Angiopep-2修饰脂质体的构建及其脑靶向性研究

Delivery capability study of Angiopep-2 Modified liposomes into brain

目的构建Angiopep-2修饰脂质体,并对其理化性质和跨血脑屏障能力进行评价。方法采用薄膜分散法制备Angiopep-2修饰脂质体(AP-LP),研究其理化特征。原代培养脑毛细血管内皮细胞(BCEC),通过定量细胞摄取实验研究BCEC对AP-LP脂质体的摄取率。复制体外模型,观察不同修饰的AP-LP穿过血脑屏障的能力。结果制备的AP-LP粒径为(125.0±15.5)nm,Zeta电位为(8.35±3.64)mV。BCEC对AP-LP脂质体的摄取率是普通脂质体的4.1倍,差异有统计学意义(P<0.05);AP-LP的透过血脑屏障能力是普通脂质体的3.6倍,两者比较差异有统计学意义(P<0.05)。结论 AP-LP制备方法简便易行,Angiopep-2修饰脂质体后,脂质体的血脑屏障穿透力增加,靶向性增加,是一种潜在高效的脑部靶向给药系统。

Objective To construct angiopep-2 modified liposome and evaluate its delivery capability into brain. Methods angiopep-2 liposome(AP-LP) was prepared by thin film dispersion method. Physical and chemical characteristics were studied. In the primary culture of BCEC cells, the uptake efficiency of AP-LP by BCEC cells was studied by quantitative cell uptake assay. In vivo study of AP-LP Crossing blood brain barrier was also investigated.Results The AP-LP diameter was(125.0 ± 15.5) nm, and the Zeta potential was(8.35 ± 3.64) mV. According to in vitro cell uptake experiments, the efficiency of AP-LP uptake by BCEC cells is 4.1 times of ordinary liposomes(P < 0.01). Capability of crossing the blood-brain barrier efficiency of AP-LP was 3.6 times of ordinary liposomes(P < 0.01). Conclusions AP-LP exerts increased capability of crossing blood brain barrier and may be a promising brain targeted drug delivery system.