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In vivo evaluation of an oral self-emulsifying drug delivery system (SEDDS) for exenatide

Menzel, Claudia, Holzeisen, Thomas, Laffleur, Flavia, Zaichik, Sergey, Abdulkarim, Muthanna, Gumbleton, Mark ORCID: and Bernkop-Schnürch, Andreas 2018. In vivo evaluation of an oral self-emulsifying drug delivery system (SEDDS) for exenatide. Journal of Controlled Release 277 , pp. 165-172. 10.1016/j.jconrel.2018.03.018

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Background The aim of the study was to develop an oral self-emulsifying drug delivery system (SEDDS) for exenatide and to evaluate its in vivo efficacy. Methods Exenatide was lipidised via hydrophobic ion pairing with sodium docusate (DOC) and incorporated in SEDDS consisting of 35% Cremophor EL, 25% Labrafil 1944, 30% Capmul-PG 8 and 10% propylene glycol. Exenatide/DOC was characterized in terms of lipophilicity evaluating the octanol/water phase distribution (logP). Exenatide/DOC SEDDS were characterized via droplet size analysis, drug release characteristics (log DSEDDS/release medium determination) and mucus permeation studies. Furthermore, the impact of orally administered exenatide/DOC SEDDS on blood glucose level was investigated in vivo on healthy male Sprague-Dawley rats. Results Hydrophobic ion pairing in a molar ratio of 1:4 (exenatide:DOC) increased the effective logP of exenatide from −1.1 to 2.1. SEDDS with a payload of 1% exenatide/DOC had a mean droplet size of 45.87 ± 2.9 nm and a Log DSEDDS/release medium of 1.9 ± 0.05. Permeation experiments revealed 2.7-fold improved mucus diffusion for exenatide/DOC SEDDS compared to exenatide in solution. Orally administered exenatide/DOC SEDDS showed a relative bioavailability (versus s.c.) of 14.62% ± 3.07% and caused a significant (p < .05) 20.6% decrease in AUC values of blood glucose levels. Conclusion According to these results, hydrophobic ion pairing in combination with SEDDS represents a promising tool for oral peptide delivery.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Additional Information: Released with a Creative Commons Attribution Non-Commercial No Derivatives License (CC BY-NC-ND)
Publisher: Elsevier
ISSN: 0168-3659
Date of First Compliant Deposit: 29 March 2018
Date of Acceptance: 18 March 2018
Last Modified: 07 Nov 2023 18:03

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