Title: Enhanced absorption of the poorly soluble drug fenofibrate by tuning its release rate from ordered mesoporous silica
Authors: Van Speybroeck, Michiel ×
Mellaerts, Randy
Mols, Rafaƫl
Do Thi, Thao
Martens, Johan
Van Humbeeck, Jan
Annaert, Pieter
Van den Mooter, Guy
Augustijns, Patrick #
Issue Date: Dec-2010
Publisher: Elsevier
Series Title: European Journal of Pharmaceutical Sciences vol:41 issue:5 pages:623-630
Abstract: The aim of the present study was to evaluate the effect of release rate from ordered mesoporous silica materials on the rate and extent of absorption of the poorly soluble drug fenofibrate. Three ordered mesoporous silica materials with different pore diameter (7.3 nm, 4.4nm and 2.7 nm) were synthesized and loaded with fenofibrate via impregnation. Release experiments were conducted under sink conditions and under supersaturating conditions in biorelevant media, simulating the fasted and the fed state. Subsequently, all silica-based formulations were evaluated in vivo (rat model). The release experiments under sink conditions indicated a clear increase in release rate with increasing pore size. However, under supersaturating conditions (FaSSIF), the, pharmaceutical performance (in terms of both the degree and duration of supersaturation), increased with decreasing pore size. The same trend was observed in vivo (fasted state): the area under the plasma concentration–time profile amounted to 102±34Mh, 86±19Mh
and 20±13Mh for the materials with pore diameter of 2.7 nm, 4.4nm and 7.3 nm, respectively. The results of this, study demonstrate that a decrease in drug release rate – and thus, a decrease of the rate at which supersaturation is created – is beneficial to the absorption of fenofibrate.
ISSN: 0928-0987
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Drug Delivery and Disposition
Centre for Surface Chemistry and Catalysis
Physical Metallurgy and Materials Engineering Section (-)
× corresponding author
# (joint) last author

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