Mehdi Hassanpour Aghdam
1, Saeed Ghanbarzadeh
2,3, Yousef Javadzadeh
4, Hamed Hamishehkar
3*1 Research Center for Pharmaceutical Nanotechnology, and Students’ Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.
2 Zanjan Pharmaceutical Nanotechnology Research Center, and Department of Pharmaceutics, Faculty of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
3 Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
4 Biotechnology Research Center and Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Abstract
Purpose: Local therapy is a valuable and strategic approach in
the treatment of lung associated diseases and dry powder inhalation (DPI)
formulations play the key role in this plan. Transfersome has been introduced
as a novel biocompatible vesicular system with potential for administration in
pulmonary drug delivery. The present study was designed to prepare
Itraconazole-loaded nanotrantransfersomal DPI formulation.
Methods: Itraconazole-loaded nanotransfersomes with three
different types of surfactant in varying concentrations were prepared and
characterized in the point of particle size distribution and morphology by
laser light scattering and scanning electron microscopy (SEM) methods. The optimized
transferosomal formulations were co-spray dried with mannitol and the
aerosolization efficiency and aerodynamic properties of dry powders were
determined by next generation impactor using a
validated HPLC technique.
Results: The volume
mean diameter of optimized nanotransfersomal formulation with lecithin:Span®
60 in the ratio of 90:10 was 171 nm with narrow size distribution pattern
which increased up to 518 nm after drug loading. Different types of surfactant
did not influence the particle size significantly. SEM images confirmed the
formation of aggregated nanoparticles in the suitable range (1-5 µm) for the
pulmonary drug delivery. Aerosolization evaluation of co-spray dried
formulations with different amounts of mannitol indicated that 2:1 ratio of
mannitol:transfersome (w:w) showed the best aerosolization efficiency (fine
particle fraction (FPF)=37%). Increasing of mannitol significantly decreased
the FPF of the optimized formulations.
Conclusion: The results of this study was introduced the potential
application of nanotransfersomes in the formulation of DPIs for lung delivery
of various drugs.