Excipient-Free Inhalable Microparticles of Azithromycin Produced by Electrospray: A Novel Approach to Direct Pulmonary Delivery of Antibiotics.
Beatriz ArauzoTania B Lopez-MendezMaría Pilar LoberaJavier Calzada-FunesJosé Luis PedrazJesus SantamariaPublished in: Pharmaceutics (2021)
Inhalation therapy offers several advantages in respiratory disease treatment. Azithromycin is a macrolide antibiotic with poor solubility and bioavailability but with a high potential to be used to fight lung infections. The main objective of this study was to generate a new inhalable dry powder azithromycin formulation. To this end, an electrospray was used, yielding a particle size around 2.5 µm, which is considered suitable to achieve total deposition in the respiratory system. The physicochemical properties and morphology of the obtained microparticles were analysed with a battery of characterization techniques. In vitro deposition assays were evaluated after aerosolization of the powder at constant flow rate (100 L/min) and the consideration of the simulation of two different realistic breathing profiles (healthy and chronic obstructive pulmonary disease (COPD) patients) into a next generation impactor (NGI). The formulation was effective in vitro against two types of bacteria, Staphylococcus aureus and Pseudomonas aeruginosa . Finally, the particles were biocompatible, as evidenced by tests on the alveolar cell line (A549) and bronchial cell line (Calu-3).
Keyphrases
- chronic obstructive pulmonary disease
- pseudomonas aeruginosa
- staphylococcus aureus
- mass spectrometry
- end stage renal disease
- lung function
- ejection fraction
- drug delivery
- newly diagnosed
- liquid chromatography
- chronic kidney disease
- cystic fibrosis
- pulmonary hypertension
- prognostic factors
- high throughput
- risk assessment
- human health
- climate change
- multidrug resistant
- mesenchymal stem cells
- methicillin resistant staphylococcus aureus
- virtual reality