Title: A screening study of surface stabilization during the production of drug nanocrystals
Authors: Van Eerdenbrugh, Bernard
Vermant, Jan
Martens, Johan
Froyen, Ludo
Van Humbeeck, Jan
Augustijns, Patrick
Van den Mooter, Guy # ×
Issue Date: Jun-2009
Publisher: American Chemical Society and American Pharmaceutical Association
Series Title: Journal of Pharmaceutical Sciences vol:98 issue:6 pages:2091-2103
Abstract: In order to establish a knowledge base for nanosuspension production, a screening was performed on 13 different stabilizers at 3 concentrations for 9 structurally different drug compounds. Concerning the stabilizers tested, the group of semi-synthetic polymers was the least performant (stable nanosuspensions were obtained in only 1 out of 10 cases). For the linear synthetic polymers, better results were obtained with povidones, however poly(vinyl alcohol) did not result in adequate stabilization. The synthetic copolymers showed even higher success rates, resulting in nanosuspensions in two out of three cases when applied at a 100 wt% concentration (relative to the drug weight). Finally, the surfactants gave the best results, with TPGS being successful at concentrations of 25 or 100 wt% of the drug weight for all compounds tested. From the point of view of drug compound, large differences could be observed upon evaluation of the relative number of formulations of that compound resulting in nanosuspensions. It was found that the hydrophobicity of the surfaces, as estimated by the adsorbed amount of TPGS per unit of surface area of nanosuspensions stabilized with 25 wt% TPGS, was decisive for the agglomeration tendency of the particles and hence the ease of nanosuspensions stabilization. (c) 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci.
ISSN: 0022-3549
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Soft Matter, Rheology and Technology Section
Centre for Surface Chemistry and Catalysis
Physical Metallurgy and Materials Engineering Section (-)
Drug Delivery and Disposition
× corresponding author
# (joint) last author

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