Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability - Archive ouverte HAL Access content directly
Journal Articles Molecules Year : 2022

Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability

(1) , (2) , (2) , (1) , (1) , (1) , (1) , (3)
1
2
3

Abstract

Baricitinib (BTB) is an orally administered Janus kinase inhibitor, therapeutically used for the treatment of rheumatoid arthritis. Recently it has also been approved for the treatment of COVID-19 infection. In this study, four different BTB-loaded lipids (stearin)-polymer (Poly(d,l-lactide-co-glycolide)) hybrid nanoparticles (B-PLN1 to B-PLN4) were prepared by the single-step nanoprecipitation method. Next, they were characterised in terms of physicochemical properties such as particle size, zeta potential (ζP), polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL). Based on preliminary evaluation, the B-PLN4 was regarded as the optimised formulation with particle size (272 ± 7.6 nm), PDI (0.225), ζP (−36.5 ± 3.1 mV), %EE (71.6 ± 1.5%) and %DL (2.87 ± 0.42%). This formulation (B-PLN4) was further assessed concerning morphology, in vitro release, and in vivo pharmacokinetic studies in rats. The in vitro release profile exhibited a sustained release pattern well-fitted by the Korsmeyer–Peppas kinetic model (R2 = 0.879). The in vivo pharmacokinetic data showed an enhancement (2.92 times more) in bioavailability in comparison to the normal suspension of pure BTB. These data concluded that the formulated lipid-polymer hybrid nanoparticles could be a promising drug delivery option to enhance the bioavailability of BTB. Overall, this study provides a scientific basis for future studies on the entrapment efficiency of lipid-polymer hybrid systems as promising carriers for overcoming pharmacokinetic limitations.
Fichier principal
Vignette du fichier
molecules-27-00168-v2.pdf (3.21 Mo) Télécharger le fichier
Origin : Publisher files allowed on an open archive

Dates and versions

hal-03518575 , version 1 (10-01-2022)

Identifiers

Cite

Md. Khalid Anwer, Essam A Ali, Muzaffar Iqbal, Mohammed Muqtader Ahmed, Mohammed F Aldawsari, et al.. Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability. Molecules, 2022, 27 (1), pp.168. ⟨10.3390/molecules27010168⟩. ⟨hal-03518575⟩
81 View
44 Download

Altmetric

Share

Gmail Facebook Twitter LinkedIn More