PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery
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 f...
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| Format: | Article |
| Language: | English |
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IOP Publishing
2022-01-01
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| Series: | Materials Research Express |
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| Online Access: | https://doi.org/10.1088/2053-1591/ac9d26 |
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| author | Hina Raza Yusra Ilahi Zermina Rashid Shabnam Nazir Suryyia Manzoor Mohamed Deifallah Yousif |
| author_facet | Hina Raza Yusra Ilahi Zermina Rashid Shabnam Nazir Suryyia Manzoor Mohamed Deifallah Yousif |
| author_sort | Hina Raza |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-12T15:34:29Z |
| format | Article |
| id | doaj.art-7e215216c346443ca3f712166ef6e7df |
| institution | Directory Open Access Journal |
| issn | 2053-1591 |
| language | English |
| last_indexed | 2024-03-12T15:34:29Z |
| publishDate | 2022-01-01 |
| publisher | IOP Publishing |
| record_format | Article |
| series | Materials Research Express |
| spelling | doaj.art-7e215216c346443ca3f712166ef6e7df2023-08-09T16:18:25ZengIOP PublishingMaterials Research Express2053-15912022-01-0191111530110.1088/2053-1591/ac9d26PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral deliveryHina Raza0Yusra Ilahi1Zermina Rashid2https://orcid.org/0000-0002-6537-6864Shabnam Nazir3Suryyia Manzoor4Mohamed Deifallah Yousif5https://orcid.org/0000-0003-2180-0480Faculty of Pharmacy, Bahauddin Zakariya University , Multan, PakistanFaculty of Pharmacy, Bahauddin Zakariya University , Multan, PakistanDepartment of Pharmacy, The Women University Multan , Multan, PakistanInstitute of Pharmaceutical Science, King’s College London, London, United KingdomInstitute of Chemical Sciences, Bahauddin Zakariya University , Multan, PakistanUCL School of Pharmacy, University College London , London, United KingdomCeftriaxone 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.https://doi.org/10.1088/2053-1591/ac9d26ceftriaxone sodiumsodium alginatestarchmicroparticlesPBPK modellingoral delivery |
| spellingShingle | Hina Raza Yusra Ilahi Zermina Rashid Shabnam Nazir Suryyia Manzoor Mohamed Deifallah Yousif PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery Materials Research Express ceftriaxone sodium sodium alginate starch microparticles PBPK modelling oral delivery |
| title | PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery |
| title_full | PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery |
| title_fullStr | PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery |
| title_full_unstemmed | PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery |
| title_short | PBPK modelling of ceftriaxone Na-loaded starch-sodium alginate polymeric blend prepared by water-in-oil emulsification for oral delivery |
| title_sort | pbpk modelling of ceftriaxone na loaded starch sodium alginate polymeric blend prepared by water in oil emulsification for oral delivery |
| topic | ceftriaxone sodium sodium alginate starch microparticles PBPK modelling oral delivery |
| url | https://doi.org/10.1088/2053-1591/ac9d26 |
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