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PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery

Raza, Hina; Ilahi, Yusra; Rashid, Zermina; Nazir, Shabnam; Manzoor, Suryyia; Yousif, Mohamed Deifallah; (2022) PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery. Materials Research Express 10.1088/2053-1591/ac9d26. (In press). Green open access

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Abstract

Ceftriaxone is a third-generation cephalosporin antibiotic effective against many bacterial infections. However, owing to its instability in the gastrointestinal tract (GIT), it is administered by injections, which is an unfavourable route of administration. Therefore, the aim of this study was to formulate ceftriaxone into biodegradable and thermally stable polymeric blend microparticles that are suitable for oral delivery. The drug-loaded microparticles were prepared by the water-in-oil (W/O) emulsion method and consisted of starch and sodium alginate (NaAlg) as a polymeric matrix and glutaraldehyde (GA) as a cross-linking agent. Characterization of these particles using scanning electron microscopy (SEM) showed that the particles were spherical in shape with a smooth surface. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) of these particles showed no drug-polymer interactions. The highest percentage yield of particles was obtained at 3% polymer concentration. The particle size increased slightly after drug loading. The drug loading and entrapment efficiency appeared to increase with increasing polymer concentration. In vitro drug release at pH 1.2 and pH 7.4, revealed that drug release was below 20% at the acidic pH, while at pH 7.4, drug release of up to 85% was observed. The release mechanism followed first-order and Fickian diffusion patterns. Plasma concentration-time profiles were simulated for subcontinental Asian populations using commercial PBPK software, and the results suggest that microencapsulation of ceftriaxone sodium in a polymeric blend could represent a promising approach for controlled oral delivery of the drug, with enhanced absorption and bioavailability of the drug.

Type: Article
Title: PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery
Open access status: An open access version is available from UCL Discovery
DOI: 10.1088/2053-1591/ac9d26
Publisher version: https://doi.org/10.1088/2053-1591%2Fac9d26
Language: English
Additional information: As the Version of Record of this article is going to be/has been published on a gold open access basis under a CC BY 3.0 licence, this Accepted Manuscript is available for reuse under a CC BY 3.0 licence immediately. Although reasonable endeavours have been taken to obtain all necessary permissions from third parties to include their copyrighted content within this article, their full citation and copyright line may not be present in this Accepted Manuscript version. Before using any content from this article, please refer to the Version of Record on IOPscience once published for full citation and copyright details, as permission may be required. All third party content is fully copyright protected, and is not published on a gold open access basis under a CC BY licence, unless that is specifically stated in the figure caption in the Version of Record.
UCL classification: UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
URI: https://discovery.ucl.ac.uk/id/eprint/10158270
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