| 摘要: |
| 目的 构建angiopep-2与转铁蛋白共修饰脂质体,并对其跨血脑屏障能力进行评价。方法 制备angiopep-2与转铁蛋白(TF)共修饰脂质体(ANG/TF-LPs),考察其粒径、Zeta电位和血清稳定性等理化特征。通过定量细胞摄取实验考察脑内皮bEnd.3细胞对ANG/TF-LPs的摄取效率。构建血脑屏障体外模型,考察不同脂质体的跨血脑屏障能力。结果 所制备的ANG/TF-LPs粒径为(93.2±13.5) nm, Zeta 电位为(7.55±1.85) mV,且在24 h内具有良好的血清稳定性。体外细胞摄取实验表明,bEnd.3细胞对ANG/TF-LPs的摄取效率分别是TF-LPs、ANG-LPs和LPs的2.9倍、2.4倍和4.8倍,差异具有统计学意义(P<0.01)；ANG/TF-LPs的跨血脑屏障效率分别是TF-LPs、ANG-LPs和LPs的3.1倍、2.9倍和5.4倍,差异具有统计学意义(P<0.01)。结论 ANG/TF-LPs制备工艺简单,经过angiopep-2与转铁蛋白修饰后,脂质体的跨血脑屏障能力显著增强,是一种潜在高效的脑部靶向给药系统。 |
| 关键词: angiopep-2 转铁蛋白 脂质体 脑靶向 血脑屏障 |
| DOI：10.3724/SP.J.1008.2014.01083 |
| 投稿时间：2014-01-01修订日期：2014-05-08 |
| 基金项目: |
|
| Angiopep-2 and transferrin co-modified liposome for targeted drug delivery across the blood-brain barrier |
| DONG Xiang*,CHANG Geng |
(Department of Neurology, The First Affiliated Hospital of Dalian Medical University, Dalian 116011, Liaoning, China
*Corresponding authors) |
| Abstract: |
| Objective To prepare angiopep-2 and transferrin co-modified liposomes (ANG/TF-LPs) and to observe their property of passing the blood-brain barrier (BBB). Methods ANG/TF-LPs were prepared by film-ultrasonic method. The particle size, Zeta potential and stability in fetal bovine serum (FBS) of ANG/TF-LPs were evaluated. The cellular uptake of ANG/TF-LPs by bEnd.3 cells in vitro was observed to evaluate the targeting efficiency. The in vitro BBB model was used to evaluate the ability of liposomes passing the BBB. Results The diameter of the prepared ANG/TF-LPs was (93.2±13.5) nm, the Zeta potential was (7.55±1.85) mV, and they were stable in FBS within 24 h. It was found that the uptake of ANG/TF-LPs by bEnd.3 cells was 2.9, 2.4 and 4.8 folds those of transferrin modified liposomes (TF-LPs), angiopep-2 modified liposomes (ANG-LPs) and liposomes (LPs), respectively (P<0.01). The efficiency of ANG/TF-LPs passing the BBB was 3.1, 2.9 and 5.4 folds those of TF-LPs, ANG-LPs and LPs, respectively (P<0.01). Conclusion The angiopep-2 and transferrin co-modified liposomes are easy to prepare, and the modification can enhance the BBB passing ability, making the prepared liposomes a promising brain drug delivery system. |
| Key words: angiopep-2 transferrin liposomes brain targeting blood-brain barrier |
