Design and Production of Respirable Effervescent Microparticles to Enhance Drug Penetration Through Lung Mucus
Abstract
Background/Objectives: Dry powder inhalation (DPI) is a promising strategy for the treatment of respiratory diseases such as cystic fibrosis (CF), where thick and viscous mucus limits drug penetration and contributes to persistent infection and inflammation. Although inhalation allows rapid drug action with reduced systemic exposure, its efficacy depends on the ability of inhaled drugs to achieve and maintain therapeutic concentrations in the lungs and to overcome airway barriers. This study aimed to develop and characterize effervescent dry powder formulations designed to enhance mucus permeabilization through mechanical disruption while delivering an antibiotic. Methods: Effervescent microparticles containing sodium bicarbonate, an organic acid (citric or tartaric acid), and levofloxacin were produced by spray drying using a triple-fluid nozzle to control component distribution and prevent premature effervescence. The influence of functional excipients, including L-leucine and mannitol, on particle formation, aerosol performance, and process yield was evaluated. Microparticles were characterized in terms of morphology, fine particle fraction (FPF), and effervescence-related properties. Results: Formulations containing L-leucine and citric acid reduced particle agglomeration and achieved a fine particle fraction of up to approximately 18%, although with a lower process yield. In contrast, formulations based on tartaric acid and mannitol improved both production yield and…
Read the paper
Related studies
- Ferulic acid regulates the AKT/GSK-3β/CRMP-2 signaling pathway in a middle cerebral artery occlusion animal model
- Novel Pharmacokinetic/Pharmacodynamic Parameters Quantify the Exposure–Effect Relationship of Levofloxacin against Fluoroquinolone-Resistant Escherichia coli
- Photochemical behavior of levofloxacin
- Correlation Between Dissolution Profiles of Salt-Form Drugs in Biorelevant Bicarbonate Buffer and Oral Drug Absorption: Importance of Dose/ Fluid Volume Ratio
- Evaluation of the synergistic potential and mechanisms of action for de novo designed cationic antimicrobial peptides
- Synthesis of [11C]levofloxacin
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.