Top-Down Production of Drug Nanocrystals - Nanosuspension Stabilization, Miniaturization and Transformation Into Solid Products

In this presentation, a number of subtopics of crystalline drug nanosuspensions will be discussed. The main focus lies on (i) their physical stabilization, and (ii) spray-drying and freeze-drying processes for further transformation into solid products. For both, the conservation of the beneficial dissolution properties of the nanosuspensions is considered as a key evaluation criterion.

Relevant references:

[1] Van Eerdenbrugh B, Vermant J, Martens JA, Froyen L, Van Humbeeck J, Augustijns P, Van den Mooter G. 2009. A screening study of surface stabilization during the production of drug nanocrystals. J Pharm Sci. 98(6): 2091-2103.

[2] Van Eerdenbrugh B, Stuyven B, Froyen L, Van Humbeeck J, Martens JA, Augustijns P, Van den Mooter G. 2009. Downscaling drug nanosuspension production: processing aspects and physicochemical characterization. AAPS PharmSciTech. 10(1): 44-53.

[3] Van Eerdenbrugh B, Van den Mooter G, Augustijns P. 2008. Top-down production of drug nanocrystals: nanosuspension stabilization, miniaturization and transformation into solid products (mini-review). Int J Pharm. 364(1): 64-75.

[4] Van Eerdenbrugh B, Froyen L, Van Humbeeck J, Martens JA, Augustijns P, Van den Mooter G. 2008. Alternative matrix formers for nanosuspension solidification: Dissolution performance and X-ray microanalysis as an evaluation tool for powder dispersion. Eur J Pharm Sci. 35(4): 344-353.

[5] Van Eerdenbrugh B, Vercruysse S, Martens JA, Vermant J, Froyen L, Van Humbeeck J, Van den Mooter G, Augustijns P. 2008. Microcrystalline cellulose, a useful alternative for sucrose as a matrix former during freeze-drying of drug nanosuspensions - a case study with itraconazole. Eur J Pharm Biopharm. 70(2): 590-596.

[6] Van Eerdenbrugh B, Froyen L, Van Humbeeck J, Martens JA, Augustijns P, Van den Mooter G. 2008. Drying of crystalline drug nanosuspensions - the importance of surface hydrophobicity on dissolution behavior upon redispersion. Eur J Pharm Sci. 35(1-2): 127-135.

[7] Van Eerdenbrugh B, Froyen L, Martens JA, Blaton N, Augustijns P, Brewster M, Van den Mooter G. 2007. Characterization of physico-chemical properties and pharmaceutical performance of sucrose co-freeze-dried solid nanoparticulate powders of the anti-HIV agent loviride prepared by media milling. Int J Pharm. 338(1-2): 198-206.