1. Use of magnoflorine-phospholipid complex to permeate blood-brain barrier and treat depression in the CUMS animal model.
- Author
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Li B, Han L, Cao B, Yang X, Zhu X, Yang B, Zhao H, and Qiao W
- Subjects
- Animals, Antidepressive Agents administration & dosage, Antidepressive Agents blood, Aporphines administration & dosage, Aporphines blood, Behavior, Animal drug effects, Depression metabolism, Disease Models, Animal, Male, Mice, Inbred ICR, Permeability, Antidepressive Agents therapeutic use, Aporphines therapeutic use, Blood-Brain Barrier metabolism, Depression drug therapy, Drug Carriers chemistry, Phospholipids chemistry
- Abstract
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.
- Published
- 2019
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