ArticleAntimicrobial agents and chemotherapy2014
Biopharmaceutical characterization of nebulized antimicrobial agents in rats: 2. Colistin.
Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 62 citations in OpenAlex.
- Physiologically Based Pharmacokinetic Modeling of Inhaled Polymyxin B: From Rabbit Optimization to Human Predictions.Pharmaceutical research · 2026Article
- A Comparative Pharmacokinetics Study of Orally and Intranasally Administered 8-Nitro-1,3-benzothiazin-4-one (BTZ043) Amorphous Drug Nanoparticles.ACS pharmacology & translational science · 2024Article
- Biopharmaceutical profiling of anti-infective sanggenons fromInternational journal of pharmaceutics: X · 2024Article
- No Emergence of Colistin Resistance in the Respiratory Tract of Lung Transplant Patients Treated With Inhaled Colistin.Transplant international : official journal of the European Society for Organ Transplantation · 2024Observational
- Pharmacokinetic Considerations for Optimizing Inhaled Spray-Dried Pyrazinoic Acid Formulations.Molecular pharmaceutics · 2023Article
- Antiviral efficacy of favipiravir against Zika and SARS-CoV-2 viruses in non-human primates.Nature communications · 2022Article
- Aerosolized antibiotics in the treatment of hospital-acquired pneumonia/ventilator-associated pneumonia.The Korean journal of internal medicine · 2022Review
- Can Drug Repurposing be Effective Against Carbapenem-Resistant Acinetobacter baumannii?Current microbiology · 2021Review
- Optimal control for colistin dosage selection.Journal of pharmacokinetics and pharmacodynamics · 2021Article
- Nebulized Colistin in Ventilator-Associated Pneumonia and Tracheobronchitis: Historical Background, Pharmacokinetics and Perspectives.Microorganisms · 2021Review
- Treatment of infections caused by Gram-negative pathogens: current status on the pharmacokinetics/pharmacodynamics of parenteral and inhaled polymyxins in patients.International journal of antimicrobial agents · 2020Review
- Comparison between Colistin Sulfate Dry Powder and Solution for Pulmonary Delivery.Pharmaceutics · 2020Article
- Control of the Lung Residence Time of Highly Permeable Molecules after Nebulization: Example of the Fluoroquinolones.Pharmaceutics · 2020Review
- Effective pharmacotherapy for lung abscess in a patient with alcoholism.Respiratory medicine case reports · 2020Article
- Preclinical Pharmacokinetic and Pharmacodynamic Data To Support Cefoxitin Nebulization for the Treatment of Mycobacterium abscessus.Antimicrobial agents and chemotherapy · 2019Article
- Pulmonary Pharmacokinetics of Oseltamivir Carboxylate in Rats after Nebulization or Intravenous Administration of Its Prodrug, Oseltamivir Phosphate.Antimicrobial agents and chemotherapy · 2019Article
- Effects of the antibiotic component on in-vitro bacterial killing, physico-chemical properties, aerosolization and dissolution of a ternary-combinational inhalation powder formulation of antibiotics for pan-drug resistant Gram-negative lung infections.International journal of pharmaceutics · 2019Article
- A Breath of Fresh Air in the Fog of Antimicrobial Resistance: Inhaled Polymyxins for Gram-Negative Pneumonia.Antibiotics (Basel, Switzerland) · 2019Review
- Biopharmaceutical Characterization of Nebulized Antimicrobial Agents in Rats: 6. Aminoglycosides.Antimicrobial agents and chemotherapy · 2018Article
- Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling of Aerosolized Colistin in a Mouse Lung Infection Model.Antimicrobial agents and chemotherapy · 2018Article
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The purpose of this study was to investigate the pharmacokinetic properties of colistin following intrapulmonary administration of colistin sulfate in rats. Colistin was infused or delivered in nebulized form at a dose of 0.35 mg/kg of body weight in rats, and plasma drug concentrations were measured for 4 h after administration. Bronchoalveolar lavages (BAL) were also conducted at 0.5, 2, and 4 h after intravenous (i.v.) administration and administration via nebulized drug to estimate epithelial lining fluid (ELF) drug concentrations. Unbound colistin plasma concentrations at distribution equilibrium (2 h postdosing) were almost identical after i.v. infusion and nebulized drug inhalation. ELF drug concentrations were undetectable in BAL samples after i.v. administration, but they were about 1,800 times higher than unbound plasma drug levels at 2 h and 4 h after administration of the nebulized drug. Simultaneous pharmacokinetic modeling of plasma and ELF drug concentrations was performed with a model characterized by a fixed physiological volume of ELF (VELF), a passive diffusion clearance (QELF) between plasma and ELF, and a nonlinear influx transfer from ELF to the central compartment, which was assessed by reducing the nebulized dose of colistin by 10-fold (0.035 mg kg(-1)). The km was estimated to be 133 μg ml(-1), and the Vmax, in-to-Km ratio was equal to 2.5 × 10(-3) liter h(-1) kg(-1), which was 37 times higher than the QELF (6.7 × 10(-5) liter h(-1) kg(-1)). This study showed that with the higher ELF drug concentrations after administration via nebulized aerosol than after intravenous administration, for antibiotics with low permeability such as colistin, nebulization offers a real potential over intravenous administration for the treatment of pulmonary infections.
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