Development of carrier free montelukast dry powder inhalation formulation

Abstract

While there are several approaches for treating pulmonary diseases, dry powder inhaler systems for pulmonary delivery have the encouraging potential to be alternative routes to oral drug administration. Particle engineering for pulmonary delivery can be performed by changing spray-drying conditions and formulation parameters which have an effect on the characteristics and morphology of particles. The present study aimed to prepare Montelukast sodium microparticles using the spray-drying technique to improve their respirable fraction and, as a result, their systemic bioavailability. In this study, microparticles were prepared using optimized process parameters and were characterized for aerosolization efficiency and different physicochemical parameters, including morphology, fine particle fraction (FPF), mass median aerodynamic diameter (MMAD), and geometric standard deviation (GSD) using scanning electron microscope (SEM), powder X-ray diffractometer, and Next Generation Impactor. Moreover, ammonium bicarbonate was used to reduce the aerodynamic diameter and aggregation of microparticles. SEM images showed that microparticles were in the appropriate range and had the appropriate shape and surface characteristics for pulmonary delivery. FPF, MMAD, and GSD for the optimized formulation were 48.3آ±5 %, 3.63آ±5.4 ?m, and 1.86آ±0.05, respectively. The addition of ammonium bicarbonate did not improve the aerosolization efficiency indexes. An evaluation of the aerosolization performance of spray-dried formulations indicated that the concentration of feed solution and solvent type substantially influenced aerosolization efficiency.