Characterization of Physicochemical Properties of Spray-dried Solid Dispersions Loaded with Unmodified Crystalline Fenofibrate

Author(s): Abid Mehmood Yousaf , Dong Wuk Kim , Jong Oh Kim , Pahn-Shick Chang , Hyung Hee Baek , Soo-Jeong Lim , Kwan Hyung Cho , Chul Soon Yong , Han-Gon Choi .

Journal Name: Current Pharmaceutical Analysis

Volume 11 , Issue 2 , 2015

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Abstract:

To accomplish a new solid dispersion providing optimized aqueous solubility and dissolution of fenofibrate without modifying the crystalline nature of the hydrophobic drug, different formulations were prepared with water, polyvinylpyrrolidone (PVP) and sodium lauryl sulphate (SLS) using the spray-drying technique. The influence of the relative quantities of PVP and SLS on the dissolution and aqueous solubility of fenofibrate in the solid dispersion was determined. The solid dispersion exhibiting highest solubility and dissolution was subjected to scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) for physicochemical characterization. Converse to other conventional solid dispersion systems, this solid dispersion diminished the hydrophobicity of the drug by adhering hydrophilic constituents to the irregular surface of the crystalline drug during the spray drying process. In particular, the solid dispersion containing fenofibrate/PVP/SLS at a ratio of 2.5/1.5/1 (w/w/w) enormously ameliorated the aqueous solubility of fenofibrate compared to the drug powder (53.46±4.69 vs. 0.004±0.001 μg/ml). Moreover, the dissolution was approximately 75% at 30 minutes with this solid dispersion. Thus, the solid dispersion loaded with the crystalline fenofibrate might be a promising pharmaceutical product to administer poorly water-soluble drug via the oral route.

Keywords: Crystalline, dissolution, fenofibrate, solid dispersion, solubility, spray-drying.

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Article Details

VOLUME: 11
ISSUE: 2
Year: 2015
Page: [139 - 144]
Pages: 6
DOI: 10.2174/1573412910666141110223457
Price: $58

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