Evaluating the Effect of Sodium Alginate and Sodium Carboxymethylcellulose on Pulmonary Delivery of Levofloxacin Spray-Dried Microparticles Publisher Pubmed



Alizadeh H¹ ; Khoshhal P¹ ; Mirmoeini MS¹ ; Gilani K¹ Show Affiliations
Source: DARU, Journal of Pharmaceutical Sciences Published:2024

Abstract

Background: Patients with cystic fibrosis commonly suffer from lung infections caused by Pseudomonas aeruginosa. Recently, the Levofloxacin (LVF) nebulizing solution (Quinsair®) has been prescribed for the antimicrobial management. The sustained-release (SR) dry powder formulation of LVF is a convenient alternative to Quinsair®. It has the potential to enhance patient convenience and decrease the likelihood of drug resistance over time. Objective: In this paper, we set forth to formulate and evaluate the potential application of sodium alginate (SA) and sodium carboxymethylcellulose (SCMC) for sustained pulmonary delivery of LVF. Methods: The spray-dried (SD) LVF microparticles were formulated using SCMC and SA along with L-leucine (Leu). The microparticles were analyzed in terms of particle size, morphology, x-ray diffraction (XRD), in-vitro drug release, and aerodynamic properties. Selected formulations were further proceeded to short-term stability test. Results: The polymer-containing samples displayed process yield of 33.31%–39.67%, mean entrapment efficiency of 89% and volume size within the range of 2–5 μm. All the hydrogel microparticles were amorphous and exhibited rounded morphology with surface indentations. Formulations with a drug-to-excipient ratio of 50:50 and higher, showed a 24-h SR. The aerodynamic parameters were fine particle fraction and emitted dose percentage ranging between 46.21%–60.6% and 66.67%–87.75%, respectively. The short-term stability test revealed that the formulation with a 50:50 drug-to-excipient ratio, containing SA, demonstrated better physical stability. Conclusion: The selected formulation containing SA has the potential to extend the release duration. However, further enhancements are required to optimize its performance. Graphical abstract: (Figure presented.) © The Author(s), under exclusive licence to Tehran University of Medical Sciences 2024.