Inhalation of Tetrandrine-hydroxypropyl-β-cyclodextrin Inclusion Complexes for Pulmonary Fibrosis Treatment.,Molecular Pharmaceutics

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Inhalation of Tetrandrine-hydroxypropyl-β-cyclodextrin Inclusion Complexes for Pulmonary Fibrosis Treatment.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-03-06 , DOI: 10.1021/acs.molpharmaceut.0c00026
Wenqiang Su _{1,

2} , Yinmei Liang _{1,

2} , Zhiping Meng _{1,

2} , Xuanyu Chen _{1,

2} , Manqi Lu ₃ , Xingxing Han _{1,

2} , Xiaomin Deng _{1,

2} , Qichun Zhang _{1,

2} , Huaxu Zhu _{1,

2,

4} , Tingming Fu _{1,

2,

4}

Affiliation

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.

中文翻译：

吸入粉防己碱-羟丙基-β-环糊精包合物对肺纤维化的治疗。

肺纤维化（PF）是一种间质性肺疾病，具有进行性呼吸道疾病和致命性呼吸困难的特征。粉防己碱（TET）是中草药Stephania tetrandra S. Moore的主要活性成分，该药物已在临床上用于治疗风湿病，肺癌和矽肺病。在这项工作中，粉防己碱-羟丙基-β-环糊精包合物（TET-HP-β-CD）被开发用于通过吸入给药治疗肺纤维化。TET-HP-β-CD通过冷冻干燥方法制备，并使用级联撞击器，差示扫描量热法（DSC），X射线衍射（XRD）和傅里叶变换红外光谱（FT-IR）进行鉴定。使用博来霉素诱导的肺纤维化大鼠模型评估吸入的TET和TET-HP-β-CD的作用。动物存活，肺中羟脯氨酸含量和肺组织学检查。结果表明，吸入TET-HP-β-CD可以减轻炎症和纤维化，限制肺中羟脯氨酸的积累，调节PF发育过程中的蛋白表达，并改善术后生存期。而且，与静脉内给药相比，TET-HP-β-CD的雾化递送主要在肺中积累，并且全身分布有限。目前的结果表明，吸入TET-HP-β-CD是治疗肺纤维化的诱人候选物。与静脉内给药相比，TET-HP-β-CD的雾化输送主要在肺中积累，并且全身分布有限。目前的结果表明，吸入TET-HP-β-CD是治疗肺纤维化的诱人候选物。与静脉内给药相比，TET-HP-β-CD的雾化输送主要在肺中积累，并且全身分布有限。目前的结果表明，吸入TET-HP-β-CD是治疗肺纤维化的诱人候选物。

更新日期：2020-03-06

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