载阿帕替尼纳米胶束对脐静脉内皮细胞的抑制作用研究

发布时间：2018-08-23 19:01

【摘要】：目的:探讨载阿帕替尼(apatinib)纳米胶束对脐静脉内皮细胞(HUVECs)的抑制作用及其释放规律与安全性。方法:分别用紫外-吸收法和溶血实验检测载apatinib纳米胶束的释放率与使用安全性,然后分别用CCK-8实验、迁移实验、体外小管形成实验观察载apatinib纳米胶束对HUVECs的抑制作用。结果:载apatinib纳米胶束有短暂的突释效应(2 h达20.5%),随后呈缓慢释放(72 h达62.9%),其溶血实验阴性。载apatinib纳米胶束与单纯apatinib均能明显抑制HUVECs的增殖,并呈浓度与时间依赖性(均P0.05);48 h内载apatinib纳米胶束对HUVECs的抑制率小于单纯apatinib组(48 h IC50:1.385μmol/L vs.0.768μmol/L,P=0.012),但随着时间延长至72 h,载apatinib纳米胶束的抑制率超过单纯apatinib(63.34%vs.59.70%,P=0.005)。载apatinib纳米胶束与单纯apatinib均能明显抑制HUVECs的迁移及小管形成,并呈浓度与释放时间依赖性,且体外释放3 d的载apatinib纳米胶束对HUVECs迁移及成管的抑制超过单纯apatinib(均P0.05)。结论:载apatinib纳米胶束具备良好的安全性及缓释性,对apatinib进行纳米包载可增强apatinib对HUVECs的抑制作用并延长apatinib的作用时间窗。
[Abstract]:Aim: to investigate the inhibitory effect of apatinib (apatinib) nanoparticles on (HUVECs) in umbilical vein endothelial cells (HUVEC) and its release regularity and safety. Methods: the release rate and safety of apatinib loaded nano-micelles were detected by UV-absorption and hemolysis methods respectively. Then the inhibition effect of apatinib nanoparticles on HUVECs was observed by CCK-8 experiment migration experiment and tubule formation experiment in vitro. Results: the apatinib nanoparticles showed a transient release effect (20. 5% at 2 h), followed by slow release (62. 9% at 72 h). The hemolysis test was negative. Both apatinib loaded nano-micelles and apatinib alone could significantly inhibit the proliferation of HUVECs. The inhibition rate of apatinib nanoparticles on HUVECs was lower than that of apatinib group (48 h IC50:1.385 渭 mol/L vs.0.768 渭 mol/L,P=0.012) in a dose-dependent and time-dependent manner (P0.05), but the inhibition rate of apatinib nanoparticles was higher than that of apatinib alone (63.34vs.59.70% P0.005) with the time prolonging to 72 h. Both apatinib loaded nano-micelles and apatinib could inhibit the migration and tubule formation of HUVECs in a dose-dependent manner, and the inhibition of HUVECs migration and tubule formation by apatinib nanoparticles released for 3 days in vitro was higher than that of apatinib alone (P0.05). Conclusion: apatinib nanoparticles have good safety and sustained-release properties. Nano-encapsulation of apatinib can enhance the inhibitory effect of apatinib on HUVECs and prolong the time window of apatinib.
【作者单位】：上海交通大学医学院附属新华医院普通外科;上海市胆道疾病研究所;华东理工大学材料学院;
【基金】：上海市科委纳米专项基金资助项目(11nm0503700) 新华医院滚动基金资助项目(XHYYGD2015036)
【分类号】：R96

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