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Stimulation of GLP-1 secretion and delivery of GLP-1 agonists via nanostructured lipid carriers


Nanoparticulate based drug delivery systems have been extensively studied to efficiently encapsulate and deliver peptides orally. However, most of the existing data mainly focus on the nanoparticles as a drug carrier, but the ability of nanoparticles itself having biological effect have not been exploited. Herein, we hypothesize that nanostructured lipid carriers (NLC) could activate the endogenous glucagon-like peptide-1 (GLP-1) secretion and also act as oral delivery systems for GLP-1 analogs (Exenatide and Liraglutide). NLC effectively encapsulated the peptides, majority of which was only released in the intestinal condition. NLC, with and without peptide encapsulation, showed effective induction of GLP-1 secretion in vitro from the enteroendocrinal L-cells (GLUTag). NLC also showed 2.9-fold increase in the permeability of Exenatide across the intestinal cell monolayer. The intestinal administration of the Exenatide and Liraglutide loaded NLC did not demonstrate any glucose lowering effect on normal mice. Further, ex vivo studies depicted that the NLC mainly adhered to the mucus layer. In conclusion, this study demonstrates that NLC needs further optimization to overcome mucosal barrier in the intestine; nonetheless, this study also presents a promising strategy to use a dual-action drug delivery nanosystem which synergizes its own biological effect and that of the encapsulated drug molecule.

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Publication details

The article was received on 17 Oct 2017, accepted on 28 Nov 2017 and first published on 28 Nov 2017

Article type: Paper
DOI: 10.1039/C7NR07736J
Citation: Nanoscale, 2017, Accepted Manuscript
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    Stimulation of GLP-1 secretion and delivery of GLP-1 agonists via nanostructured lipid carriers

    N. Shrestha, O. Bouttefeux, K. Vanvarenberg, P. Lundquist, J. Cunarro, S. Tovar, G. Khodus, E. Andersson, Å. V. Keita, C. Gonzalez Dieguez, P. Artursson, V. Préat and A. Beloqui, Nanoscale, 2017, Accepted Manuscript , DOI: 10.1039/C7NR07736J

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