Abstract：
OBJECTIVES:The development of inhaled products to treat or to prevent lung infection is a very active research field in drug delivery. The pulmonary route is extremely attractive but very challenging. This paper reports the study of excipient, capsule brand and device influence on the aerodynamic behavior of dry powder formulations to treat tuberculosis. METHODS:A capreomycin hydrophobic salt was powdered using spray-drying and formulated using lactose (added after spray-drying, external excipient) or L-leucine (added before spray-drying, internal excipient). Aerosolization performances were investigated loading the formulations in 2 different capsule brands and aerosolizing them with 3 different devices. RESULTS:Capreomycin oleate and capreomycin oleate/l-leucine powders were produced with a yield around 70%. Capreomycin oleate powder was composed of particles with an irregular surface. Particles of capreomycin oleate/l-leucine were roundish and wrinkled on the surface. Capreomycin oleate/l-leucine formulation gave the highest values of respirable fraction in all cases. Statistical analysis asserted the significant effect on the respirable fraction of the powder (p≤0.001), the capsule brand (p≤0.01) and the device (p≤0.05). CONCLUSIONS:The use of L-leucine as internal excipient allows one to avoid the use of lactose, obtaining a carrier-free formulation. Even though differences are not very large, to obtain the highest RFE, the best choice between capsule and device is Quali-V(®) and model 8.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Schoubben A,Blasi P,Giontella A,Giovagnoli S,Ricci Mdoi
10.1016/j.ijpharm.2015.08.012subject
Has Abstractpub_date
2015-10-15 00:00:00pages
40-8issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(15)30109-5journal_volume
494pub_type
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