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article · Saudi Pharmaceutical Journal

Eco-friendly synthesis of functionalized chitosan-based nanoantibiotic system for potential delivery of linezolid as antimicrobial agents

202031 citationsOpen accessKafr el-Sheikh University

In plain language

Functionalised chitosan nanoparticles have been synthesised using an eco-friendly microwave process without harsh conditions to deliver the antibiotic linezolid. The drug was successfully integrated into both the internal and external surfaces of chitosan modified with 3, 5-dinitrosalicylic acid, forming an aggregated nanostructure with an average diameter of approximately 150 nanometres. The resulting formulation achieved a drug release efficiency of 98.4 per cent within 100 minutes. When tested against diverse microbial targets, the combined nanoantibiotic produced substantially wider zones of inhibition than linezolid alone against methicillin-resistant Staphylococcus aureus, other bacteria, and fungi. This includes effectiveness against strains resistant to standard linezolid. Direct cell culture on the material surface showed cell viability across three days, while the mechanism of action linked antimicrobial inhibition to electrostatic charges and the generation of oxygen species.

Key takeaways

  • Linezolid was loaded onto functionalised chitosan nanoparticles averaging 150 nanometres in diameter using mild microwave synthesis.
  • The nanoantibiotic formulation attained a linezolid release efficiency of 98.4 per cent within 100 minutes.
  • The formulation demonstrated greater antimicrobial activity than linezolid alone against fungal species and multi-resistant bacteria, including resistant methicillin-resistant Staphylococcus aureus.
  • Cell viability was maintained after three days of direct cell culture on the nanoantibiotic surface.

Why it matters

Bacterial resistance to critical antibiotics poses a growing threat to public health. Pairing existing antimicrobial drugs like linezolid with biocompatible nanomaterials can overcome bacterial resistance mechanisms, including drug efflux. By boosting antimicrobial potency and restoring efficacy against resistant strains such as methicillin-resistant Staphylococcus aureus, such nanoantibiotic platforms offer viable strategies to prolong the clinical utility of established antibiotics against stubborn multi-drug-resistant infections.

Commercialisation angle

The research presents an early-stage drug delivery platform suitable for pharmaceutical developers working on antimicrobial formulations. The nanoantibiotic system could potentially support therapies targeting difficult-to-treat, drug-resistant bacterial and fungal infections. However, the study remains at the stage of laboratory synthesis, microbial zone inhibition assays, and preliminary in vitro cell viability testing, indicating that extensive preclinical validation, safety testing, and formal clinical evaluation will be needed before any commercial adoption.

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Abstract

To obtain a healthy human being with beneficial microflora against different pathogenic infections, classical antibiotics with nanosized biomaterials were used to inhibit the growth of bacterium by their potent synergistic effect. Hence, this study planned to load an oxazolidinone antibiotic named linezolid (LD) onto functionalized chitosan (CN) with 3, 5- dinitrosalyslic acid (DA) via microwave synthesis without harsh condition. The exploring synergistic effect of linezolid (LD) with CN/DA controllable nanostructure was compact efflux-mediated methicillin-resistant <i>Staphylococcus aureus</i> (MRSA) burden and other selected bactericide Gram-positive (<i>(S. aureus),</i> Gram-negative (<i>E. coli</i>), <i>Fungi (C. albicans), Yeast (A. niger),</i> and <i>E. faecalis</i>. The obtained results showed that LD was incorporated into both the internal and external surface of the aggregated CN/DA nanosystem with an average diameter of 150 nm ± 4 hints of the drug loading. Owing to the nature of functionalized CN, the release efficiency attains 98.4% within 100 min. The designed LD@CN/DA exhibited inhibition zone 54 mm, 59 mm, 69 mm, 54 mm, 57 mm, and 24 mm against the tested microbes respectively rather than individual LD. The major target of the current research is achieved by using LD@CN/DA as a nanoantibiotic system that has exceptional consistently active against multi-resistant pathogens, in between MRSA which resist LD. Also, cell viability was performed even after three days of direct cell culture on the surface of the designed nanoantibiotic. The mechanism of microbial inhibition was correlated and rationalized to different charges and the presence of oxygen species against microbial infections. Our findings provide a deep explanation about nanostructured antibiotics design with enhanced potentially pathogen-specific activity.

Research topics

  • Advanced Drug Delivery Systems
  • Ionic liquids properties and applications
  • Chemical and Physical Properties in Aqueous Solutions

Sustainable Development Goals

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DOI: 10.1016/j.jsps.2020.06.005

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