Enhanced Bioavailability of Poorly Soluble Drugs by Co-spray Drying with Mesoporous Materials

Shou-Cang Shen1, Wai Kiong Ng1, Leonard Chia1, Reginald B. H. Tan1,2

1 Institute of Chemical and Engineering Sciences, 1 Pesek Road, Jurong Island, Singapore 627833. 2 Department of Chemical and Biomolecular Engineering, The National University of Singapore, 4 Engineering Drive 4, Singapore 117576

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Summary
Co-spray drying with ordered mesoporous silica (such as SBA-15) exhibited excellence in enhancement of bioavailability for poorly aqueous-soluble drugs by production of stable amorphous solid dispersion. Model poorly soluble drugs, such as ibuprofen (IBU), indomethacin (IDMC) and fenofibrate (FEN) have been investigated in this study. After co-spray drying, most drug molecules were entrapped inside the straight mesoporous channels and the morphology of SBA-15 submicron particles remained unchanged. IBU confined inside the mesoporous structure was in the amorphous state shown by PXRD and DSC measurements. The amorphous state of IBU in the solid dispersion showed remarkable stability when subject to stress test condition of 40°C/75%RH in open pans for 12 months. The dissolution rate of IBU from the co-spray dried solid dispersion was significantly enhanced to achieve a rapid release. Even after the accelerated stability test, the rapid drug release property was well preserved.

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