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
AffiliationCollege of Pharmacy, The University of Arizona
Department of Medicine, Division of Translational & Regenerative Medicine, College of Medicine, The University of Arizona
Division of Translational & Regenerative Medicine, College of Medicine, The University of Arizona
The BIO5 Research Institute, The University of Arizona
Institute of the Environment, The University of Arizona
KeywordsAdvanced spray drying
Lung vascular disease
Respiratory drug delivery
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CitationMuralidharan, P.; Acosta, M.F.; Gomez, A.I.; Grijalva, C.; Tang, H.; Yuan, J.X.-J.; Mansour, H.M. 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. Antioxidants 2021, 10, 427.
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AbstractThis 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. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.
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Except where otherwise noted, this item's license is described as Copyright © 2021 by the authors. Licensee MDPI, Basel, Switzerland. This is an open access article distributed under the Creative Commons Attribution License.