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Oral bioavailability enhancement of agomelatine by loading into nanostructured lipid carriers: Peyer’s patch targeting approach

Authors Prajapati JB, Verma SD, Patel AA

Received 14 October 2016

Accepted for publication 21 November 2016

Published 15 March 2018 Volume 2018:13(T-NANO 2014 Abstracts) Pages 35—38

DOI https://doi.org/10.2147/IJN.S124703

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Lei Yang


Jagruti B Prajapati, Sneha D Verma, Amit A Patel

Department of Ppharmaceutics and Ppharmaceutical Technology, Rramanbhai Patel College of Ppharmacy, Charotar University of Science and Technology, Changa, Gujarat, India


Abstract: Agomelatine (AGM) is a new antidepressant drug with a novel mechanism of action and fewer side effects compared with older antidepressants. AGM is a melatonin receptor (MT1 and MT2) agonist and 5-hydroxytryptamine receptor (5-HT2C) antagonist. In the present study, the enhancement of the oral bioavailability of AGM was formulated and loaded into nanostructured lipid carriers (NLCs), using ultrasonication method. In vitro and ex vivo drug release was performed using a dialysis bag and rat duodenum, respectively. Our pharmacodynamic study showed that AGM–NLCs are more efficacious than a pure drug and marketed product, and confocal microscopy revealed lymphatic uptake of AGM–NLCs. The present study concluded that the NLCs enhanced the oral bioavailability of AGM (6.5-fold) by avoiding its first-pass metabolism by way of lymphatic uptake.

Keywords: agomelatine, nanostructured lipid carriers, antidepressant drug

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