Development of tiotropium inhalation formulations for the treatment of chronic obstructive pulmonary disease

Abstract

Tiotropium, a longer acting anticholinergic bronchodilator, has been widely used for treatment of chronic obstructive pulmonary disease (COPD). To improve the therapeutic effect of tiotropium, we developed various inhalation microparticular formulations of tiotropium using starch, hyaluronate, bovine serum albumin (BSA), and poly(lactide-co-glycolide) (PLGA). All formulations showed ~90 % inhalation efficiency in the lung epithelium of BALB/c mice after initial administration. Interestingly, when compared to other formulations using starch, hyaluronate, and BSA, the inhalation formulation of tiotropium using PLGA showed longer drug residence (up to 7 days) in in vivo lung epithelium. We believe that this microparticle system is expected to improve the treatment efficacy for the patients with COPD by maintaining drug therapeutic effect during the extended period after initial inhalation. © 2013 The Korean Society of Pharmaceutical Sciences and Technology.