The Use of Borneol as an Enhancer for Targeting Aprotinin-Conjugated PEG-PLGA Nanoparticles to the Brain
The Use of Borneol as an Enhancer for Targeting Aprotinin-Conjugated PEG-PLGA Nanoparticles to the Brain
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DOI：
10.1007/s11095-013-1055-y
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发表时间：
2013-10-01
影响因子：
3.7
通讯作者：
Wang, Jianxin
中科院分区：
文献类型：
--
作者：
Zhang, Lin;Han, Limei;Wang, Jianxin
目的：探讨冰片对抑肽蛋白偶联聚乙二醇-聚l -乳酸-羟基乙酸纳米颗粒（Apr-NP）脑靶向效率及负载石杉碱A （Hup A）纳米颗粒对AD大鼠脑靶向活性的影响。采用乳液和溶剂蒸发法制备了Apr-NP。采用香豆素-6作为示踪剂，评价脑毛细血管内皮细胞（BCECs）对Apr-NP单独或联合冰片的摄取情况。通过体内显像和Hup A在脑内的分布，研究口服或不口服冰片时Apr-NP在大鼠脑内的传递情况。采用Morris水迷宫法评价负载Hup A纳米颗粒（Apr-NP-Hup）对小鼠记忆的改善效果。与冰片共孵育可增加bcec对纳米颗粒的吸收。同时给药冰片可显著增强大鼠脑内纳米颗粒的活性。负载Hup A纳米颗粒与冰片联合后，其改善AD大鼠记忆损伤的药理作用明显增强。冰片是一种很有前途的脑靶向递送系统增强剂。冰片与抑肽蛋白修饰的纳米颗粒共同给药，可显著提高纳米颗粒的脑靶向效率。
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 .Apr-NP was prepared by emulsion and solvent evaporation method. The uptake of Apr-NP alone or combined with borneol by brain capillary endothelial cells (BCECs) was evaluated by incorporating coumarin-6 as a tracer. In vivo imaging and the distribution of Hup A in the brain were measured to investigate the brain delivery of Apr-NP in rats, with or without the oral administration of borneol. Morris water maze was used to evaluate the memory improvement effect of Hup A loaded nanoparticles (Apr-NP-Hup).Co-incubation with borneol could increase the uptake of nanoparticles by BCECs. Nanoparticles delivered into the rat brain were enhanced significantly by the co-administration of borneol. The pharmacological effects of Hup A loaded nanoparticles on improving the memory impairment of AD rats were greatly improved when combined with borneol.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.