharmacokinet. 17 (1992) 39-44
32. Yuan Q., Li X.R., Wang H.J., Li X.Y., and Liu Y. The absorption kinetics of silymarin microemulsion in rat intestine. Acta Pharm. Sin. 39 (2004) 631-634
33. Charman W.N., and Stella V.J. Transport of lipophilic molecules by the intestinal lymphatic system. Adv. Drug Deliv. Rev. 7 (1991) 1-14