Production, characterisation, and in vitro nebulisation performance of budesonide-loaded PLA nanoparticles

Abstract

The aim of this study is to prepare a nanosuspension of budesonide for respiratory delivery using nebuliser by optimising its particle size and characterising its in vitro deposition behaviour. PLA (poly lactic acid)–budesonide nanosuspension (BNS) was prepared using high-pressure emulsification/solvent evaporation method. To optimise particle size, different parameters such as PLA concentration, sonication time, and amplitude were investigated. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscope (SEM) analyses were performed to characterise the prepared PLA–budesonide nanoparticles. The in vitro aerodynamic characteristics of the PLA–BNS using a jet nebuliser were estimated and compared with that of commercially available suspension formulation of budesonide.

Budesonide-loaded PLA nanoparticles with fine particle size (an average size of 224–360 nm), narrow size distribution, and spherical and smooth surface were prepared. The optimum condition for preparation of fine particle size for aerosolisation was found to be at PLA concentration of 1.2 mg/ml and amplitude of 70 for 75 s sonication time. The in vitro aerosolisation performance of PLA–BNS compared to that of commercial budesonide indicated that it has significantly (p < 0.05) smaller mass median aerodynamic diameter (MMAD) value with an enhancement in fine particle fraction (FPF) value. Improving the in vitro deposition of budesonide, PLA–BNS could be considered as a promising alternative suspension formulation for deep lung delivery of the drug using nebuliser.

• Budesonide
• in vitro deposition
• nanosuspension
• nebuliser
• PLA nanoparticles

Acknowledgements

This work was financially supported by the Grant no. 90-01-87-13157 from Tehran University of Medical Sciences, Tehran, Iran.