Gastrointestinal behavior of nano- and microsized fenofibrate: In vivo evaluation in man and in vitro simulation by assessment of the permeation potential

European Journal of Pharmaceutical Sciences

Volumn 77, Issue , 2015, Pages 40-47

  Hens, Bart ^a   Brouwers, Joachim ^a   Corsetti, Maura ^b   Augustijns, Patrick ^a  

^a DEPARTMENT OF PHARMACEUTICAL AND PHARMACOLOGICAL SCIENCES   (Belgium)

^b UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Clinical study; Dialysis; Dissolution; Fenofibrate; Microparticles; Nanoparticles; Permeation; Solubility permeability interplay

Indexed keywords

FENOFIBRATE; ANTILIPEMIC AGENT; MICROSPHERE; NANOPARTICLE;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG PENETRATION; DRUG SOLUBILITY; ENCAPSULATION; FEMALE; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; IN VIVO STUDY; INTESTINE FLUID; MALE; NORMAL HUMAN; PRIORITY JOURNAL; CHEMISTRY; DRUG EFFECTS; GASTROINTESTINAL TRACT; SOLUBILITY;

FENOFIBRATE; GASTROINTESTINAL TRACT; HUMANS; HYPOLIPIDEMIC AGENTS; IN VITRO TECHNIQUES; MICROSPHERES; NANOPARTICLES; SOLUBILITY;

EID: 84931261722     PISSN: 09280987     EISSN: 18790720     Source Type: Journal    
DOI: 10.1016/j.ejps.2015.05.023     Document Type: Article

References (29)

