摘要
目的探索153Sm-柠檬酸(citrate)-纳米羟基磷灰石(nano-HA)的体内、体外生物学性能。方法采用溶胶-凝胶法合成nano-HA,用电镜和X线衍射鉴定其性能。制备高纯度放射纯度核素153Sm。采用独立变数法,研究153Sm-citrate-nano-HA的最佳标记条件和体外稳定性能,并进行新西兰兔显像,比较nano-HA、153Sm-citrate、153Sm-citrate-nano-HA对肝癌SMMC-7721和乳腺癌MCF-7细胞的体外抑制作用,利用MTT法测细胞生存率。结果nano-HA为针状结晶,径向10~30nm,轴向70~100nm。nano-HA的体外稳定性能好,标记率均在95%以上。153Sm-citrate-nano-HA正常新西兰兔显像对比度较好,骨骼系统显示清晰,肾脏显影,血中放射性下降较快。153Sm-citrate-nano-HA、nano-HA、153Sm-citrate对肝癌SMMC-7721和乳腺癌MCF-7细胞的半抑制率浓度分别是1.89mg/L和0.094mg/L、3.31mg/L和0.52mg/L、4.32mg/L和0.67mg/L;153Sm-citrate-nano-HA对肿瘤生长的抑制率明显高于nano-HA和153Sm-citrate。结论153Sm-citrate-nano-HA骨组织摄取好,对肿瘤细胞有明显抑制作用,有望成为新型的骨肿瘤和骨转移癌的治疗药物。
Objective To investigate the biological character of new agent ass Sm-citrate-nano- Hydroxyapatite （nano-HA） in vitro and in vivo, and to explore a new radiopharmaceutical for the target therapy of bone metastasis cancer. Methods The nano-HA was synthesized by collosol-gelatum method, and evaluated by transmission electron microscopy （TEM） and X-ray diffraction （XRD）. ^153 Sm was produced at a high specific activity and excellent radionuclidic purity, with which nano-HA was labeled by citrate transfer ligands in the best environment. By adopting the independent variable method, we also studied the optimally labeled condition and stability of ^153 Sm-citrate-nano-HA in vitro. And ^153 Sm-citrate-nano-HA was injected into normal rabbits for radio scanning performed. The cancer cell SMMC-7721 and MCF-7 cell lines were divided into two groups, and treated with nano-HA, ^153 Sm-citrate and ^153 Sm-citrate-nano-HA in vitro respectively, of which the cell survival rate was measured by MTT methods. Results Through the detections of TEM, XRD showed that nano-HA consisted of needle-like microcrystals. The label rate of ^153 Sm-citrate-nano-HA was more than 95%, and extremely stable in vitro. The radio scanning of normal rabbits showed the skeletal system to be clear, and other systems, for example liver, spleen and kidney, could also be seen. The cell culture experiments in vitro indicated that ^153 Sm-citrate-nano-HA strongly inhibited the proliferation of SMMC-7721 and MCF-7 cells. ^153 Sm-citrate- nano-HA＇s half effective inhibition concentrations were 1.89 mg/L and 0. 094 mg/L respectively; nano-HA＇s half effective inhibition concentrations were 3.31 mg/L and 0. 52 mg/L respectively; ^153 Sm-citrate＇s half effective inhibition concentrations were 4. 32 mg/L and 0. 67 mg/L respectively. Conclusions is3 Sm-citrate-nano-HA shows fine biological properties, and is well worth for further researched and prepared as a promising potential radiopharmaceutical in nuclidic treatment for cancer bone metastases.
出处
《四川大学学报（医学版）》
CAS
CSCD
北大核心
2007年第6期1017-1020,共4页
Journal of Sichuan University(Medical Sciences)
基金
四川省科技厅基金(04yY029-075-2)资助
