Formulation and In Vitro Evaluation of Sterically Stabilised Phospholipid Nanomicelles Loaded with Beclomethasone Dipropionate for Nebulisation

摘要

Purpose: The aim of this study was to formulate and evaluate the potential of sterically stabilised phospholipid nanomicelles (SSMs) loaded with beclomethasone dipropionate (BDP) for pulmonary delivery through nebulisation. Method: BDP-SSMs were prepared by the coprecipitation and reconstitution method and characterised for different physicochemical and aerodynamic properties. Results: Particle size of BDP-SSMs determined by photon correlation spectroscopy (PCS) was 19.89±0.67 nm with polydispersity index of approximately 0.22±0.02. At 5mM of PEG5000-DSPE, the maximum solubilisation efficiency of BDP was 209.65±7.74 ng/ml with a single-sized peak population. Zeta potential measurement of BDP-SSMs was -28.03±2.05 mV. The entrapment efficiency (%EE), yield (%Y) and drug loading (%DL) of the lyophilised formulations were 100.87±3.5, 95.11±0.38 and 0.72± 0.03%, respectively. TEM photograph of BDP-SSMs revealed spherical nanoparticles. BDP-SSMs exhibited a prolonged dissolution behaviour as compared to solubilised BDP powder (P <0.05). Aerodynamic characteristic values of BDP-SSMs using Pari LC or Omron nebulisers were equivalent and more superior than some marketed inhaler products. Conclusion: SSMs showed great potential as pulmonary delivery systems for BDP as they exhibited high pulmonary deposition and prolonged in vitro release.