期刊
COLLOIDS AND SURFACES B-BIOINTERFACES
卷 101, 期 -, 页码 475-480出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.colsurfb.2012.07.019
关键词
Anti-emetics; Caco-2 cell; Enhanced permeation; Granisetron; Lipid nanoemulsion
资金
- Sunchon National University Research Fund
- National Research Foundation of Korea (NRF)
- Korean government (MEST) [2011-0030635]
A new lipid nanoemulsion (DIE) system containing granisetron (GRN) was developed and its in vitro permeation-enhancing effect was evaluated using Caco-2 cell monolayers. Particle size, polydispersity index (PI) and stability of the prepared GRN-loaded LNE systems were also characterized. The mean diameters of prepared LNEs were around 50 nm with PI < 0.2. Developed LNEs were stable at 4 degrees C in the dark place over a period of 12 weeks. In vitro drug dissolution and cytotoxicity studies of GRN-loaded LNEs were performed. GRN-loaded LNEs exhibited significantly higher drug dissolution than GRN suspension at pH 6.8 for 2h (P<0.05). In vitro permeation study in Caco-2 cell monolayers showed that the LNEs significantly enhanced the drug permeation compared to GRN powder. The in vivo toxicity study in the rat jejunum revealed that the prepared GRN-loaded LNE was as safe as the commercial formulation (Kytril). These results suggest that LNE could be used as a potential oral liquid formulation of GRN for anti-emetic treatment on the post-operative and chemotherapeutic patients. (C) 2012 Elsevier B.V. All rights reserved.
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