Cytotoxicity and Biological Efficacy of Exendin-4-Encapsulated Solid Lipid Nanoparticles in INS-1 Cells

• Main Authors: Hee-Sook Jun, Gongdeuk Bae, Young Tag Ko, Yoon Sin Oh
• Format: Article
• Language: English
• Published: Hindawi Limited 2015-01-01
• Series: Journal of Nanomaterials
• Online Access: http://dx.doi.org/10.1155/2015/753569

Exendin-4 (Ex-4), a peptide of glucagon-like peptide-1 receptor agonist, is a potent insulinotropic agent and alternative drug delivery systems to increase therapeutic utility have been explored. We developed exendin-4-encapsulated solid lipid nanoparticles (Eudragit Ex-4 SLNs) and compared the effects of Eudragit Ex-4 SLNs with those of native Ex-4 on INS-1 cells. We observed no significant toxic effects of nanoparticles at concentrations from 1 nM to 100 nM. Similar to Ex-4, Eudragit Ex-4 SLNs stimulated the production of cyclic AMP at 10 nM. Moreover, unlike treatment with the vehicle, treatment with 10 nM Eudragit Ex-4 SLNs increased insulin mRNA levels and insulin secretion. These insulinotropic effects of Eudragit Ex-4 SLNs were comparable to those of Ex-4. Thus, our in vitro results suggest that the biological effects of Eudragit Ex-4 SLNs are similar to those of Ex-4, and further in vivo pharmacokinetic studies are required to propose an alternative sustained release drug system.