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

Tran, Tuan Hiep, Poudel, Bijay K., Marasini, Nirmal, Chi, Sang-Cheol, Choi, Han-Gon, Yong, Chul Soon and Kim, Jong Oh (2013) Preparation and evaluation of raloxifene-loaded solid dispersion nanoparticle by spray-drying technique without an organic solvent. International Journal of Pharmaceutics, 443 1-2: 50-57. doi:10.1016/j.ijpharm.2013.01.013


Author Tran, Tuan Hiep
Poudel, Bijay K.
Marasini, Nirmal
Chi, Sang-Cheol
Choi, Han-Gon
Yong, Chul Soon
Kim, Jong Oh
Title Preparation and evaluation of raloxifene-loaded solid dispersion nanoparticle by spray-drying technique without an organic solvent
Journal name International Journal of Pharmaceutics   Check publisher's open access policy
ISSN 0378-5173
1873-3476
Publication date 2013-02-25
Year available 2013
Sub-type Article (original research)
DOI 10.1016/j.ijpharm.2013.01.013
Open Access Status Not Open Access
Volume 443
Issue 1-2
Start page 50
End page 57
Total pages 8
Place of publication Amsterdam, Netherlands
Publisher Elsevier BV
Language eng
Formatted 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 AUC0-∞ and Cmax 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.
Keyword Bioavailability
Nanoparticles
Raloxifene
Solubility
Spray drying
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Chemistry and Molecular Biosciences
 
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Created: Sat, 04 Jun 2016, 12:39:44 EST by Nirmal Marasini on behalf of Learning and Research Services (UQ Library)