A supersaturating delivery system of silibinin exhibiting high payload achieved by amorphous nano-complexation with chitosan

European Journal of Pharmaceutical Sciences

Volumn 89, Issue , 2016, Pages 163-171

  Nguyen, Minh Hiep ^a   Yu, Hong ^a   Dong, Bingxue ^a   Hadinoto, Kunn ^a  

^a Nanyang Technological University   (Singapore)

Author keywords

Amorphous drug; Milk thistle; Nanopharmaceuticals; Silybin; Silymarin

Indexed keywords

CHITOSAN NANOPARTICLE; SILIBININ; CHITOSAN; COLLOID; DRUG CARRIER; NANOPARTICLE; SILYMARIN;

ARTICLE; COMPLEX FORMATION; CONTROLLED STUDY; DRUG DELIVERY SYSTEM; DRUG SOLUBILITY; DRUG STORAGE; PARTICLE SIZE; PH; PRIORITY JOURNAL; ZETA POTENTIAL; BIOAVAILABILITY; CHEMISTRY; COLLOID; DRUG STABILITY; PROCEDURES; SOLUBILITY;

BIOLOGICAL AVAILABILITY; CHITOSAN; COLLOIDS; DRUG CARRIERS; DRUG DELIVERY SYSTEMS; DRUG STABILITY; NANOPARTICLES; PARTICLE SIZE; SILYMARIN; SOLUBILITY;

EID: 84966839219     PISSN: 09280987     EISSN: 18790720     Source Type: Journal    
DOI: 10.1016/j.ejps.2016.04.036     Document Type: Article

References (33)

