Title: Solubility increases associated with crystalline drug nanoparticles: Methodologies and significance
Authors: Van Eerdenbrugh, Bernard ×
Vermant, Jan
Martens, Johan
Froyen, Ludo
Van Humbeeck, Jan
Van den Mooter, Guy
Augustijns, Patrick #
Issue Date: 2010
Publisher: American Chemical Society
Series Title: Molecular Pharmaceutics vol:7 issue:5 pages:1858-1870
Abstract: In this manuscript, the determination of solubility of crystalline drug nanosuspensions by a range of methods is critically investigated. As the determinations of solubility were performed in the presence of the solubilizing nanosuspension stabilizer D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS), the potential effects of this excipient on the measurements were studied first, Solubility data of nanosuspensions of itraconazole, loviride, phenytoin and naproxen were generated using different methodologies. Data obtained using separation-based methodologies (centrifugation, filtration and ultracentrifugation) proved to be of limited use, due to poor nanoparticle separation efficiencies and/or significant adsorption of TPGS onto the nanoparticle surfaces. Light scattering and turbidity were found to be more suitable for the determination of nanosuspension solubility. The obtained data show that, unlike earlier reports, the solubility increases due to nanosizing are small, with measured increases of only 15%. These solubility increases are in fair agreement with what would be predicted based on the Ostwald-Freundlich equation.
ISSN: 1543-8384
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Drug Delivery and Disposition
Soft Matter, Rheology and Technology Section
Centre for Surface Chemistry and Catalysis
Physical Metallurgy and Materials Engineering Section (-)
× corresponding author
# (joint) last author

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