Abstract：
:We investigated the feasibility of preparing high-potency tacrolimus dry powder for inhalation using thin film freezing (TFF). We found that using ultra-rapid freezing can increase drug loading up to 95% while maintaining good aerosol performance. Drug loading affected the specific surface area and moisture sorption of TFF formulations, but it did not affect the chemical stability, physical stability, and dissolution of tacrolimus. Tacrolimus remained amorphous after storage at 40 °C/75% RH, and 25 °C/60% RH for up to 6 months. Lactose functioned as a bulking agent, and it had little to no effect as a stabilizer for amorphous tacrolimus due to a lack of interaction between the drug and excipient. Additionally, the aerosol performance of TFF tacrolimus/lactose (95/5) did not significantly change after six months of storage at 25 °C/60% RH. For processing parameters, the solids content and the processing temperature did not affect the aerosol performance of tacrolimus. Furthermore, both low- and high-resistance RS01 showed optimal and consistent aerosol performance over the 1-4 kPa pressure drop range. In conclusion, TFF is a suitable technology for producing inhalable powder that contain high drug loading and have less flow rate dependence.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Sahakijpijarn S,Moon C,Ma X,Su Y,Koleng JJ,Dolocan A,Williams RO 3rddoi
10.1016/j.ijpharm.2020.119490subject
Has Abstractpub_date
2020-08-30 00:00:00pages
119490eissn
0378-5173issn
1873-3476pii
S0378-5173(20)30474-9journal_volume
586pub_type
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