Continuous and scalable process for water-redispersible nanoformulation of poorly aqueous soluble APIs by antisolvent precipitation and spray-drying

International Journal of Pharmaceutics

Volumn 404, Issue 1-2, 2011, Pages 198-204

  Hu, Jun ^a   Ng, Wai Kiong ^a   Dong, Yuancai ^a   Shen, Shoucang ^a   Tan, Reginald B H ^a,b  

^a INSTITUTE OF CHEMICAL AND ENGINEERING SCIENCES   (Singapore)

^b NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

Author keywords

Antisolvent precipitation; Fenofibrate; Nanocrystal; Nanoformulation; Poorly water soluble drug; Spray drying

Indexed keywords

DODECYL SULFATE SODIUM; FENOFIBRATE; HYDROXYPROPYLMETHYLCELLULOSE; LACTOSE; MANNITOL; NANOCRYSTAL;

AQUEOUS SOLUTION; ARTICLE; DRUG FORMULATION; NANOPHARMACEUTICS; PRECIPITATION; PRIORITY JOURNAL; SPRAY DRYING;

CALORIMETRY, DIFFERENTIAL SCANNING; CHEMICAL PRECIPITATION; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; DRUG COMPOUNDING; EXCIPIENTS; FEASIBILITY STUDIES; FENOFIBRATE; HYPOLIPIDEMIC AGENTS; KINETICS; LACTOSE; LIGHT; MANNITOL; METHYLCELLULOSE; MICROSCOPY, ELECTRON, SCANNING; NANOPARTICLES; NANOTECHNOLOGY; POLYSORBATES; POWDERS; SCATTERING, RADIATION; SODIUM DODECYL SULFATE; SOLUBILITY; SOLVENTS; SURFACE PROPERTIES; TECHNOLOGY, PHARMACEUTICAL; X-RAY DIFFRACTION;

EID: 78650679657     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2010.10.055     Document Type: Article

References (35)

