The mechanism of the opening of the blood–brain barrier by borneol: A pharmacodynamics and pharmacokinetics combination study

摘要: Abstract Ethnopharmacological relevance Borneol is widely used in traditional Chinese medicine to facilitate the distribution of central nervous system (CNS) drugs brain due its ability open blood–brain barrier (BBB), however, underlying mechanism still unclear. In this study, effect borneol on different regions were investigated explore mechanism. Materials and methods After oral administration (0.1, 0.2 g/kg) for seven consecutive days, SD rats injected with Rh123 (1.0 mg/kg). The concentrations detected four cortex, hippocampus, hypothalamus striatum by a small animal vivo imaging fluorescence microplate reader respectively. ultrastructures BBB examined. Moreover, expressions transporters ATP-binding cassette (ABC) family, multidrug resistance 1a (Mdr1a), 1b (Mdr1b), protein 1 (Mrp1), Mrp4, Mrp5 breast cancer (Bcrp) analyzed. Finally, deliveries plasma examined pharmacokinetics study. Results Administration 0.2 g/kg produced loose structure tight junction void between endothelial cell mesangial cell. at 0.1 g/kg increased delivery hippocampus obviously. Permeability index followed similar trend. Protein expression assays showed that decreased Mdr1 Mrp1 hypothalamus. Further RT-PCR study both Mdr1a Mdr1b demonstrated cortex was most least, between. Conclusions tissue specific BBB-opening effect, which associated regulation ultrastructure tissues Mdr1a, Mrp1. present indicated should be concert targeting or exert synergistic maximum.