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Purpose:To evaluate the effect of borneol on the brain targeting efficiency of Aprotinin-conjugated poly(ethyleneglycol)-poly(L-lactic-co-glycolic acid) nanoparticles(Apr-NP) and the activity of huperzine A (Hup A) loaded nanoparticles to AD rats.Method:Apr-NP was prepared by emulsion and solvent evaporation method.The uptakeof Apr-NPalone or combined with borneol by brain capillary endothelial cells (BCECs) was evaluated by incorporatingcoumarin-6 as a tracer.In vivo imaging and the distribution of Hup A in the brain was measured thebrain delivery of Apr-NP in rats,with or without the oraladministration of bomeol.Morris water maze was used to evaluatethe memory improvement effect of HupA loaded nanoparticles (Apr-NP-Hup).Results:Co-incubation with borneol could increase the uptake of nanoparticles by BCECs.Nanoparticles delivered into the brain were enhanced significantly by the co-administration of bomoel.The pharmacological effects of Hup A loaded nanoparticles on improving the memory impairment of AD rats were greatly improved when combined with borneol.Conclusions:Borneol is a promising enhancer for brain-targeting delivery systems.When co-administered with aprotinin-modified nanoparticles, borneol could improve the brain targeting efficiency of nanoparticles significantly.