Pulmonary
fibrosis (PF) is a kind of interstitial lung disease
with the features of progressive and often fatal dyspnea. Tetrandrine
(TET) is the major active constituent of Chinese herbal Stephania
tetrandra S. Moore, which has already applied clinically
to treat rheumatism, lung cancer, and silicosis. In this work, a tetrandrine-hydroxypropyl-β-cyclodextrin
inclusion compound (TET-HP-β-CD) was developed for the treatment
of pulmonary fibrosis via inhalation administration. TET-HP-β-CD
was prepared by the freeze-drying method and identified using the
cascade impactor, differential scanning calorimetry (DSC), X-ray diffraction
(XRD), and Fourier transform infrared spectrum (FT-IR). A bleomycin-induced
pulmonary fibrosis rat model was used to assess the effects of inhaled
TET and TET-HP-β-CD. Animal survival, hydroxyproline content
in the lungs, and lung histology were detected. The results showed
that inhalation of TET-HP-β-CD alleviated inflammation and fibrosis,
limited the accumulation of hydroxyproline in the lungs, regulated
protein expression in PF development, and improved postoperative survival.
Moreover, nebulized delivery of TET-HP-β-CD accumulated chiefly
in the lungs and limited systemic distribution compared with intravenous
administration. The present results indicated that inhalation of TET-HP-β-CD
is an attractive candidate for the treatment of pulmonary fibrosis.
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