1. R. Angelico, A. Ceglie, P. Sacco, G. Colafemmina, M. Ripoli, and A. Mangia Phyto-liposomes as nanoshuttles for water-insoluble silybin-phospholipid complex Int. J. Pharm. 471 2014 173 181
2. T.C. Bai, G.B. Yan, J. Hu, H.L. Zhang, and C.G. Huang Solubility of silybin in aqueous poly(ethylene glycol) solution Int. J. Pharm. 308 2006 100 106
3. D. Biedermann, E. Vavrikova, L. Cvak, and V. Kren Chemistry of silybin Nat. Prod. Rep. 31 2014 1138 1157
4. J. Brouwers, M.E. Brewster, and P. Augustijns Supersaturating drug delivery systems: the answer to solubility-limited oral bioavailability? J. Pharm. Sci. 98 2009 2549 2572
5. X. Cao, W.W. Deng, M. Fu, Y. Zhu, H.F. Liu, L. Wang, J. Zeng, Y.W. Wei, X.M. Xu, and J.N. Yu Seventy-two-hour release formulation of the poorly soluble drug silybin based on porous silica nanoparticles: in vitro release kinetics and in vitro/in vivo correlations in beagle dogs Eur. J. Pharm. Sci. 48 2013 64 71
6. N. CaramLelham, F. Hed, and L.O. Sundelof Adsorption of charged amphiphiles to oppositely charged polysaccharides - a study of the influence of polysaccharide structure and hydrophobicity of the amphiphile molecule Biopolymers 41 1997 765 772
7. W.S. Cheow, T.Y. Kiew, Y. Yang, and K. Hadinoto Amorphization strategy affects the stability and supersaturation profile of amorphous drug nanoparticles Mol. Pharm. 11 2014 1611 1620
8. M.T. Cook, G. Tzortzis, D. Charalampopoulos, and V.V. Khutoryanskiy Production and evaluation of dry alginate-chitosan microcapsules as an enteric delivery vehicle for probiotic bacteria Biomacromolecules 12 2011 2834 2840
9. S. Das, P. Roy, R.G. Auddy, and A. Mukherjee Silymarin nanoparticle prevents paracetamol-induced hepatotoxicity Int. J. Nanomedicine 6 2011 1291 1301
10. G. Deep, and R. Agarwal Antimetastatic efficacy of silibinin: molecular mechanisms and therapeutic potential against cancer Cancer Metastasis Rev. 29 2010 447 463
11. M.S. El-Samaligy, N.N. Afifi, and E.A. Mahmoud Evaluation of hybrid liposomes-encapsulated silymarin regarding physical stability and in vivo performance Int. J. Pharm. 319 2006 121 129
12. F. Fraschini, G. Demartini, and D. Esposti Pharmacology of silymarin Clin. Drug Investig. 22 2002 51 65
13. O.P. Gupta, S. Sing, S. Bani, N. Sharma, S. Malhotra, B.D. Gupta, S.K. Banerjee, and S.S. Handa Anti-inflammatory and anti-arthritic activities of silymarin acting through inhibition of 5-lipoxygenase Phytomedicine 7 2000 21 24
14. P. Kidd, and K. Head A review of the bioavailability and clinical efficacy of milk thistle phytosome: a silybin-phosphatidylcholine complex (siliphos (R)) Altern. Med. Rev. 10 2005 193 203
15. R. Laitinen, K. Lobmann, C.J. Strachan, H. Grohganz, and T. Rades Emerging trends in the stabilization of amorphous drugs Int. J. Pharm. 453 2013 65 79
16. F.Q. Li, and J.F. Hu Improvement of the dissolution rate of silymarin by means of solid dispersions Chem. Pharm. Bull. (Tokyo) 52 2004 972 973
17. L.G. Naso, E.G. Ferrer, N. Butenko, I. Cavaco, L. Lezama, T. Rojo, S.B. Etcheverry, and P.A.M. Williams Antioxidant, DNA cleavage, and cellular effects of silibinin and a new oxovanadium(IV)/silibinin complex J. Biol. Inorg. Chem. 16 2011 653 668
18. M.H. Nguyen, H. Yu, T.Y. Kiew, and K. Hadinoto Cost-effective alternative to nano-encapsulation: amorphous curcumin-chitosan nanoparticle complex exhibiting high payload and supersaturation generation Eur. J. Pharm. Biopharm. 96 2015 1 10
19. D. Pooja, D.J.B. Bikkina, H. Kulhari, N. Nikhila, S. Chinde, Y.M. Raghavendra, B. Sreedhar, and A.K. Tiwari Fabrication, characterization and bioevaluation of silibinin loaded chitosan nanoparticles Int. J. Biol. Macromol. 69 2014 267 273
20. M.F. Qiu, W. Jia, S.S. Li, Z.H. Xu, X. Sun, X.R. Wang, Y.Y. Zhang, and G.X. Xie A new silymarin preparation based on solid dispersion technique Adv. Ther. 22 2005 595 600
21. M. Rinaudo, G. Pavlov, and J. Desbrieres Influence of acetic acid concentration on the solubilization of chitosan Polymer 40 1999 7029 7032
22. M. Saunders, K. Podluii, S. Shergill, G. Buckton, and P. Royall The potential of high speed DSC (hyper-DSC) for the detection and quantification of small amounts of amorphous content in predominantly crystalline samples Int. J. Pharm. 274 2004 35 40
23. K. Sonaje, E.Y. Chuang, K.J. Lin, T.C. Yen, F.Y. Su, M.T. Tseng, and H.W. Sung Opening of epithelial tight junctions and enhancement of Paracellular permeation by chitosan: microscopic, ultrastructural, and computed-tomographic observations Mol. Pharm. 9 2012 1271 1279
24. N. Sun, X. Wei, B. Wu, J. Chen, Y. Lu, and W. Wu Enhanced dissolution of silymarin/polyvinylpyrrolidone solid dispersion pellets prepared by a one-step fluid-bed coating technique Powder Technol. 182 2008 72 80
25. F. Tajarobi, A. Larsson, H. Matic, and S. Abrahmsen-Alami The influence of crystallization inhibition of HPMC and HPMCAS on model substance dissolution and release in swellable matrix tablets Eur. J. Pharm. Biopharm. 78 2011 125 133
26. E. Theodosiou, K. Purchartova, H. Stamatis, F. Kolisis, and V. Kren Bioavailability of silymarin flavonolignans: drug formulations and biotransformation Phytochem. Rev. 13 2014 1 18
27. Y. Wang, D. Zhang, Z. Liu, G. Liu, C. Duan, L. Jia, F. Feng, X. Zhang, Y. Shi, and Q. Zhang In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery Nanotechnology 21 2010
28. J.-W. Wu, L.-C. Lin, S.-C. Hung, C.-W. Chi, and T.-H. Tsai Analysis of silibinin in rat plasma and bile for hepatobiliary excretion and oral bioavailability application J. Pharm. Biomed. Anal. 45 2007 635 641
29. W. Wu, Y. Wang, and L. Que Enhanced bioavailability of silymarin by self-microemulsifying drug delivery system Eur. J. Pharm. Biopharm. 63 2006 288 294
30. Y.Y. Xiao, Y.M. Song, Z.P. Chen, and Q.N. Ping The preparation of silybin-phospholipid complex and the study on its pharmacokinetics in rats Int. J. Pharm. 307 2006 77 82
31. G. Yang, Y. Zhao, N. Feng, Y. Zhang, Y. Liu, and B. Dang Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids Asian J. Pharm. Sci. 10 2015 194 202
32. T.H. Yeh, L.W. Hsu, M.T. Tseng, P.L. Lee, K. Sonjae, Y.C. Ho, and H.W. Sung Mechanism and consequence of chitosan-mediated reversible epithelial tight junction opening Biomaterials 32 2011 6164 6173
33. J.Q. Zhang, J. Liu, Y.L. Li, and B.R. Jasti Preparation and characterization of solid lipid nanoparticles containing silibinin Drug Deliv. 14 2007 381 387