Enhancing the stability, BBB permeability and neuroprotective activity of verbascoside in vitro using lipid nanocapsules in combination with menthol. (15th July 2023) - Wu, Lipeng
Graphical abstract: Highlights: VER-RM-LNC was prepared by a simple phase inversion temperature method. VER encapsulated into LNC showed enhanced stability and a reduced release profile. VER-RM-LNC combined with menthol can increase the neuroprotective activity of VER. Abstract: 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 Aβ25-35 .