Mechanistic Insight into the Enhanced Anti-Pulmonary Hypertension Efficacy of Wogonin Co-Amorphous

<b>Background:</b> Pulmonary hypertension (PH) remains a life-threatening rare disease characterized by inflammation and oxidative stress in pulmonary artery smooth muscle cells (PASMCs). Wogonin (Wog), a plant-derived polyphenolic compound extracted from <i>Scutellaria baicalensis...

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Main Authors: Zhongshui Xie, Yucai Chen, Jiaqi Xie, Yan Lei, Chunxue Jia, Yulu Liang, Hongjuan Wang, Jianmei Huang
Format: Article
Language:English
Published: MDPI AG 2025-05-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/6/724
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Summary:<b>Background:</b> Pulmonary hypertension (PH) remains a life-threatening rare disease characterized by inflammation and oxidative stress in pulmonary artery smooth muscle cells (PASMCs). Wogonin (Wog), a plant-derived polyphenolic compound extracted from <i>Scutellaria baicalensis</i> Georgi, exhibits notable antioxidant activity and anti-PH efficacy, whereas its clinical applications are greatly limited by poor aqueous solubility. <b>Methods</b>: Herein, an innovative wogonin-aloperine co-amorphous (Wog-Alop) was developed to improve the aqueous solubility and, thus, anti-PH efficacy of Wog. <b>Results</b>: As expected, the aqueous solubility of Wog-Alop is about 40-fold that of Wog; meanwhile, the Wog-Alop demonstrates better oral bioavailability and anti-PH efficacy than Wog; moreover, the Wog-Alop exhibits significantly enhanced capacity to attenuate oxidative stress in human PASMCs compared to Wog. <b>Conclusions</b>: The results suggested that Wog-Alop could not only improve the solubility of Wog, thereby enhancing its oral bioavailability but also alleviate Wog’s oxidative stress effects. These synergistic effects ultimately culminate in the enhanced anti-PH efficacy of Wog. In summary, the present study developed an innovative co-amorphous strategy for the delivery of Wog and improved its anti-PH efficacy.
ISSN:1999-4923