The influence on the oral bioavailability of solubilized and suspended drug in a lipid nanoparticle formulation: In vitro and in vivo evaluation.

Autor: Elbrink K; University of Antwerp, Department of Pharmaceutical Technology and Biopharmacy, Universiteitsplein 1, 2610 Wilrijk, Belgium. Electronic address: Kimberley.Elbrink@uantwerpen.be., Van Hees S; University of Antwerp, Department of Pharmaceutical Technology and Biopharmacy, Universiteitsplein 1, 2610 Wilrijk, Belgium. Electronic address: Sofie.VanHees@uantwerpen.be., Roelant D; Janssen Pharmaceutica, Discovery Sciences, DMPK, Turnhoutseweg 30, 2340 Beerse, Belgium. Electronic address: DROELANT@its.jnj.com., Loomans T; Janssen Pharmaceutica, Discovery Sciences, DMPK, Turnhoutseweg 30, 2340 Beerse, Belgium. Electronic address: TLOOMANS@its.jnj.com., Holm R; Janssen Pharmaceutica, Drug Product and Development, Parenterals and Liquids, Turnhoutseweg 30, 2340 Beerse, Belgium; University of Southern Denmark, Department of Physics, Chemistry, and Pharmacy, Campusvej 55, 5230 Odense, Denmark. Electronic address: rholm@ITS.JNJ.com., Kiekens F; University of Antwerp, Department of Pharmaceutical Technology and Biopharmacy, Universiteitsplein 1, 2610 Wilrijk, Belgium. Electronic address: Filip.Kiekens@uantwerpen.be.
Jazyk: angličtina
Zdroj: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V [Eur J Pharm Biopharm] 2022 Oct; Vol. 179, pp. 1-10. Date of Electronic Publication: 2022 Aug 27.
DOI: 10.1016/j.ejpb.2022.08.010
Abstrakt: The present study investigated the oral bioavailability of celecoxib when incorporated into solid lipid nanoparticles either dissolved or suspended. In vitro drug release in different media, in vivo performance, and in vitro-in vivo correlation were conducted. The results revealed that the compound was successfully encapsulated into the nanocarriers with good physicochemical properties for oral administration. The in vitro release profiles followed the Weibull model, with significant differences between the formulations containing the solubilized and the suspended compound. Furthermore, in vitro release data could be used to rank the observed in vivo bioavailability. The relative bioavailability of celecoxib from the solid lipid nanoparticles was 2.5- and 1.8-fold higher for the drug solubilized and suspended solid lipid nanoparticle formulation, respectively, when compared to the celecoxib reference. A significant difference was observed between the plasma concentration-time profiles and pharmacokinetic parameters for the three investigated formulations. Finally, this investigation displayed promising outcomes that both solubilized and suspended celecoxib in the lipid core of the solid lipid nanoparticles offers the potential to improve the compound's oral bioavailability and thereby reduce the dosing frequency.
Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2022 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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