title: A novel lipid nanoemulsion system for improved permeation of granisetron.
abstract: A new lipid nanoemulsion (LNE) 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°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.
authors.affiliation: College of Pharmacy, Pusan National University, Busan 609-735, Republic of Korea.
authors.forename: Hea-Jeong
authors.initials: HJ
authors.lastname: Doh
authors.forename: Yunjin
authors.initials: Y
authors.lastname: Jung
authors.forename: Prabagar
authors.initials: P
authors.lastname: Balakrishnan
authors.forename: Hyun-Jong
authors.initials: HJ
authors.lastname: Cho
authors.forename: Dae-Duk
authors.initials: DD
authors.lastname: Kim
mesh_terms: D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D002470:Cell Survival / Q000187:drug effects; D004655:Emulsions; D017829:Granisetron / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D007583:Jejunum / Q000187:drug effects; D008055:Lipids; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D051381:Rats; D012995:Solubility
chemical_list: D000932:Antiemetics; D004655:Emulsions; D017829:Granisetron; D008055:Lipids