Rapamycin-based inhaled therapy for potential treatment of COPD-related inflammation: production and characterization of aerosolizable nano into micro (NiM) particles
Emanuela Fabiola Craparo, Marta Cabibbo, Cinzia Scialabba, Luca Casula, Francesco Lai, Gennara Cavallaro
Abstract
-Man) was used to provide the macrophage-targeting lipid shell. The successful formation of Rapa@Man-LPHNPs was confirmed by TEM and DSC analyses. The loaded drug (4.3 wt% of the total weight) was slowly released from the polymeric core and protected from hydrolysis, with the amount of intact drug after 24 h of incubation in the medium being equal to 74 wt% (compared to 40% when the drug is freely incubated at the same concentration). To obtain a formulation administrable by inhalation, Rapa@Man-LPHNPs were entrapped inside PVA : LEU microparticles by using the nano into micro (NiM) strategy, specifically by spray drying (SD) in the presence of a pore-forming agent. In this way, NiM particles with geometric and theoretical aerodynamic diameters equal to 4.52 μm and 3.26 μm, respectively, were obtained. Furthermore, these particles showed optimal nebulization performance, having an FPF and an MMAD equal to 27.5% and 4.3 μm, respectively.