Liposomal nanoparticles control the uptake of ciprofloxacin across respiratory epithelia

Pharm Res. 2012 Dec;29(12):3335-46. doi: 10.1007/s11095-012-0827-0. Epub 2012 Jul 26.

Abstract

Purpose: Liposomal ciprofloxacin nanoparticles were developed to overcome the rapid clearance of antibiotics from the lungs. The formulation was evaluated for its release profile using an air interface Calu-3 cell model and further characterised for aerosol performance and antimicrobial activity.

Methods: Liposomal and free ciprofloxacin formulations were nebulised directly onto Calu-3 bronchial epithelial cells placed in an in vitro twin-stage impinger (TSI) to assess the kinetics of release. The aerosol performance of both the liposomal and free ciprofloxacin formulation was characterised using the next generation impactor. Minimum inhibitory and bactericidal concentrations (MICs and MBCs) were determined and compared between formulations to evaluate the antibacterial activity.

Results: The liposomal formulation successfully controlled the release of ciprofloxacin in the cell model and showed enhanced antibacterial activity against Pseudomonas aeruginosa. In addition, the formulation displayed a respirable aerosol fraction of 70.5 ± 2.03% of the emitted dose.

Conclusion: Results indicate that the in vitro TSI air interface Calu-3 model is capable of evaluating the fate of nebulised liposomal nanoparticle formulations and support the potential for inhaled liposomal ciprofloxacin to provide a promising treatment for respiratory infections.

MeSH terms

  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / pharmacokinetics*
  • Anti-Bacterial Agents / pharmacology
  • Cell Line
  • Ciprofloxacin / administration & dosage*
  • Ciprofloxacin / pharmacokinetics*
  • Ciprofloxacin / pharmacology
  • Humans
  • Liposomes / chemistry
  • Microbial Sensitivity Tests
  • Nanoparticles / chemistry
  • Pseudomonas Infections / drug therapy
  • Pseudomonas aeruginosa / drug effects
  • Respiratory Mucosa / metabolism*

Substances

  • Anti-Bacterial Agents
  • Liposomes
  • Ciprofloxacin