白蛋白索拉非尼纳米粒的制备与体外抗肝肿瘤活性评价  

Preparation of sorafenib loaded human serum albumin nanoparticles and evaluation of their anti⁃hepatic tumor activity in vitro

作　　者：高文慧 吴锦俊 简晓顺 贾小婷[3] 李靖 GAO Wenhui;WU Jinjun;JIAN Xiaoshun;JIA Xiaoting;LI Jing(Department of Pharmacy,Affiliated Cancer Hospital&Institute of Guangzhou Medical University,Guangzhou 510095,China;不详)

机构地区：[1]广州医科大学附属肿瘤医院药学部,广州510095 [2]广州中医药大学国际中医药转化医学研究所,广州510006 [3]广州医科大学肿瘤研究所,广州510095 [4]广州医科大学附属肿瘤医院泌尿外科,广州510095

出　　处：《实用医学杂志》2021年第11期1392-1396,共5页The Journal of Practical Medicine

基　　金：广东省自然科学基金(编号:2017A03031046);广州市恶性肿瘤治疗转化医学重点实验室建设项目(编号:2014SY000014)。

摘　　要：目的制备人血白蛋白包被的索拉非尼纳米粒(HSA⁃SRF⁃NPs),并评价其体外抗肝肿瘤活性。方法化学交联法制备HSA⁃SRF⁃NPs,采用粒度分析仪和透射电镜对其进行表征,并计算载药量和包封率。荧光显微镜观察纳米粒在BEL⁃7402肝癌细胞内的蓄积,IncuCyte ZOOM系统评价纳米粒对BEL⁃7402细胞的增殖抑制作用,流式细胞技术和Western blotting法考察HSA⁃SRF⁃NPs对BEL⁃7402细胞的促凋亡能力。结果HSA⁃SRF⁃NPs的水合粒径为(75.8±2.6)nm,Zeta电位为⁃(19.00±1.02)mV,载药量和包封率分别为(4.23±0.03)%和(92.52±2.40)%,能在BEL⁃7402细胞内蓄积,对BEL⁃7402细胞的增殖抑制作用和促凋亡作用显著优于索拉非尼。结论HSA⁃SRF⁃NPs制剂性质良好,能显著提高索拉非尼的抗肝肿瘤活性,具有潜在的临床应用前景。Objective Human serum albumin⁃sorafenib nanoparticles(HSA⁃SRF⁃NPs)were prepared and then their anti⁃hepatic tumor activity was evaluated in vitro.Methods HSA⁃SRF⁃NPs were prepared by chem⁃ical cross⁃linking method,and their characterization was studied by a laser granulometer and a transmission elec⁃tron microscope.The drug loading volume and encapsulation rate were calculated.Accumulation of nanoparticles in BEL⁃7402 cells was observed by a fluorescence microscope,the proliferation inhibition of BEL⁃7402 cells by nanoparticles was evaluated by the IncuCyte ZOOM system,and the proapoptotic effect of HSA⁃SRF⁃NPs on BEL⁃7402 cells was detected by flow cytometry and Western blotting.Results The particle size of HSA⁃SRF⁃NPs was(75.8±2.6)nm and the Zeta potential was(-19.00±1.02)mV,and the drug loading volume and encapsulation rate were(4.23±0.03)%and(92.52±2.40)%,respectively.HSA⁃SRF⁃NPs could accumulate in BEL⁃7402 cells,the proliferation inhibition and proapoptotic effect of HSA⁃SRF⁃NPs were significantly stronger than those of sorafenib.Conclusions HSA⁃SRF⁃NPs possess better properties,which can significantly improve the anti⁃hepatic tumor activity of sorafenib.They have potential prospect of clinical applications.

关 键 词：索拉非尼 人血白蛋白 纳米粒 肝癌 

分 类 号：R944.9[医药卫生—药剂学]