Reference : Impregnation of mesoporous silica with poor aqueous soluble molecule using pressurize...
Scientific journals : Article
Engineering, computing & technology : Materials science & engineering
Physical, chemical, mathematical & earth Sciences : Chemistry
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/247409
Impregnation of mesoporous silica with poor aqueous soluble molecule using pressurized carbon dioxide: is the solubility in the supercritical and subcritical phase a critical parameter?
English
Koch, Nathan [University of Liège (ULiège), Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, Belgium > > > >]
Jennotte, Olivier [University of Liège (ULiège), Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, Belgium > > > >]
Grignard, Bruno [University of Liège (ULiège), Complex and Entangled Systems from Atoms to Materials (CESAM) Research Unit, Center for Education and Research on Macromolecules (CERM), Belgium > > > >]
Lechanteur, Anna [University of Liège (ULiège), Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, Belgium > > > >]
Evrard, Brigitte mailto [University of Liège (ULiège), Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, Belgium > > > >]
1-Jul-2020
European Journal of Pharmaceutical Sciences
Elsevier
150
105332
Yes (verified by ORBi)
International
0928-0987
1879-0720
Amsterdam
Netherlands
[en] supercritical carbon dioxide ; mesoporous silica
[en] Recently, mesoporous silica (MS) has been used as a material able to maintain amorphous state of active compounds and therefore, enhance the oral bioavailability of BCSII drugs. Among impregnation methods of MS, techniques using supercritical carbon dioxide (sc-CO2) are promising tools. Solubility of compounds in sc-CO2 is reported as one of the most critical parameters, which usually limits its use in drug formulation. Indeed, most of compounds have poor solubility in sc-CO2. The aim of this work is to compare different MS and to study alternative processes using pressurized CO2 for insoluble molecule in sc-CO2. By using high pressure reactor, DSC, HPLC and in vitro dissolution tests, the crystallinity and dissolution profiles of MS with different pore size (6.6 nm, 25.0 nm and 2.5 nm) impregnated with fenofibrate (FF) under sc-CO2 were compared to select the most appropriate carrier. Then, the selected MS has been impregnated under supercritical, subcritical and atmospheric conditions. We have shown that the MS pore size of 6.6 nm provides the higher amorphous drug loading capacity as well as the faster and higher drug dissolution. In addition, FF-MS formulations produced with pressurized CO2 as fusion medium, both in subcritical and supercritical conditions; give similar crystallinity and dissolution results compared to those produced with supercritical fluids as solvent. Through this study, we show new possibilities of using CO2 for insoluble compounds in this fluid.
Center for Education and Research on Macromolecules (CERM) ; Complex and Entangled Systems from Atoms to Materials (CESAM) Research Unit ; Laboratory of Pharmaceutical Technology and Biopharmacy
FEDER - Fonds Européen de Développement Régional
SOLPHARE project
Researchers
http://hdl.handle.net/2268/247409
10.1016/j.ejps.2020.105332

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