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

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...

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Bibliographic Details
Published in:Drug delivery 2019-01, Vol.26 (1), p.566-574
Main Authors: Li, Bingjie, Han, Linmeng, Cao, Bingyan, Yang, Xiaoying, Zhu, Xuehui, Yang, Bing, Zhao, Haodong, Qiao, Wei
Format: Article
Language:English
Subjects:
Antidepressants
Bioavailability
Blood-brain barrier
Drug delivery systems
Drugs
Efficiency
Ethanol
Flavonoids
in vivo blood-brain distribution
Laboratories
Magnoflorine-phospholipid complex
Medical research
Permeability
pharmacological evaluation
Pharmacy
physicochemical characterization
Spectrum analysis
western blotting analysis
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Summary: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.
ISSN:1071-7544
1521-0464
DOI:10.1080/10717544.2019.1616236