Preparation and evaluation of raloxifene-loaded solid dispersion nanoparticle by spray-drying technique without an organic solvent

Title
Preparation and evaluation of raloxifene-loaded solid dispersion nanoparticle by spray-drying technique without an organic solvent
Author(s)
김종오트란탄힙포우델비자이마라시니니르말지상철[지상철]최한곤[최한곤]용철순
Keywords
DISSOLUTION RATE; IBUPROFEN; BIOAVAILABILITY; SOLUBILITY; DELIVERY; HCL
Issue Date
201302
Publisher
ELSEVIER SCIENCE BV
Citation
INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.443, no.1-2, pp.50 - 57
Abstract
The aim of this study was to improve the physicochemical properties and bioavailability of a poorly water-soluble drug, raloxifene by solid dispersion (SD) nanoparticles using the spray-drying technique. These spray-dried SD nanoparticles were prepared with raloxifene (RXF), polyvinylpyrrolidone (PVP) and Tween 20 in water. Reconstitution of optimized RXF-loaded SD nanoparticles in pH 1.2 medium showed a mean particle size of approximately 180 nm. X-ray diffraction and differential scanning calorimetry indicated that RXF existed in an amorphous form within spray-dried nanoparticles. The optimized formulation showed an enhanced dissolution rate of RXF at pH 1.2, 4.0, 6.8 and distilled water as compared to pure RXF powder. The improved dissolution of raloxifene from spray-dried SD nanoparticles appeared to be well correlated with enhanced oral bioavailability of raloxifene in rats. Furthermore, the pharmacokinetic parameters of the spray-dried SD nanoparticles showed increased AUC(0-infinity) and C-max of RXF by approximately 3.3-fold and 2.3-fold, respectively. These results suggest that the preparation of RXF-SD nanoparticles using the spray drying technique without organic solvents might be a promising approach for improving the oral bioavailability of RXF. (C) 2013 Elsevier B.V. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/26527http://dx.doi.org/10.1016/j.ijpharm.2013.01.013
ISSN
0378-5173
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약학대학 > 약학부 > Articles
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