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Verfasst von:Heshmati, Nasim [VerfasserIn]   i
 Cheng, Xinlai [VerfasserIn]   i
 Eisenbrand, Gerhard [VerfasserIn]   i
 Fricker, Gert [VerfasserIn]   i
Titel:Enhancement of oral bioavailability of E804 by self-nanoemulsifying drug delivery system (SNEDDS) in rats
Verf.angabe:Nasim Heshmati, Xinlai Cheng, Gerhard Eisenbrand, Gert Fricker
Jahr:2016
Jahr des Originals:2013
Umfang:8 S.
Teil:volume:102
 year:2013
 number:10
 pages:3792-3799
 extent:8
Fussnoten:Gesehen am 29.04.2021 ; Available online 4 January 2016
Titel Quelle:Enthalten in: Journal of pharmaceutical sciences
Ort Quelle:Amsterdam : Elsevier, 1911
Jahr Quelle:2013
Band/Heft Quelle:102(2013), 10, Seite 3792-3799
ISSN Quelle:1520-6017
Abstract:Indirubin and its derivatives have been shown to interrupt the cell cycle by inhibiting cyclin-dependent kinases, explaining their long-time use in traditional Chinese medicine for the treatment of chronic myelocytic leukemia. A potent derivative of indirubin, indirubin-3′-oxime 2,3-dihydroxypropyl ether (E804), has been shown to block the Src-Stat3 and Src-Stat5 signaling pathway in human cancer cells, inducing apoptosis. The anticancer effects of E804, however, cannot be easily examined in vivo because of its poor water solubility and low absorption. The aim of this study was to develop and evaluate a self-nanoemulsifying drug delivery system (SNEDDS) containing E804 for enhancing its solubility and bioavailability. Solubility of E804 was determined in various vehicles, and pseudoternary phase diagram was used to evaluate the self-emulsifying existence area. The SNEDDS composed of Capmul MCM (oil), Solutol HS 15 (surfactant), and polyethylene glycol 400 (cosurfactant) on the ratio of 20.5:62.5:16 loaded 1.5% of E804. The particle size of droplets was found to be 16.8 and 140 nm, and SNEDDS was stable after freeze-thaw cycles and upon dilution in HCl 0.1 N and pH 7.4 HBSS++. The ability of formulation for absorption enhancement was studied in rats in vivo after oral administration. The results showed that the developed SNEDDS increased the E804 bioavailability 984.23% compared with the aqueous suspension. Our studies for the first time show that the developed SNEDDS can be used as a possible formulation for E804 to improve its solubility and oral bioavailability. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:3792-3799, 2013
DOI:doi:10.1002/jps.23696
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

Volltext ; Verlag: https://doi.org/10.1002/jps.23696
 Volltext: https://www.sciencedirect.com/science/article/pii/S002235491530900X
 DOI: https://doi.org/10.1002/jps.23696
Datenträger:Online-Ressource
Sprache:eng
Sach-SW:bioavailability
 drug delivery
 E804
 excipients
 formulation
 indirubin
 self-nanoemulsifying drug delivery system (SNEDDS)
 solubility
K10plus-PPN:175660925X
Verknüpfungen:→ Zeitschrift

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