Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability
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(<span style="...
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MDPI AG
2021-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/1/168 |
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| author | Md. Khalid Anwer Essam A. Ali Muzaffar Iqbal Mohammed Muqtader Ahmed Mohammed F. Aldawsari Ahmed Al Saqr Mohd Nazam Ansari M. Ali Aboudzadeh |
| author_facet | Md. Khalid Anwer Essam A. Ali Muzaffar Iqbal Mohammed Muqtader Ahmed Mohammed F. Aldawsari Ahmed Al Saqr Mohd Nazam Ansari M. Ali Aboudzadeh |
| author_sort | Md. Khalid Anwer |
| collection | DOAJ |
| description | 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(<span style="font-variant: small-caps;">d</span>,<span style="font-variant: small-caps;">l</span>-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 (R<sup>2</sup> = 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. |
| first_indexed | 2024-03-10T03:30:48Z |
| format | Article |
| id | doaj.art-5e777d33d3a4439baef3ccf9f0e6d314 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T03:30:48Z |
| publishDate | 2021-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-5e777d33d3a4439baef3ccf9f0e6d3142023-11-23T11:57:41ZengMDPI AGMolecules1420-30492021-12-0127116810.3390/molecules27010168Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral BioavailabilityMd. Khalid Anwer0Essam A. Ali1Muzaffar Iqbal2Mohammed Muqtader Ahmed3Mohammed F. Aldawsari4Ahmed Al Saqr5Mohd Nazam Ansari6M. Ali Aboudzadeh7Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmacology and Toxicology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaCNRS, Institut des Sciences Analytiques et de Physico-Chimie pour l’Environnement et les Matériaux, University Pau & Pays Adour, E2S UPPA, IPREM, UMR5254, 64000 Pau, FranceBaricitinib (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(<span style="font-variant: small-caps;">d</span>,<span style="font-variant: small-caps;">l</span>-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 (R<sup>2</sup> = 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.https://www.mdpi.com/1420-3049/27/1/168baricitinibbioavailabilityencapsulationhybrid nanoparticlespoly(<span style="font-variant: small-caps">d</span>,<span style="font-variant: small-caps">l</span>-lactide-coglycolide)stearin |
| spellingShingle | Md. Khalid Anwer Essam A. Ali Muzaffar Iqbal Mohammed Muqtader Ahmed Mohammed F. Aldawsari Ahmed Al Saqr Mohd Nazam Ansari M. Ali Aboudzadeh Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability Molecules baricitinib bioavailability encapsulation hybrid nanoparticles poly(<span style="font-variant: small-caps">d</span>,<span style="font-variant: small-caps">l</span>-lactide-coglycolide) stearin |
| title | Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability |
| title_full | Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability |
| title_fullStr | Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability |
| title_full_unstemmed | Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability |
| title_short | Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability |
| title_sort | development of sustained release baricitinib loaded lipid polymer hybrid nanoparticles with improved oral bioavailability |
| topic | baricitinib bioavailability encapsulation hybrid nanoparticles poly(<span style="font-variant: small-caps">d</span>,<span style="font-variant: small-caps">l</span>-lactide-coglycolide) stearin |
| url | https://www.mdpi.com/1420-3049/27/1/168 |
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