Excipient-Free Inhalable Microparticles of Azithromycin Produced by Electrospray: A Novel Approach to Direct Pulmonary Delivery of Antibiotics

• Autores principales: Beatriz Arauzo (Autor), Tania B. Lopez-Mendez (Autor), Maria Pilar Lobera (Autor), Javier Calzada-Funes (Autor), Jose Luis Pedraz (Autor), Jesus Santamaria (Autor)
• Formato: Libro
• Publicado: MDPI AG, 2021-11-01T00:00:00Z.
• Materias: article
• Acceso en línea: Connect to this object online.
• Notes: 10.3390/pharmaceutics13121988; 1999-4923
• Keywords: azithromycin; electrospray; pulmonary administration; dry powder; microparticles; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 13, Iss 12, p 1988 (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, <i>Staphylococcus aureus</i> and <i>Pseudomonas aeruginosa</i>. Finally, the particles were biocompatible, as evidenced by tests on the alveolar cell line (A549) and bronchial cell line (Calu-3).