Dry powder inhalation of celecoxib nanoparticles: Formulation and in-vitro characterization

Abstract

The aim of the present study was to develop and optimize Celecoxib (CAS number: 169590-42-5) nanocrystals for pulmonary delivery potential for application in lung cancer. Nanocrystals were prepared by the liquid anti solvent precipitation method using lecithin as a stabilizer. According to the limited number of approved excipients for application in the formulations intended to be used for pulmonary delivery, a narrow range of materials documented as generally recognized as safe (GRAS) excipient such as lecithin and mannitol were used in the present study. The optimized formulation in the size of 79 nm was co-spray dried with varying amounts of mannitol to form aggregated nanocrystals appropriate for application in drug delivery to the lung. The aerosolization efficiency of dry powders was determined by next generation impactor (NGI). The amount of Celecoxib in the stages of NGI was measured by an HPLC technique developed by the authors. The results of different formulations showed around 4 % fine particle fraction (FPF). The low melting point and hygroscopic characteristic of lecithin might be responsible for the observed not ideal aerosolization performance of formulations. The obligation in application of just few excipients in the formulations for pulmonary administration creates the challenge of being open while at the same time preparing efficient formulations for pulmonary delivery. é 2015 ECV Editio Cantor Verlag, Aulendorf (Germany).