Abstract
Olanzapine, a lipophilic antipsychotic drug, has poor oral bioavailability due to hepatic first-pass metabolism. Solid Lipid Nanoparticles (SLNs) of Olanzapine were developed using lipids (Stearic acid and Glyceryl monostearate), soy lecithin, poloxamer 188 and charge modifier stearyl amine by microemulsion technique. The aim of this research was to find out whether the bioavailability of olanzapine can be improved by administering olanzapine SLN orally to Wistar rats. Area under curve was increased (up to 4-fold) and clearance was decreased when olanzapine entrapped in SLNs with stearylamine were administered orally compared with that of olanzapine suspension. The enhanced relative bioavailability by the SLNs formulation might be attributed to avoidance of first-pass hepatic metabolism by intestinal lymphatic transport, direct uptake of nanoparticles through the GI tract, increased permeability by surfactants, and decreased degradation and clearance. These results indicate that olanzapine can be loaded into solid lipid nanoparticles for improvement of its oral bioavailability.
Keywords: Bioavailability, cationic, microemulsion, olanzapine, oral delivery, solid lipid nanoparticles
Current Nanoscience
Title:Olanzapine Loaded Cationic Solid Lipid Nanoparticles for Improved Oral Bioavailability
Volume: 9 Issue: 1
Author(s): Sumeet Sood, Natarajan Jawahar, Kunal Jain, Kuppusamy Gowthamarajan and Subramania Nainar Meyyanathan
Affiliation:
Keywords: Bioavailability, cationic, microemulsion, olanzapine, oral delivery, solid lipid nanoparticles
Abstract: Olanzapine, a lipophilic antipsychotic drug, has poor oral bioavailability due to hepatic first-pass metabolism. Solid Lipid Nanoparticles (SLNs) of Olanzapine were developed using lipids (Stearic acid and Glyceryl monostearate), soy lecithin, poloxamer 188 and charge modifier stearyl amine by microemulsion technique. The aim of this research was to find out whether the bioavailability of olanzapine can be improved by administering olanzapine SLN orally to Wistar rats. Area under curve was increased (up to 4-fold) and clearance was decreased when olanzapine entrapped in SLNs with stearylamine were administered orally compared with that of olanzapine suspension. The enhanced relative bioavailability by the SLNs formulation might be attributed to avoidance of first-pass hepatic metabolism by intestinal lymphatic transport, direct uptake of nanoparticles through the GI tract, increased permeability by surfactants, and decreased degradation and clearance. These results indicate that olanzapine can be loaded into solid lipid nanoparticles for improvement of its oral bioavailability.
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Cite this article as:
Sood Sumeet, Jawahar Natarajan, Jain Kunal, Gowthamarajan Kuppusamy and Nainar Meyyanathan Subramania, Olanzapine Loaded Cationic Solid Lipid Nanoparticles for Improved Oral Bioavailability, Current Nanoscience 2013; 9 (1) . https://dx.doi.org/10.2174/1573413711309010007
DOI https://dx.doi.org/10.2174/1573413711309010007 |
Print ISSN 1573-4137 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6786 |
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