载雷公藤内酯醇靶向超声微泡的制备及对乳腺癌细胞增殖抑制的初步研究  

Preparation of triptolide-loaded ultrasound-targeted microbubbles and preliminary study on proliferation inhibition of breast cancer cells

作　　者：陈子合 黄健 黄春鑫 刘慧临 CHEN Zi-he;HUANG Jian;HUANG Chun-xin(School of Medical Technology,Qiqihar Medical University,Qiqihar 161003,China)

机构地区：[1]齐齐哈尔医学院医学技术学院,161003 [2]齐齐哈尔医学院附属第二医院超声科,161006

出　　处：《中国实用医药》2022年第25期186-190,共5页China Practical Medicine

基　　金：黑龙江省卫生健康委科技计划(项目编号:20210202080380)。

摘　　要：目的制备一款协载雷公藤内酯醇靶向于叶酸受体的超声微泡,评价其表征并对叶酸受体高表达人乳腺癌MCF-7细胞的治疗效果进行初步研究。方法薄膜水化法制备叶酸修饰载雷公藤内酯醇靶向超声微泡(FA-TLUM)。采用动态光散射法检测水合粒径和Zeta电位;紫外分光光度法进行载药量和包封率的测定;倒置荧光显微镜观察微泡表面叶酸偶联情况以及体外寻靶能力;CCK-8法检测细胞毒性。结果FA-TLUM水动力尺寸(1.36±0.03)μm,Zeta电位(-16.55±0.36)mV;载药量(10.85±0.48)%,包封率(75.94±3.36)%;微泡表面可见明显绿色荧光分布;体外寻靶实验显示,细胞表面可见大量微泡聚集;与其他组相比,FA-TLUM联合超声组对MCF-7细胞的增殖抑制作用更强,差异具有统计学意义(P<0.05)。结论成功制备出FA-TLUM且FA-TLUM联合超声靶向破碎技术能够增强对MCF-7细胞的增殖抑制作用,因此有望为临床治疗乳腺癌提供新的方法和思路。Objective To prepare an ultrasonic microbubble co-loaded with ryanodine lactone alcohol targeting the folate receptor,evaluate its characterization and perform a preliminary study on the therapeutic effect of folate receptor high expression human breast cancer MCF-7 cells.Methods Folic acid-modified triptolideloaded ultrasound-targeted microbubbles(FA-TLUM)were prepared by thin film hydration method;the hydrated particle size and Zeta potential were detected by dynamic light scattering;the drug loading and encapsulation efficiency were determined by UV spectrophotometry;the coupling of folic acid on the surface of microbubbles and the targeting ability in vitro were observed by inverted fluorescence microscope;the cytotoxicity was detected by CCK-8 assay.Results The hydrodynamic size of FA-TLUM was(1.36±0.03)μm,and the zeta potential was(-16.55±0.36)mV;the drug loading was(10.85±0.48)%,and the encapsulation rate was(75.94±3.36)%;A clear green fluorescence distribution was visible on the surface of microvesicles.;in vitro targeting experiments showed that a large number of microbubbles aggregated on the cell surface;compared with other groups,the proliferation of MCF-7 cells was more inhibited by FA-TLUM combined with ultrasound.Compared with other groups,the proliferation of MCF-7 cells was inhibited by FA-TLUM combined with ultrasound,and the difference was statistically significant(P<0.05).Conclusion FA-TLUM is successfully prepared,and FA-TLUM combined with ultrasound-targeted fragmentation technology could enhance the inhibitory effect on the proliferation of MCF-7 cells,so it is expected to provide new methods and ideas for clinical treatment of breast cancer.

关 键 词：雷公藤内酯醇 乳腺癌 超声微泡 叶酸 

分 类 号：R737.9[医药卫生—肿瘤]