Design and Comprehensive Characterization of Tetramethylpyrazine (TMP) for Targeted Lung Delivery as Inhalation Aerosols in Pulmonary Hypertension (PH): In Vitro Human Lung Cell Culture and In Vivo Efficacy.
Design and Comprehensive Characterization of Tetramethylpyrazine (TMP) for Targeted Lung Delivery as Inhalation Aerosols in Pulmonary Hypertension (PH): In Vitro Human Lung Cell Culture and In Vivo Efficacy.
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DOI：
10.3390/antiox10030427
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发表时间：
2021-03-11
期刊：
影响因子：
--
通讯作者：
Mansour HM
中科院分区：
文献类型：
--
作者：
Muralidharan P;Acosta MF;Gomez AI;Grijalva C;Tang H;Yuan JX;Mansour HM
这是第一项关于设计和开发新型天然抗氧化剂治疗药物川芎嗪（TMP）（也称为川芎嗪）的创新吸入制剂的研究。TMP从属于甘草类的中草药中获得。已知它具有抗氧化特性。它可以作为Nrf 2/ARE激活剂和Rho/ROCK抑制剂。本研究报告首次全面表征原料TMP（非喷雾干燥）和喷雾干燥TMP在一个系统的方式，使用热分析，电子显微镜，光学显微镜，和拉曼光谱。使用三种不同的FDA批准的基于单位剂量胶囊的人干粉吸入器装置测试喷雾干燥的TMP的体外气溶胶分散性能。对来自人肺不同区域的肺细胞进行体外人细胞研究，以检查TMP的生物相容性和非细胞毒性。此外，使用野百合碱（MCT）诱导的PH大鼠模型，在体内测试了吸入TMP作为液体和干粉吸入气雾剂的疗效。
This is the first study reporting on the design and development innovative inhaled formulations of the novel natural product antioxidant therapeutic, tetramethylpyrazine (TMP), also known as ligustrazine. TMP is obtained from Chinese herbs belonging to the class of Ligusticum. It is known to have antioxidant properties. It can act as a Nrf2/ARE activator and a Rho/ROCK inhibitor. The present study reports for the first time on the comprehensive characterization of raw TMP (non-spray dried) and spray dried TMP in a systematic manner using thermal analysis, electron microscopy, optical microscopy, and Raman spectroscopy. The in vitro aerosol dispersion performance of spray dried TMP was tested using three different FDA-approved unit-dose capsule-based human dry powder inhaler devices. In vitro human cellular studies were conducted on pulmonary cells from different regions of the human lung to examine the biocompatibility and non-cytotoxicity of TMP. Furthermore, the efficacy of inhaled TMP as both liquid and dry powder inhalation aerosols was tested in vivo using the monocrotaline (MCT)-induced PH rat model.
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