Journal
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
Volume 87, Issue 1, Pages 114-124Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejpb.2013.12.015
Keywords
Raloxifene HCl; Solid lipid nanoparticle; Box-Bhenken design; Design of experiments; Everted gut sac; Lymphatic transport; Glyceryl behenate
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Funding
- University Grants Commission (UGC), India [39-176/2010 (SR)]
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Raloxifene HCI (RLX) shows low oral bioavailability (<2%) in humans due to poor aqueous solubility and extensive (>90%) metabolism in gut. Lipid nanoparticles (SLN) with glyceryl tribehenate were designed to enhance drug's oral bioavailability. Box-Bhenken design was used to optimize manufacturing conditions. Optimized SLN had particle size of 167 +/- 3 nm and high encapsulation efficiency (>92%). Oral bioavailability of RLX from SLN was improved by 3.24 folds compared to free RLX in female Wistar rats. Both clathrin and caveolae mediated endocytosis pathways were involved in the uptake of SLN. Lymphatic transport inhibitor, cycloheximide significantly reduced oral bioavailability of SLN. (C) 2014 Elsevier B.V. All rights reserved.
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