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

摘要:

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。

Abstract:

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?