Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments

Amir Maghrabia,1 Mariza Boughdady,2 Mahasen Meshali2 1Department of Pharmacy, Urology and Nephrology Center, Mansoura University, Mansoura, 35516, Egypt; 2Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, EgyptCorrespondence: Amir MaghrabiaDepartment of Pharmacy...

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Autores principales:	Maghrabia A, Boughdady M, Meshali M
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	ceftriaxone chitosan shellac nanoparticles oral factorial design Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/c3c682a4ac164e73bad20284c0e0a6ff
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spelling	oai:doaj.org-article:c3c682a4ac164e73bad20284c0e0a6ff2021-12-02T16:39:24ZDesign and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments1178-2013https://doaj.org/article/c3c682a4ac164e73bad20284c0e0a6ff2021-08-01T00:00:00Zhttps://www.dovepress.com/design-and-optimization-of-new-enteric-nanoparticles-of-ceftriaxone-fo-peer-reviewed-fulltext-article-IJNhttps://doaj.org/toc/1178-2013Amir Maghrabia,1 Mariza Boughdady,2 Mahasen Meshali2 1Department of Pharmacy, Urology and Nephrology Center, Mansoura University, Mansoura, 35516, Egypt; 2Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, EgyptCorrespondence: Amir MaghrabiaDepartment of Pharmacy, Urology and Nephrology Center, Mansoura University, Mansoura, 35516, EgyptTel +201007285809Fax +20502247496Email amir2007_pharm@yahoo.comPurpose: Development of new strategies for oral delivery of existing antibiotics administered exclusively through intravenous route is one of the global priorities of pharmaceutical research. The encapsulation of these active pharmaceutical agents within nanosized natural products offers several traits due to their tunable surface properties. Ceftriaxone (CTX) is an injectable, third-generation cephalosporin that suffers poor oral bioavailability.Methods: In the present study, ionic gelation of two biopolymers, namely chitosan (CH) and shellac (SH), was implemented to consolidate CTX, within elegant nanoparticles (NPs) for oral administration that would increase its bioavailability and sustainability. Quality by design approach (23 full factorial design) was adopted to optimize CTX-loaded nanoparticles. The optimized formula (F2) was characterized through transmission electron microscopy (TEM), Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC). In vitro release behavior and stability study were also evaluated. Pharmacokinetic studies of enteric-coated hard gelatin capsules (HGCs) loaded with F2-NPs were finally assessed.Results: The optimized spherical F2-NPs had a mean particle size of 258 nm, zeta potential of about +30.1 and appreciable drug entrapment efficiency of 83%. The in vitro drug release profile of F2-NPs in pH 7.4 experienced biphasic configuration with an initial burst release for an hour, followed by a sustained release over 15 h with Higuchi model and non-Fickian diffusion mechanism (R2=0.9852). High stability upon storage at refrigerated and room temperature for 3 months and good flow properties (θ= 32.2 and HR= 1.13) of the optimized formula were also conferred. In vivo pharmacokinetic assessment in rabbits fruitfully displayed 92% absolute bioavailability of CTX.Conclusion: The obtained results provide evidence for the potential combination of CH and SH in NPs preparation to enhance the oral bioavailability of CTX.Keywords: ceftriaxone, chitosan, shellac, nanoparticles, oral, factorial designMaghrabia ABoughdady MMeshali MDove Medical Pressarticleceftriaxonechitosanshellacnanoparticlesoralfactorial designMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 5937-5953 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	ceftriaxone chitosan shellac nanoparticles oral factorial design Medicine (General) R5-920
spellingShingle	ceftriaxone chitosan shellac nanoparticles oral factorial design Medicine (General) R5-920 Maghrabia A Boughdady M Meshali M Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments
description	Amir Maghrabia,1 Mariza Boughdady,2 Mahasen Meshali2 1Department of Pharmacy, Urology and Nephrology Center, Mansoura University, Mansoura, 35516, Egypt; 2Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, EgyptCorrespondence: Amir MaghrabiaDepartment of Pharmacy, Urology and Nephrology Center, Mansoura University, Mansoura, 35516, EgyptTel +201007285809Fax +20502247496Email amir2007_pharm@yahoo.comPurpose: Development of new strategies for oral delivery of existing antibiotics administered exclusively through intravenous route is one of the global priorities of pharmaceutical research. The encapsulation of these active pharmaceutical agents within nanosized natural products offers several traits due to their tunable surface properties. Ceftriaxone (CTX) is an injectable, third-generation cephalosporin that suffers poor oral bioavailability.Methods: In the present study, ionic gelation of two biopolymers, namely chitosan (CH) and shellac (SH), was implemented to consolidate CTX, within elegant nanoparticles (NPs) for oral administration that would increase its bioavailability and sustainability. Quality by design approach (23 full factorial design) was adopted to optimize CTX-loaded nanoparticles. The optimized formula (F2) was characterized through transmission electron microscopy (TEM), Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC). In vitro release behavior and stability study were also evaluated. Pharmacokinetic studies of enteric-coated hard gelatin capsules (HGCs) loaded with F2-NPs were finally assessed.Results: The optimized spherical F2-NPs had a mean particle size of 258 nm, zeta potential of about +30.1 and appreciable drug entrapment efficiency of 83%. The in vitro drug release profile of F2-NPs in pH 7.4 experienced biphasic configuration with an initial burst release for an hour, followed by a sustained release over 15 h with Higuchi model and non-Fickian diffusion mechanism (R2=0.9852). High stability upon storage at refrigerated and room temperature for 3 months and good flow properties (θ= 32.2 and HR= 1.13) of the optimized formula were also conferred. In vivo pharmacokinetic assessment in rabbits fruitfully displayed 92% absolute bioavailability of CTX.Conclusion: The obtained results provide evidence for the potential combination of CH and SH in NPs preparation to enhance the oral bioavailability of CTX.Keywords: ceftriaxone, chitosan, shellac, nanoparticles, oral, factorial design
format	article
author	Maghrabia A Boughdady M Meshali M
author_facet	Maghrabia A Boughdady M Meshali M
author_sort	Maghrabia A
title	Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments
title_short	Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments
title_full	Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments
title_fullStr	Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments
title_full_unstemmed	Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments
title_sort	design and optimization of new enteric nanoparticles of ceftriaxone for oral delivery: in vitro and in vivo assessments
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/c3c682a4ac164e73bad20284c0e0a6ff
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Design and Optimization of New Enteric Nanoparticles of Ceftriaxone for Oral Delivery: In vitro and in vivo Assessments

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