Journal
MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS
Volume 58, Issue -, Pages 1131-1137Publisher
ELSEVIER
DOI: 10.1016/j.msec.2015.09.018
Keywords
Starch; Three-dimensional ordered macroporous; Felodipine; Insoluble drug; The dissolution rate; Relative bioavailability
Categories
Funding
- National Natural Science Foundation of China [81302707]
- Natural Science Foundation of Liaoning Province [2013022052]
- Principal Fund of Liaoning Medical University [AH2014020]
- Dr. Start-up Foundation of Liaoning Province [20141195]
- Construction of Clinical Cardiovascular System Drug Evaluation Research Technology platform [2012ZX09303016-002]
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In this study, silica nanospheres with different particle sizes were used as hard template for synthesis of a starch with a novel three-dimensional ordered macroporous structure (3DOMTS). As a pharmaceutical adjuvant, 3DOMTS was used to improve the dissolution rate and oral relative bioavailability of water-insoluble drugs. Felodipine (FOP) was chosen as a model drug and was loaded into the 3DOMTS by solvent evaporation. FOP loading into 3DOMTS with different pore sizes was characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), differential scanning calorimeter (DSC), powder X-ray diffractometer (PXRD) and Fourier-Transform Infrared (FTIR). The results obtained showed that FOP was present in the pores in an amorphic or microcrystalline state. The in vitro dissolution results showed that 3DOMTS could effectively improve the dissolution rate of FOP in comparison with commercial common tablets. Pharmacokinetic results indicated that the oral relative bioavailability of self-made FDP-3DOMTS tablets were 184%, showing that 3DOMTS produced a significantly increased oral absorption of FOP. In conclusion, 3DOMTS exhibits the dual potential of improving the dissolution rate of poorly water soluble drugs and the novel filler produced by direct compression technology confirming that 3DOMTS will be useful for many applications in the field of pharmaceutics. (c) 2015 Elsevier B.V. All rights reserved.
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