Use of magnoflorine-phospholipid complex to permeate blood-brain barrier and treat depression in the CUMS animal model

Drug Delivery

Bing Yang¹  Bingjie Li²  Bingyan Cao²  Wei Qiao²  Xuehui Zhu²  Haodong Zhao²  Linmeng Han²  Xiaoying Yang² 

[1] Department of Cell Biology, School of Basic Medical Science, Tianjin Medical University, Tianjin, Chin;Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmacy, Tianjin Medical University, Tianjin, China;

关键词: Magnoflorine-phospholipid complex;    physicochemical characterization;    in vivo;    pharmacological evaluation;    western blotting analysis;   

DOI  :  10.1080/10717544.2019.1616236

来源: publisher

【 摘 要 】

To improve the liposolubility and blood-brain barrier permeability of magnoflorine, a new formulation of magnoflorine-phospholipid complex was prepared, characterized, and pharmacologically evaluated in the chronic unpredictable mild stress animal model. In this paper, the magnoflorine-phospholipid complex was synthesized and its characterization was determined. The antidepressant-like and antioxidant activity of magnoflorine-phospholipid complex was investigated by behavioral tests and western blotting analysis. As a result, the magnoflorine-phospholipid complex displayed high encapsulation efficiency and significantly improved the oil-water participate coefficient. In vivo blood-brain distribution study, the magnoflorine-phospholipid complex extended the duration of magnoflorine in blood and help magnoflorine to permeate the blood-brain barrier into brain. In behavioral tests, the magnoflorine-phospholipid complex significantly decreased immobility time compared to model control group in both FST and TST. Furthermore, the magnoflorine-phospholipid complex increased the expression of antioxidative stress-related proteins by the western blotting analysis. These findings strongly suggest that the phospholipid complex could significantly improve liposolubility, drug properties of magnoflorine and help magnoflorine permeate blood-brain barrier and exert the antidepressant effect.

【 授权许可】

CC BY