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作 者:王硕[1,2] 李永盛[1,2] 边睿[1,2] 戴一星 郎美东[3] 刘颖斌[1,2] 施伟斌[1,2]
机构地区:[1]上海交通大学医学院附属新华医院普通外科,上海200092 [2]上海市胆道疾病研究所,上海200092 [3]华东理工大学材料学院,上海200237
出 处:《中国普通外科杂志》2017年第5期597-606,共10页China Journal of General Surgery
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)
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P<0.05);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P<0.05)。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。Objective: To investigate the inhibitory effect of apatinib-loaded nanomicelles on human umbilical vein endothelial cells (HUVECs) as well as its release pattern and safety. Methods: The release rate and use safety of apatinib-loaded nanomicelles was determined by ultraviolet spectrophotometry method and hemolytic assay, respectively. And then, the inhibitory effect of apatinib-loaded nanomicelles on HUVECs was tested by CCK-8 assa)5 migration assay and tube formation assa)5 respectively. Results: The apatinib-loaded nanomicelles showed a transient immediate-release (2 h release rate reached 20.5%) and then a slow release (72 h release rate was 62.9%), and the results of hemolytic assay were negative. The proliferation of HUVECs was significantly inhibited by either apatinib-loaded nanomicelles or free apatinib in a concentration- and time-dependent manner (all P〈0.0S); the inhibition rate of apatinib-loaded nanomicelles on HUVECs was lower than those of free apatinib within 48 h (48 h ICs0:1.385 ~mol/L vs. 0.768 ~tmol/L, P=0.012), but it surpassed that of free apatinib with time up to 72 h (63.34% vs. 59.70%, P=0.005). The migration and tube formation of HUVECs were significantly suppressed by both apatinib-loaded nanomicelles and free apatinib in a concentration- and releasing time-dependent manner, and the inhibitory effects of apatinib-loaded nanomicelles with 3-d release on migration and tube formation of HUVECs were significantly greater than those of free apatinib (both P〈0.05). Conclusion: The apatinib-loaded nanomicelles have good safety and sustained release property. Nanoencapsulation can enhance the inhibitory effect of apatinib on HUVECs and extend its action time window.
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