The influence of surfactant on the properties of albendazole-bile salts particles designed for lung delivery

Abstract

Albendazole is a first line drug for the treatment of several parasitic diseases in humans. Some parasites target the lungs, however lung delivery of albendazole has so far not been reported. We have developed albendazole-based powders suitable for pulmonary delivery, and studied the impact of surfactant on the formulation properties. High-pressure homogenization followed by spray drying was used to produce inhalable particles of albendazole containing the bile salts sodium taurocholate and sodium glycocholate. The process resulted in porous microparticles, that exhibited good spray drying yield (>50%), low moisture contents (<1%) and aerodynamic D90 < 5 μm. The particles showed adequate aerosolization performance either for normal conditions (respiratory fraction > 71%) or conditions that simulate decreased respiratory capacity (respiratory fraction > 49%). The powders did not disturb lung surfactant function. The comparison between both formulations has revealed that the properties of the surfactants affect mainly the particle size of the suspensions and the porosity of the powders. The higher porosity of the albendazole-sodium taurocholate powder led to an enhanced aerodynamic performance of the formulation compared to albendazole-sodium glycocholate. The developed albendazole powders may pave a way for local lung treatment of parasitic diseases.