Preparation of Co-Amorphous Levofloxacin Systems for Pulmonary Application

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery
• Antimicrobial Resistance

Background:

• Levofloxacin (LEV) is vital for lung infections but causes severe side effects.
• Reducing systemic LEV concentrations is needed to mitigate toxicity and antibiotic excretion.
• Novel pulmonary drug delivery systems are required to address these challenges.

Purpose of the Study:

• To develop a pulmonary-applicable levofloxacin (LEV) formulation.
• To create co-amorphous LEV-L-arginine (ARG) particles for enhanced lung delivery.
• To assess the feasibility of sustainable antibiotic therapy through improved LEV formulation.

Main Methods:

• Co-amorphous LEV-ARG particles were prepared using spray drying.
• Characterization involved SEM, DSC, XRD, FTIR, and next-generation impactor analysis.
• Process parameters like solvent composition and temperature were optimized.

Main Results:

• Spray drying successfully produced co-amorphous LEV-ARG particles.
• A 30% ethanol solvent yielded superior aerodynamic properties compared to aqueous solutions.
• The formulation achieved a fine particle fraction >50% and emitted dose >95%, suitable for pulmonary application.

Conclusions:

• The developed co-amorphous LEV-ARG formulation is suitable for pulmonary delivery.
• The spray drying process is robust and scalable for producing effective antibiotic particles.
• This approach offers a promising strategy for sustainable antibiotic therapy with reduced side effects.