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Liposomal Nanoparticles Control the Uptake of Ciprofloxacin Across Respiratory Epithelia

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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.

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Authors and Affiliations

  1. Advanced Drug Delivery Group, Faculty of Pharmacy (A15), The University of Sydney, Sydney, NSW, 2006, Australia

    Hui Xin Ong, Daniela Traini & Paul M Young

  2. Pharmaceutical Sciences, Aradigm Corporation, Hayward, California, USA

    David Cipolla & Igor Gonda

  3. School of Pharmacy, Graduate School of Health, University of Technology Sydney, Broadway, Sydney, NSW, 2007, Australia

    Mary Bebawy

  4. School of Molecular Bioscience, Faculty of Science (G08), University of Sydney, Sydney, NSW, 2006, Australia

    Helen Agus

Authors
  1. Hui Xin Ong
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  2. Daniela Traini
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  3. David Cipolla
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  4. Igor Gonda
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  5. Mary Bebawy
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  6. Helen Agus
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  7. Paul M Young
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Correspondence to Paul M Young.

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Ong, H.X., Traini, D., Cipolla, D. et al. Liposomal Nanoparticles Control the Uptake of Ciprofloxacin Across Respiratory Epithelia. Pharm Res 29, 3335–3346 (2012). https://doi.org/10.1007/s11095-012-0827-0

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  • DOI: https://doi.org/10.1007/s11095-012-0827-0

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