DRY POWDER INHALER BASED ON FLUOROQUINOLONE AND POLYELECTROLYTES: A REVIEW

M. F. RAZUC; N. CESCHAN; J. PIÑA; V. BUCALÁ; M. V. RAMIREZ RIGO

Cordoba

Congreso; 3 rd International Meeting on Pharmaceutical Sciences,; 2014

Universidad Nacional de Cordoba

Some of the most important bacteria that cause lethal pulmonary infections are Mycobacterium tuberculosis and Pseudomonas aeruginosa. Fluoroquinolones (F) are switerionic antibiotics that are active against these bacteria. In this sense, the pulmonary route offers the advantages of delivering the drug directly to the infection site and reducing systemic toxicity. Dry powder inhalers (DPI) have become increasingly popular as a pulmonary delivery system because of the following reasons: high chemical stability, environmentally friendly and a breath actuated delivery. Besides, ionizable drugs can be combined with polyelectrolytes (PE) that have opposite charge. This strategy could modify stability, solubility, dissolution or permeation of drugs. Therefore, administering PE-F complexes as DPI may improve the bioavailability and/or stability of F for this route. The aim of this work is to review scientific reports in order to determine the potentiality of obtaining particles of PE-F complexes for pulmonary administrations and to highlight the main achievements and challenges in the area. The materials analyzed were the cationic PE chitosan and the anionic PEs dextran, alginic acid, hyaluronic-acid, poly(lactic-co-glycolic-acid) and poly(ε-caprolactone). The particles were prepared by spray-drying or spray-freeze-drying techniques, using aqueous solutions and/or organic solvents. The obtained particles were rounded, monodisperse and had suitable aerodynamic diameters to reach the lower respiratory tract. The effect of the processing variables on particles´ size was also studied. The microbiological activity of the powders remained unchanged and high drug loading was achieved. Moreover, the PE-F particles were found to be carriers that can target F to the action sites improving the drug bioavailability, due to changes in the bioadherence and mucociliary clearance and, thus, in the drug stability, dissolution and permeability of the drug. These powders combined the attractive characteristics of PE-F complexes and inhalable particles. Therefore, these materials have been proved to be invaluable carriers of F to the lower respiratory tract. The specific challenges are to obtain particles through a simple and environmentally friendly technique with high bioavailability.