VEGFR Ⅱ介导靶向微泡显像剂的制备及体外肿瘤靶向性实验研究  

Preparation of VEGFR Ⅱ-mediated Targeted Microbubble Image Agent and its Cancer Targeting Ability in vitro

作　　者：陈颖[1] 

机构地区：[1]江苏大学附属医院药剂科,江苏镇江212001

出　　处：《中国药师》2017年第1期73-76,共4页China Pharmacist

基　　金：江苏大学临床医学专项基金项目(编号:JDLCZX017)

摘　　要：目的:制备血管内皮生长因子受体Ⅱ(VEGFRⅡ)介导的靶向六氟化硫微泡显像剂,并评价其对乳腺癌细胞MCF-7的靶向性。方法:采用薄膜分散-超声法制备六氟化硫微泡显像剂,以粒径分布为评价指标,通过Box-Behnken效应面法优化六氟化硫微泡显像剂的处方,采用吸附法制备VEGFRⅡ介导靶向微泡显像剂,并对VEGFRⅡ介导靶向微泡显像剂的表观形态、粒径分布、Zeta电位进行表征;用免疫荧光法检测VEGFRⅡ介导靶向微泡显像剂的靶向作用。结果:VEGFRⅡ介导靶向微泡显像剂的平均粒径为(3.81±0.32)μm,多聚分散系数为0.261±0.037,Zeta电位为(-25.7±2.8)m V;透射电镜观察其大小比较均匀,呈规则球形或类球形分布;免疫荧光实验结果显示VEGFRⅡ介导靶向微泡显像剂在体外能与乳腺癌细胞MCF-7特异性结合。结论:通过吸附法可成功制备VEGFRⅡ介导靶向微泡显像剂,在体外具有较强的寻靶能力。Objective： To prepare vascular endothelial growth factor receptor Ⅱ （VEGFR Ⅱ ）-mediated targeted sulphur hexafluo- ride microbubble image agent and evaluate its targeting ability in human breast cancer MCF-7 in vitro. Methods： The sulphur hexafluo- ride microbubble image agent was prepared by a membrane dispersion-ultrasonic method and optimized by Box-Behnken design using design-expert 8.0.6 software. VEGFR Ⅱ -mediated targeted microbubble image agent was prepared by an absorption method. VEGFR If-mediated targeted microbubble image agent was characterized by the morphology, particle size distribution and zeta potential. The targeting ability of the image agent in human breast cancer MCF-7 in vitro was detected by an immunofluorescent assay. Results： The particle size, polydispersion index and zeta potential of VEGFR lI -mediated targeted microbubble image agent was （3.81 ± 0.32） μm, 0.261± 0.037 and （ -25.7 ± 2.8） mV, respectively. The microbubbles were small and spherical with smooth surface as seen under a transmission electron microscope. VEGFR Ⅱ -mediated targeted microbubble image agent could combine with human breast cancer MCF-7 specifically in vitro. Conclusion： The absorption preparation technology of the targeted microbubble image agent is feasible, and the microbubble image agent has strong and especial targeting function in vitro.

关 键 词：血管内皮生长因子受体Ⅱ 靶向微泡显像剂 薄膜分散-超声法 免疫荧光法 

分 类 号：R944.99[医药卫生—药剂学] R965.1[医药卫生—药学]