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

Development of new approaches for oral delivery of an existing antiviral drug aimed to enhance its permeability and hence bioavailability. Ganciclovir (GC) is an antiviral drug that belongs to class III in biopharmaceutical classification. The encapsulation of poorly absorbed drugs within nanosized particles offers several characteristics to drug due to their acquired surface properties. In the following study, the solvent evaporation technique was used to incorporate GC, within elegant nanosize particles using cyclodextrin and shellac polymers for enhancing its permeability and release pattern. Formulation variables were optimized using 2 3 full factorial design. The prepared formulations were assessed for yield, particle size, content, and micromeritics behavior. The optimized formula (F6) was identified through differential scanning calorimetry and Fourier transform infrared. In vitro release and stability were also assessed. Pharmacokinetic parameters of optimized nano GC solid dispersion particles (NGCSD-F6) were finally evaluated. The optimized formula (F6) showed a mean particle size of 288.5 ± 20.7 nm, a zeta potential of about 23.87 ± 2.27, and drug content 95.77 ± 2.1%. The in vitro drug release pattern of F6 showed an initial burst release followed by a sustained release over the next 12 h. The optimized formula showed accepted stability upon storage at room and refrigerator temperatures for 6 months with good flowing properties (Carr’s index = 18.28 ± 0.44). In vivo pharmacokinetic study in rabbits revealed 2.2 fold increases in the bioavailability of GC compared with commercial convention tablets. The study affords evidence for the success of the solid dispersion technique under specified conditions in improvement of bioavailability of GC.

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“…Previous study by Maghrabia et al. showed relevant results for ceftriaxone (Maghrabia et al., 2021 ).…”

Section: Resultsmentioning

confidence: 81%

Design and optimization of ganciclovir solid dispersion for improving its bioavailability

Gaber¹,

Alnwiser²,

Alotaibi³

et al. 2022

Drug Delivery

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“…However, treatment with cephalosporins was not investigated in the POET trial, and bioavailability of these antibiotic drugs is unfortunately comparatively low [ 39 ]. Nonetheless, novel formulations are being investigated at the moment, which could help to put outpatient treatment with AC in patients with E. faecalis IE into practice in the near future [ 40 , 41 ].…”

Section: Discussionmentioning

confidence: 99%

Time to abandon ampicillin plus gentamicin in favour of ampicillin plus ceftriaxone in Enterococcus faecalis infective endocarditis? A meta-analysis of comparative trials

et al. 2021

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Background Current guidelines recommend either ampicillin plus ceftriaxone (AC) or amoxicillin/ampicillin plus gentamicin (AG) with an equivalent class IB recommendation in Enterococcus faecalis endocarditis. However, previous observational studies suggest that AC might be favourable in terms of adverse events. Objectives To investigate whether AC is non-inferior to AG, and if it is associated with less adverse events. Methods In June 2021, a systematic literature search using the databases PubMed/MEDLINE, CDSR, CENTRAL, CCAs, EBM Reviews, Web of Science and LILACS was conducted by two independent reviewers. Studies were considered eligible if (P) patients included were ≥ 18 years of age and had IE with E. faecalis, (I) treatment with AC was compared to (C) treatment with AG and (O) outcomes on in-hospital mortality, nephrotoxicity and adverse events requiring drug withdrawal were reported. Odds ratios and 95% confidence intervals were calculated using random-effects models with the Mantel–Haenszel method, the Sidik–Jonkman estimator for τ2 and the Hartung–Knapp adjustment. Results Treatment with AC was non-inferior to AG, as depicted by no significant differences in-hospital mortality, 3-month mortality, relapses or treatment failure. Furthermore, AC was associated with a lower prevalence of nephrotoxicity (OR 0.45 [0.26–0.77], p = 0.0182) and drug withdrawal due to adverse events (OR 0.11 [0.03–0.46], p = 0.0160) than AG. Conclusions Treatment with AC was non-inferior to treatment with AG, and it was associated with a reduced prevalence of nephrotoxicity and drug withdrawal due to adverse events. Thus, combination therapy with AC appears favourable over AG in patients with E. faecalis IE. Graphical abstract

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“…Various types of EC-based oral delivery approaches have been implemented for vitamin D 3 (hydroxyapatite) and ceftriaxone (chitosan) . Khanal et al developed an EC bacteriophage tablet for immunocompromised patients (specifically for intensive care units in hospitals).…”

Section: Type Of Tabletized Nanomedicinementioning

confidence: 99%

Tabletized Nanomedicine: From the Current Scenario to Developing Future Medicine

Tiwari,

Kolli,

Chauhan

et al. 2024

ACS Nano

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The limitations of conventional therapeutic treatments prevailed in the development of nanotechnology-based medical formulations, termed nanomedicine. Nanomedicine is an advanced medicine that often consists of therapeutic agent(s) embedded in biodegradable or biocompatible nanomaterial-based formulations. Among nanomedicine approaches, tablet (oral) nanomedicine is still under development. In tabletized nanomedicine, the dynamic interplay between nanoformulations and the intricate milieu of the gastrointestinal tract simulates a pivotal role, particularly accentuating the influence exerted upon the luminal, mucosal, and epithelial cells. In this work, we document the perspectives and opportunities of nanoformulations toward the development of tabletized nanomedicine. This review also unveils the notion of integrating nanomedicine within a tablet formulation, which facilitates the controlled release of drugs, biomolecules, and agent(s) from the formulation to achieve a better therapeutic response. Finally, an attempt was made to explore current trends in nanomedicine technology such as bacteriophage, probiotic, and oligonucleotide tabletized nanomedicine and the combination of nanomedicine with imaging agents, i.e., nanotheranostics.

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

Cited by 8 publications

References 54 publications

Design and optimization of ganciclovir solid dispersion for improving its bioavailability

Design and optimization of ganciclovir solid dispersion for improving its bioavailability

Time to abandon ampicillin plus gentamicin in favour of ampicillin plus ceftriaxone in Enterococcus faecalis infective endocarditis? A meta-analysis of comparative trials

Tabletized Nanomedicine: From the Current Scenario to Developing Future Medicine

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