A novel lipid nanoemulsion system for improved permeation of granisetron

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 2 h (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.

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► Granisetron (GRN)-loaded novel lipid nanoemulsion (LNE) systems were prepared.
► Nano-sized spherical droplet was observed and drug release from LNEs was improved.
► In vitro permeation of GRN from LNEs was enhanced.
► In vitro and in vivo toxicity of GRN-loaded LNE seemed to be negligible.