Solubility increases associated with crystalline drug nanoparticles: Methodologies and significance

Molecular Pharmaceutics

Volumn 7, Issue 5, 2010, Pages 1858-1870

  Van Eerdenbrugh, Bernard ^a,b   Vermant, Jan ^c   Martens, Johan A ^c   Froyen, Ludo ^c   Humbeeck, Jan Van ^c   Van Den Mooter, Guy ^b   Augustijns, Patrick ^b  

^a PURDUE UNIVERSITY   (United States)

^b DEPARTMENT OF PHARMACEUTICAL AND PHARMACOLOGICAL SCIENCES   (Belgium)

^c UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Crystalline drug nanosuspensions; Mie scattering; nanosuspension solubility; Ostwald Freundlich equation; solubility determination

Indexed keywords

EXCIPIENT; ITRACONAZOLE; LOVIRIDE; NAPROXEN; PHENYTOIN; SULFATHIAZOLE; TOCOFERSOLAN;

ARTICLE; CENTRIFUGATION; DRUG SOLUBILITY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; LIGHT SCATTERING; NANOFILTRATION; NANOSUSPENSION; PARTICLE SIZE; PRIORITY JOURNAL; REFRACTION INDEX; SEPARATION TECHNIQUE; SOLUBILIZATION; SUSPENSION; TURBIDITY; ULTRACENTRIFUGATION;

ACETAMIDES; ACETOPHENONES; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; DRUG STABILITY; EXCIPIENTS; ITRACONAZOLE; LIGHT; MICELLES; NANOPARTICLES; NAPROXEN; NEPHELOMETRY AND TURBIDIMETRY; PARTICLE SIZE; PHENYTOIN; POLYETHYLENE GLYCOLS; SCATTERING, RADIATION; SOLUBILITY; SUSPENSIONS; VITAMIN E;

EID: 77957729463     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp100209b     Document Type: Article

References (32)

