Journal
JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
Volume 14, Issue 7, Pages 4820-4831Publisher
AMER SCIENTIFIC PUBLISHERS
DOI: 10.1166/jnn.2014.8722
Keywords
Bioavailability; Lymphatic Transport; Oral Drug Delivery; Raloxifene; Solid Lipid Nanoparticles
Categories
Funding
- National Research Foundation of Korea (NRF)
- Ministry of Education, Science and Technology [2012R1A2A2A02044997, 2012R1A1A1039059]
- National Research Foundation of Korea [2012R1A1A1039059] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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.
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