Enhancing the stability, BBB permeability and neuroprotective activity of verbascoside in vitro using lipid...

Verbascoside (VER) shows promising neuroprotective activity. However, the instability and low permeability in crossing the blood-brain barrier (BBB) greatly hinder its application. In the present study, verbascoside was encapsulated into lipid nanocapsules (LNC) by reverse micelle (RM) to increase its stability. Besides, we used VER-RM-LNC combined with an envoy drug, menthol, to improve its BBB permeability and neuroprotective activity. VER-RM-LNC was prepared by the phase inversion temperature method, resulting in an encapsulation efficiency of nearly 85 %. The formulated VER-RM-LNC was stable for 6 months at 4 °C. VER encapsulated into LNC possessed enhanced stability and a reduced release profile. Menthol increased the cellular uptake and the permeability of VER-RM-LNC in the BBB model in vitro. In addition, the improved neuroprotective activity of VER through incubation with menthol and VER-RM-LNC was verified in the neurotoxic human brain microvascular endothelial cells model induced by Aβ_25-35.