1. G.E. Amidon, W.I. Higuchi, and N.F.H. Ho Theoretical and experimental studies of transport of micelle-solubilized solutes J. Pharm. Sci. 71 1982 77 84
2. G.L. Amidon, H. Lennernäs, V.P. Shah, and J.R. Crison A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability Pharm. Res. 12 1995 413 420
3. P. Augustijns, B. Wuyts, B. Hens, P. Annaert, J. Butler, and J. Brouwers A review of drug solubility in human intestinal fluids: implications for the prediction of oral absorption Eur. J. Pharm. Sci. 57 2014 322 332
4. L.Z. Benet, F. Broccatelli, and T.I. Oprea BDDCS applied to over 900 drugs AAPS J. 13 2011 519 547
5. 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
6. S.T. Buckley, K.J. Frank, G. Fricker, and M. Brandl Biopharmaceutical classification of poorly soluble drugs with respect to "enabling formulations" Eur. J. Pharm. Sci. 50 2013 8 16
7. S.M. Fischer, S.T. Buckley, W. Kirchmeyer, G. Fricker, and M. Brandl Application of simulated intestinal fluid on the phospholipid vesicle-based drug permeation assay Int. J. Pharm. 422 2012 52 58
8. K.J. Frank, K.M. Rosenblatt, U. Westedt, P. Hölig, J. Rosenberg, M. Mägerlein, G. Fricker, and M. Brandl Amorphous solid dispersion enhances permeation of poorly soluble ABT-102: true supersaturation vs. apparent solubility enhancement Int. J. Pharm. 437 2012 288 293
9. K.J. Frank, U. Westedt, K.M. Rosenblatt, P. Hölig, J. Rosenberg, M. Mägerlein, M. Brandl, and G. Fricker Impact of FaSSIF on the solubility and dissolution-/permeation rate of a poorly water-soluble compound Eur. J. Pharm. Sci. 47 2012 16 20
10. P.-H. Guivarc'h, M.G. Vachon, and D. Fordyce A new fenofibrate formulation: results of six single-dose, clinical studies of bioavailability under fed and fasting conditions Clin. Ther. 26 2004 1456 1469
11. A. Hanafy, H. Spahn-Langguth, G. Vergnault, P. Grenier, M. Tubic Grozdanis, T. Lenhardt, and P. Langguth Pharmacokinetic evaluation of oral fenofibrate nanosuspensions and SLN in comparison to conventional suspensions of micronized drug Adv. Drug Deliv. Rev. 59 2007 419 426
12. N. Holmstock, T.D. Bruyn, J. Bevernage, P. Annaert, R. Mols, J. Tack, and P. Augustijns Exploring food effects on indinavir absorption with human intestinal fluids in the mouse intestine Eur. J. Pharm. Sci. 49 2013 27 32
13. E. Jantratid, N. Janssen, C. Reppas, and J.B. Dressman Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update Pharm. Res. 25 2008 1663 1676
14. L. Jia, H. Wong, C. Cerna, and S.D. Weitman Effect of nanonization on absorption of 301029: ex vivo and in vivo pharmacokinetic correlations determined by liquid chromatography/mass spectrometry Pharm. Res. 19 2002 1091 1096
15. D. Juenemann, E. Jantratid, C. Wagner, C. Reppas, M. Vertzoni, and J.B. Dressman Biorelevant in vitro dissolution testing of products containing micronized or nanosized fenofibrate with a view to predicting plasma profiles Eur. J. Pharm. Biopharm. 77 2011 257 264
16. E.S. Kostewicz, B. Abrahamsson, M. Brewster, J. Brouwers, J. Butler, S. Carlert, P.A. Dickinson, J. Dressman, R. Holm, S. Klein, J. Mann, M. McAllister, M. Minekus, U. Muenster, A. Müllertz, M. Verwei, M. Vertzoni, W. Weitschies, and P. Augustijns In vitro models for the prediction of in vivo performance of oral dosage forms Eur. J. Pharm. Sci. 57 2014 342 366
17. C.A. Lipinski Drug-like properties and the causes of poor solubility and poor permeability J. Pharmacol. Toxicol. Methods 44 2000 235 249
18. C. Markopoulos, F. Thoenen, D. Preisig, M. Symillides, M. Vertzoni, N. Parrott, C. Reppas, and G. Imanidis Biorelevant media for transport experiments in the Caco-2 model to evaluate drug absorption in the fasted and the fed state and their usefulness Eur. J. Pharm. Biopharm. 86 2014 438 448
19. J.M. Miller, A. Beig, B.J. Krieg, R.A. Carr, T.B. Borchardt, G.E. Amidon, G.L. Amidon, and A. Dahan The solubility-permeability interplay: mechanistic modeling and predictive application of the impact of micellar solubilization on intestinal permeation Mol. Pharm. 8 2011 1848 1856
20. M. Nakarani, A.K. Misra, J.K. Patel, and S.S. Vaghani Itraconazole nanosuspension for oral delivery: formulation, characterization and in vitro comparison with marketed formulation Daru 18 2010 84 90
21. C.J.H. Porter, N.L. Trevaskis, and W.N. Charman Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs Nat. Rev. Drug. Discov. 6 2007 231 248
22. R. Sauron, M. Wilkins, V. Jessent, A. Dubois, C. Maillot, and A. Weil Absence of a food effect with a 145 mg nanoparticle fenofibrate tablet formulation Int. J. Clin. Pharmacol. Ther. 44 2006 64 70
23. L.E. Schmidt, and K. Dalhoff Food-drug interactions Drugs 62 2002 1481 1502
24. K. Sigfridsson, A.J. Lundqvist, and M. Strimfors Particle size reduction and pharmacokinetic evaluation of a poorly soluble acid and a poorly soluble base during early development Drug Dev. Ind. Pharm. 37 2011 243 251
25. J. Stappaerts, B. Wuyts, J. Tack, P. Annaert, and P. Augustijns Human and simulated intestinal fluids as solvent systems to explore food effects on intestinal solubility and permeability Eur. J. Pharm. Sci. 63 2014 178 186
26. B. Van Eerdenbrugh, J. Vermant, J.A. Martens, L. Froyen, J.V. Humbeeck, G. Van den Mooter, and P. Augustijns Solubility increases associated with crystalline drug nanoparticles: methodologies and significance Mol. Pharm. 7 2010 1858 1870
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 155104
28. H.D. Williams, N.L. Trevaskis, S.A. Charman, R.M. Shanker, W.N. Charman, C.W. Pouton, and C.J.H. Porter Strategies to address low drug solubility in discovery and development Pharmacol. Rev. 65 2013 315 499
29. B. Zuo, Y. Sun, H. Li, X. Liu, Y. Zhai, J. Sun, and Z. He Preparation and in vitro/in vivo evaluation of fenofibrate nanocrystals Int. J. Pharm. 455 2013 267 275