Ciprofloxacin-Loaded Inorganic-Organic Composite Microparticles To Treat Bacterial Lung Infection
Frederic Tewes1,2, Julien Brillault1, Barbara Lamy1
1INSERM U 1070, Pôle Biologie-Santé, Faculté de Médecine & Pharmacie, Université de Poitiers , CHU de Poitiers, 86022 Poitiers Cedex, France.
Molecular Pharmaceutics
|December 8, 2015
Summary
Inhalable calcium microparticles were developed to sustain ciprofloxacin (CIP) antibiotic levels in the lungs, reducing systemic absorption and enhancing therapeutic efficacy against lung infections.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Infectious Diseases
Background:
- Ciprofloxacin (CIP) is an antibiotic used for lung infections via aerosolization.
- Rapid systemic absorption of CIP after lung administration leads to subtherapeutic concentrations and promotes bacterial resistance.
Purpose of the Study:
- To develop inhalable calcium-based composite microparticles for sustained CIP delivery to the lungs.
- To reduce systemic absorption and maintain effective pulmonary CIP concentrations.
Main Methods:
- Characterization of microparticle aerodynamics and micromeritics.
- FTIR and XRD analysis to determine particle composition and CIP-calcium interaction.
- In vitro release studies and Calu-3 cell monolayer transport assays.
Main Results:
- Amorphous calcium carbonate and formate formed the inorganic component; CIP and calcium interacted in a 1:1 ratio.
- Complete CIP release within 7 hours, with pH-dependent profiles.
- Up to 84% reduction in CIP apparent permeability across Calu-3 cells, with no change in antimicrobial activity.
Conclusions:
- Designed calcium-based microparticles can sustain CIP levels in the lung.
- Controlled CIP release and reduced epithelial permeability offer potential for improved lung infection treatment.
- This approach allows for controlled pharmacokinetics of CIP within the lung.
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