Increased intestinal permeation and modulation of presystemic metabolism of resveratrol formulated into self-emulsifying drug delivery systems - CNRS - Centre national de la recherche scientifique Access content directly
Journal Articles International Journal of Pharmaceutics Year : 2017

Increased intestinal permeation and modulation of presystemic metabolism of resveratrol formulated into self-emulsifying drug delivery systems

Abstract

Despite various beneficial biological properties, resveratrol lacks therapeutic applications because of poor bioavailability due to variable absorption and extensive metabolism. The present study aims at evaluating the capability of self-emulsifying drug delivery systems (SEDDS) to enhance resveratrol permeation across rat intestine and to modulate its presystemic metabolism. For that purpose, semi-solid (SS) and liquid (L) SEDDS were prepared and dispersed in an aqueous buffer to produce nanoemulsions (NE). The jejunal absorptive transepithelial fluxes (J(ms)) of resveratrol elicited by these formulations (SSNE and L-NE) and presystemic metabolization were determined on Ussing chambers. The absorptive fluxes through the intestinal epithelium from the nanoemulsions (J(ms) =20.5 +/- 3.1 mu gh (1) cm (2) SS-NE; 28.9 +/- 2.9 mu gh (1) cm (2) L-NE) were significantly increased compared to an ethanolic control solution (J(ms) = 3.4 +/- 0.3 mu gh (1) cm (2), p < 0.05). No significant variations of conductance were observed after two hours of contact between the formulations and the mucosa. Simultaneously, the presystemic metabolization pattern was modified in the case of the nanoemulsions compared to the control solution. In conclusion, our data suggests that oil-in-water nanoemulsions prepared from SEDDS dispersions of medium-chain lipids could be promising formulations for enhancing oral delivery of resveratrol. (C) 2017 Elsevier B.V. All rights reserved.
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Dates and versions

hal-03292705 , version 1 (20-07-2021)

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G. Mamadou, C. Charrueau, J. Dairou, N. Limas Nzouzi, B. Eto, et al.. Increased intestinal permeation and modulation of presystemic metabolism of resveratrol formulated into self-emulsifying drug delivery systems. International Journal of Pharmaceutics, 2017, 521 (1-2), pp.150-155. ⟨10.1016/j.ijpharm.2017.02.036⟩. ⟨hal-03292705⟩
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