1. Kesisoglou, F.; Panmai, S.; Wu, Y. Nanosizing-Oral formulation development and biopharmaceutical evaluation Adv. Drug Delivery Rev. 2007, 59, 631-644
2. Van Eerdenbrugh, B.; Van den Mooter, G.; Augustijns, P. Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products (mini-review) Int. J. Pharm. 2008, 364, 64-75
3. Rabinow, B. E. Nanosuspensions in drug delivery Nat. Rev. Drug Discovery 2004, 3, 785-796
4. Van Eerdenbrugh, B.; Vermant, J.; Martens, J. A.; Froyen, L.; Van Humbeeck, J.; Augustijns, P.; Van den Mooter, G. A Screening Study of Surface Stabilization During the Production of Drug Nanocrystals J. Pharm. Sci. 2009, 98, 2091-2103
5. Müller, R. H.; Möschwitzer, J.; Bushrab, F. N. Manufacturing of Nanoparticles by Milling and Homogenization Techniques. In Nanoparticle Technology for Drug Delivery, Drugs and the pharmaceutical sciences; Gupta, R. B.; Kompella, U. B., Eds.; Taylor & Francis Group, LLC: New York, 2006; Vol. 159, pp 21 - 51.
6. Müller, R. H.; Böhm, B. H. L. Nanosuspensions. In Emulsions and Nanosuspensions for the Formulation of Poorly Soluble Drugs; Müller, R. H.; Benita, S.; Böhm, B. H. L., Eds.; Medpharm Scientific: Stuttgart, 1998; pp 149 - 174.
7. Müller, R. H.; Böhm, B. H. L.; Grau, M. J. Nanosuspensions: A Formulation Approach for Poorly Soluble and Poorly Bioavailable Drugs. In Handbook of Pharmaceutical Controlled Release Technology; Wise, D. L., Ed.; Marcel Dekker, Inc.: New York, 2000; pp 345 - 357.
8. Radtke, M. Pure Drug Nanoparticles for the Formulation of Poorly Soluble Drugs New Drugs 2001, 3, 62-68
9. Kesisoglou, F.; Panmai, S.; Wu, Y. Application of Nanoparticles in Oral Delivery of Immediate Release Formulations Curr. Nanosci. 2007, 3, 183-190
10. Grant, D. J. W.; Brittain, H. G. Solubility of Pharmaceutical Solids. In Physical Characterization of Pharmaceutical Solids, Drugs and the pharmaceutical sciences; Brittain, H. G., Ed.; Marcel Dekker, Inc.: New York, 1995; Vol. 70, pp 321 - 386.
11. Müller, R. H.; Peters, K. Nanosuspensions for the formulation of poorly soluble drugs-I. Preparation by a size-reduction technique Int. J. Pharm. 1998, 2, 229-237
12. Hecq, J.; Deleers, M.; Fanara, D.; Vranckx, H.; Amighi, K. Preparation and characterization of nanocrystals for solubility and dissolution rate enhancement of nifedipine Int. J. Pharm. 2005, 299, 167-177
13. Dai, W. G.; Dong, L. C.; Song, Y. Q. Nanosizing of a drug/carrageenan complex to increase solubility and dissolution rate Int. J. Pharm. 2007, 342, 201-207
14. Gao, L.; Zhang, D.; Chen, M.; Zheng, T.; Wang, S. Preparation and Characterization of an Oridonin Nanosuspension for Solubility and Dissolution Velocity Enhancement Drug Dev. Ind. Pharm. 2007, 33, 1332-1339
15. Van Eerdenbrugh, B.; Stuyven, B.; Froyen, L.; Van Humbeeck, J.; Martens, J. A.; Augustijns, P.; Van den Mooter, G. Downscaling Drug Nanosuspension Production: Processing Aspects and Physicochemical Characterization AAPS PharmSciTech 2009, 10, 44-53
16. Kaneniwa, N.; Otsuka, M.; Hayashi, T. Physicochemical Characterization of Indomethacin Polymorphs and the Transformation Kinetics in Ethanol Chem. Pharm. Bull. 1985, 33, 3447-3455
17. Anwar, J.; Tarling, S. E.; Barnes, P. Polymorphism of Sulfathiazole J. Pharm. Sci. 1989, 78, 337-342
18. Saveyn, H.; Mermuys, D.; Thas, O.; van der Meeuwen, P. Determination of the refractive index of water-dispersible granules for use in laser diffraction experiments Part. Part. Syst. Charact. 2002, 19, 426-432
19. Absorption and scattering of light by small particles; Bohren, C. F.; Huffman, D. R., Eds.; Wiley & Sons, Inc.: New York, 1983.
20. Keck, C. M. Cyclosporin nanosuspensions: optimized size characterization and oral formulations. PhD Thesis. http://www.diss.fu-berlin.de/diss/receive/ FUDISS-thesis-000000002344.
21. Yang, L.; Alexandridis, P. Small-angle neutron scattering investigation of the temperature-dependent aggregation behavior of the block copolymer Pluronic L64 in aqueous solution Langmuir 2000, 16, 8555-8561
22. Goldmints, I.; Yu, G.; Booth, C.; Smith, K. A.; Hatton, T. A. Structure of (deuterated PEO)-(PPO)-(deuterated PEO) block copolymer micelles as determined by small angle neutron scattering Langmuir 1999, 15, 1651-1656
23. Eastman Chemical Company. Vitamine E TPGS-Applications and properties; Technical Brochure; 2005, PCI-102B.
24. Yu, L.; Bridgers, A.; Polli, J.; Vickers, A.; Long, S.; Roy, A.; Winnike, R.; Coffin, M. Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability Pharm. Res. 1999, 16, 1812-1817
25. Kanke, M.; Sekiguchi, K. Dissolution Behavior of Solid Drugs. II. Determination of the Transition Temperature of Sulfathiazole Polymorphs by Measuring the Initial Dissolution Rates Chem. Pharm. Bull. 1973, 21, 878-884
26. Lindfors, L.; Forssén, S.; Skantze, P.; Skantze, U.; Zackrisson, A.; Olsson, U. Amorphous Drug Nanosuspensions. 2. Experimental Determination of Bulk Monomer Concentrations Langmuir 2006, 22, 911-916
27. van de Hulst, H. C. Rigorous scattering theory for spheres of arbitrary size (Mie theory). In Light Scattering by Small Particles; van de Hulst, H. C., Ed.; Dover Publications, Inc.: New York, 1981; pp 114 - 130.
28. Sharma, P. K.; Bhatia, S. R. Effect of anti-inflammatories on Pluronic® F127: micellar assembly, gelation and partitioning Int. J. Pharm. 2004, 278, 361-377
29. Sharma, P. K.; Reilly, M. J.; Jones, D. N.; Robinson, P. M.; Bhatia, S. R. The effect of pharmaceuticals on the nanoscale structure of PEO-PPO-PEO micelles Colloids Surf. 2008, B61, 53-60
30. Matteucci, M. E.; Brettmann, B. K.; Rogers, T. L.; Elder, E. J.; Williams, R. O.; Johnston, K. P. Design of Potent Amorphous Drug Nanoparticles for Rapid Generation of Highly Supersaturated Media Mol. Pharmaceutics 2007, 4, 782-793
31. Lindfors, L.; Forssén, S.; Westergren, J.; Olsson, U. Nucleation and crystal growth in supersaturated solutions of a model drug J. Colloid Interface Sci. 2008, 325, 404-413
32. Zhang, G. G. Z.; Law, D.; Schmitt, E. A.; Qiu, Y. Phase transformation considerations during process development and manufacture of solid oral dosage forms Adv. Drug Delivery Rev. 2004, 56, 371-390