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Development of ciprofloxacin-loaded poly(vinyl alcohol) dry powder formulations for lung delivery
Dina M Silva1, Roberto Paleco2, Daniela Traini2
1School of Mechanical, Materials, Mechatronic and Biomedical Engineering, University of Wollongong, Wollongong, NSW 2522, Australia.
Abstract:
Polymeric microparticles are micro carriers for the sustained drug delivery of drugs in the lungs, used as alternatives to the use of established excipients. This study aims to develop and characterize inhalable ciprofloxacin (CPx)-loaded poly(vinyl alcohol) (PVA) microparticles by a single-step spray-drying procedure. The optimization of the processing parameters was achieved by an orthogonal design of the most relevant processing parameters (polymer concentration, feed rate and inlet temperature). The obtained spray-dried particles showed a drug encapsulation efficiency higher than 90%. Furthermore, PVA-CPx formulations, with drug contents up to 10 wt%, showed a morphology and size suitable for inhalation, with a sustained release profile over 24 h. Data from Fourier transformed infra-red spectroscopy and differential scanning calorimetry indicated absence of interaction between the polymer matrix and the drug. Aerodynamic assessment of PVA-CPx 10 wt% was determined by the next generation impactor (NGI), using spray-dried CPx as a control. The results showed improved values of mass median aerodynamic diameter (5.06±0.10μm) and a fine particle fraction (39.78±0.98%) when comparing with the CPx alone (5.33±0.39μm and 30.43±1.38%). This study highlights the potential of spray-dried PVA microparticles as drug carriers for lung local delivery of antibiotics.
Insights
This study developed inhalable ciprofloxacin-loaded poly(vinyl alcohol) microparticles for sustained lung drug delivery. The optimized microparticles demonstrated high encapsulation efficiency and improved aerodynamic properties for antibiotic treatment.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Polymeric microparticles serve as advanced carriers for sustained lung drug delivery.
- They offer an alternative to traditional excipients in pulmonary drug formulations.
Purpose of the Study:
- To develop and characterize inhalable ciprofloxacin (CPx)-loaded poly(vinyl alcohol) (PVA) microparticles.
- To optimize processing parameters for effective drug encapsulation and suitable aerodynamic properties for inhalation.
Main Methods:
- Single-step spray-drying technique was employed for microparticle fabrication.
- Orthogonal experimental design was used to optimize polymer concentration, feed rate, and inlet temperature.
- Fourier transformed infrared spectroscopy, differential scanning calorimetry, and next-generation impactor were utilized for characterization and aerodynamic assessment.
Main Results:
- Spray-dried PVA-CPx microparticles achieved over 90% drug encapsulation efficiency.
- Formulations exhibited suitable morphology and size for inhalation, with sustained drug release over 24 hours.
- Aerodynamic assessment showed improved mass median aerodynamic diameter (5.06±0.10μm) and fine particle fraction (39.78±0.98%) compared to CPx alone.
Conclusions:
- Spray-dried poly(vinyl alcohol) microparticles are effective carriers for sustained lung delivery of ciprofloxacin.
- These microparticles hold significant potential for local antibiotic delivery in the lungs, improving therapeutic outcomes.
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