Formulation and Optimization of Raloxifene-Loaded Solid Lipid Nanoparticles to Enhance Oral Bioavailability

Title
Formulation and Optimization of Raloxifene-Loaded Solid Lipid Nanoparticles to Enhance Oral Bioavailability
Author(s)
김종오트란탄힙티르거네쉬라마사미조혁준김용일포우델비자이최한곤[최한곤]용철순
Keywords
PHYSICOCHEMICAL CHARACTERIZATION; DRUG-DELIVERY; PHARMACOKINETICS; CARRIERS; HYDROCHLORIDE; STABILITY; SLN(TM); SOLVENT; PLASMA; SYSTEM
Issue Date
201407
Publisher
AMER SCIENTIFIC PUBLISHERS
Citation
JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY, v.14, no.7, pp.4820 - 4831
Abstract
The main aim of this study was to improve the oral bioavailability of raloxifene (RXF), a selective estrogen receptor modulator, by incorporation into solid lipid nanoparticles (SLN). RXF-loaded SLN was prepared by homogenization-sonication technique and characterized through physicochemical, pharmacokinetic, and cytotoxicity studies. The optimized SLN formulation exhibited a spherical shape with average size around 140 nm, easing its transport across the lymphatic system. Augmentation in the profiles of C-max (308%) and AUC (270%) indicated a significant enhancement in the rate and extent of bioavailability by SLN formulations compared to free drug. In vitro cytotoxicity study performed in NIH-3T3 cells revealed that RXF-SLN was cytocompatible, and SLN remained unchanged during the freeze-drying process. Furthermore, the optimized formulation was quite stable at room temperature for more than two months, exemplifying its superior performance. In conclusion, SLN provides a promising platform for the pronounced enhancement of RXF bioavailability.
URI
http://hdl.handle.net/YU.REPOSITORY/31574http://dx.doi.org/10.1166/jnn.2014.8722
ISSN
1533-4880
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약학대학 > 약학부 > Articles
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