1. W. Abdelwahed, G. Degobert, S. Stainmesse, and H. Fessi Freeze-drying of nanoparticles: formulation, process and storage considerations Adv. Drug Deliv. Rev. 58 2006 1688 1713
2. M.V. Chaubal, and C. Popescu Conversion of nanosuspensions into dry powders by spray drying: a case study Pharm. Res. 25 2008 2302 2308
3. H. de Waard, W.L. Hinrichs, and H.W. Frijlink A novel bottom-up process to produce drug nanocrystals: controlled crystallization during freeze-drying J. Control. Release 128 2008 179 183
4. H. de Waard, W.L. Hinrichs, M.R. Visser, C. Bologna, and H.W. Frijlink Unexpected differences in dissolution behavior of tablets prepared from solid dispersions with a surfactant physically mixed or incorporated Int. J. Pharm. 349 2008 66 73
5. Y. Dong, W.K. Ng, J. Hu, S. Shen, and R.B. Tan A continuous and highly effective static mixing process for antisolvent precipitation of nanoparticles of poorly water-soluble drugs Int. J. Pharm. 386 2009 256 261
6. Y. Dong, W.K. Ng, S. Shen, S. Kim, and R.B. Tan Preparation and characterization of spironolactone nanoparticles by antisolvent precipitation Int. J. Pharm. 375 2009 84 88
7. D.J.v. Drooge, W.L. Hinrichs, M.R. Visser, and H.W. Frijlink Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale, using differential scanning calorimetry and gravimetric water vapour sorption techniques Int. J. Pharm. 310 2006 220 229
8. N. Elvassore, A. Bertucco, and P. Caliceti Production of insulin-loaded poly(ethylene glycol)/poly(l-lactide) (PEG/PLA) nanoparticles by gas antisolvent techniques J. Pharm. Sci. 90 2001 1628 1636
9. P. Gassmann, M. List, A. Schweitzer, and H. Sucker Hydrosols - alternatives for the parenteral application of poorly water-soluble drugs Eur. J. Pharm. Biopharm. 40 1994 64 72
10. Y. Gonnissen, S.I.V. Goncalves, B.G. De Geest, J.P. Remon, and C. Vervaet Process design applied to optimise a directly compressible powder produced via a continuous manufacturing process Eur. J. Pharm. Biopharm. 68 2008 760 770 (Pubitemid 351318221)
11. D. Horn, and J. Rieger Organic nanoparticles in the aqueous phase - theory, experiment, and use Angew. Chem. Int. Ed. 40 2001 4331 4361
12. J. Hu, K.P. Johnston, and R.O. Williams 3rd Rapid dissolving high potency danazol powders produced by spray freezing into liquid process Int. J. Pharm. 271 2004 145 154 (Pubitemid 38210092)
13. J. Hu, T.L. Rogers, J. Brown, T. Young, K.P. Johnston, and R.O. Williams 3rd Improvement of dissolution rates of poorly water soluble APIs using novel spray freezing into liquid technology Pharm. Res. 19 2002 1278 1284
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. C.M. Keck, and R.H. Muller Drug nanocrystals of poorly soluble drugs produced by high pressure homogenisation Eur. J. Pharm. Biopharm. 62 2006 3 16
16. F. Kesisoglou, S. Panmai, and Y. Wu Nanosizing - oral formulation development and biopharmaceutical evaluation Adv. Drug Deliv. Rev. 59 2007 631 644
17. V. Kumar, and R.K. Prud'homme Nanoparticle stability: processing pathways for solvent removal Chem. Eng. Sci. 64 2009 1358 1361
18. H. Leuenberger New trends in the production of pharmaceutical granules: batch versus continuous processing Eur. J. Pharm. Biopharm. 52 2001 289 296 (Pubitemid 33033182)
19. Y. Liu, K. Kathan, W. Saad, and R.K. Prud'homme Ostwald ripening of beta-carotene nanoparticles Phys. Rev. Lett. 98 2007
20. M.E. Matteucci, M.A. Hotze, K.P. Johnston, and R.O. Williams Drug nanoparticles by antisolvent precipitation: mixing energy versus surfactant stabilization Langmuir 22 2006 8951 8959
21. E. Merisko-Liversidge, G.G. Liversidge, and E.R. Cooper Nanosizing: a formulation approach for poorly-water-soluble compounds Eur. J. Pharm. Sci. 18 2003 113 120
22. R.H. Mueller, and C.M. Keck Second generation of drug nanocrystals for delivery of poorly soluble drugs: smartCrystal technology Eur. J. Pharm. Sci. 34 2008 S20 S21
23. R.H. Muller, and K. Peters Nanosuspensions for the formulation of poorly soluble drugs. I. Preparation by a size-reduction technique Int. J. Pharm. 160 1998 229 237
24. A. Munoz, J.P. Guichard, and P. Reginault Micronised fenofibrate Atherosclerosis 110 1994 S45 S48
25. P. Pathak, M.J. Meziani, T. Desai, and Y.P. Sun Nanosizing drug particles in supercritical fluid processing J. Am. Chem. Soc. 126 2004 10842 10843
26. B.E. Rabinow Nanosuspensions in drug delivery Nat. Rev. Drug Discov. 3 2004 785 796
27. N. Rasenack, and B.W. Muller Dissolution rate enhancement by in situ micronization of poorly water-soluble drugs Pharm. Res. 19 2002 1894 1900
28. T.L. Rogers, I.B. Gillespie, J.E. Hitt, K.L. Fransen, C.A. Crowl, C.J. Tucker, G.B. Kupperblatt, J.N. Becker, D.L. Wilson, C. Todd, C.F. Broomall, J.C. Evans, and E.J. Elder Development and characterization of a scalable controlled precipitation process to enhance the dissolution of poorly water-soluble drugs Pharm. Res. 21 2004 2048 2057
29. T.L. Rogers, A.C. Nelsen, J.H. Hu, J.N. Brown, M. Sarkari, T.J. Young, K.P. Johnston, and R.O. Williams A novel particle engineering technology to enhance dissolution of poorly water soluble drugs: spray-freezing into liquid Eur. J. Pharm. Biopharm. 54 2002 271 280
30. M. Sarkari, J. Brown, X.X. Chen, S. Swinnea, R.O. Williams, and K.P. Johnston Enhanced drug dissolution using evaporative precipitation into aqueous solution Int. J. Pharm. 243 2002 17 31
31. B.Y. Shekunov, P. Chattopadhyay, J. Seitzinger, and R. Huff Nanoparticles of poorly water-soluble drugs prepared by supercritical fluid extraction of emulsions Pharm. Res. 23 2006 196 204
32. J.W. Tom, and P.G. Debenedetti Particle formation with supercritical fluids - a review J. Aerosol Sci. 22 1991 555 584
33. M. Turk, P. Hils, B. Helfgen, K. Schaber, H.J. Martin, and M.A. Wahl Micronization of pharmaceutical substances by the Rapid Expansion of Supercritical Solutions (RESS): a promising method to improve bioavailability of poorly soluble pharmaceutical agents J. Supercrit. Fluids 22 2002 75 84
34. M. Turk, and R. Lietzow Stabilized nanoparticles of phytosterol by rapid expansion from supercritical solution into aqueous solution AAPS PharmSciTech 5 2004
35. B. Van Eerdenbrugh, G. Van den Mooter, and P. Augustijns Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products Int. J. Pharm. 364 2008 64 75