Encapsulation of the Anti-inflammatory Dual FLAP/sEH Inhibitor Diflapolin Improves the Efficiency in Human Whole Blood
Grune C, Kretzer C, Zergiebel S, Kattner S, Thamm J, Hoeppener S, Werz O, Fischer D (2022)
Publication Type: Journal article
Publication year: 2022
Journal
Book Volume: 111
Pages Range: 1843-1850
Journal Issue: 6
DOI: 10.1016/j.xphs.2021.10.030
Abstract
Diflapolin is a dual FLAP/sEH inhibitor with potent anti-inflammatory efficiency in cellular assays and experimental in vivo studies. Despite these outstanding characteristics, its high lipophilicity and plasma protein binding hamper the bioactivity in blood. To overcome these limitations, diflapolin was encapsulated in poly (lactic-co-glycolic acid) nanoparticles to develop an efficient and biocompatible drug delivery system. Two different cosolvent approaches were tested showing the possibility to exchange dimethyl sulfoxide in the organic phase by the sustainable 400 g/mol poly(ethylene glycol). A particle size of 220 nm and the amorphous encapsulation of diflapolin in high amounts rendered the nanoparticles appropriate for the intended application. Excellent biocompatibility of the nanoparticles was demonstrated in an ex ovo hen's egg model. The potent suppression of FLAP-dependent 5-lipoxygenase product formation by the nanoparticles in human whole blood, superior to the free drug, makes them to a promising drug delivery system to improve the bioactivity of diflapolin.(c) 2021 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.
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Germany (DE)How to cite
APA:
Grune, C., Kretzer, C., Zergiebel, S., Kattner, S., Thamm, J., Hoeppener, S.,... Fischer, D. (2022). Encapsulation of the Anti-inflammatory Dual FLAP/sEH Inhibitor Diflapolin Improves the Efficiency in Human Whole Blood. Journal of Pharmaceutical Sciences, 111(6), 1843-1850. https://doi.org/10.1016/j.xphs.2021.10.030
MLA:
Grune, Christian, et al. "Encapsulation of the Anti-inflammatory Dual FLAP/sEH Inhibitor Diflapolin Improves the Efficiency in Human Whole Blood." Journal of Pharmaceutical Sciences 111.6 (2022): 1843-1850.
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