硫酸长春新碱硅壳纳米颗粒制备及性质研究  

Preparation and Characterization of Vincristine Sulfate Loaded Silica Core-Shell Nanoparticles

作　　者：郑翠芳[1,2] 龚萍[2] 郑明彬[2] 张鹏飞[2] 石碧华[2] 刘小平[1] 蔡林涛[2] 

机构地区：[1]武汉理工大学化工学院,湖北武汉430070 [2]中国科学院深圳先进技术研究院生物医学与健康工程研究所,广东深圳518055

出　　处：《时珍国医国药》2011年第5期1050-1052,共3页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(No.20905050);广东省自然科学基金(No.9478922035-X003399);中国博士后科学基金(No.20090450587)

摘　　要：目的制备硫酸长春新碱硅壳纳米颗粒(VCR-SiNPs)并对其相关性质进行研究。方法采用反相微乳液法在盐酸氟化钠催化条件下成功制备包载硫酸长春新碱的硅壳纳米颗粒。以粒径、载药量、包封率为指标,考察催化剂的摩尔比、加药量对VCR-SiNPs的影响;透析法分析药物释放行为;MTT法研究其体外抗癌活性。结果随着盐酸与氟化钠摩尔比的增大VCR-SiNPs的粒径逐渐增大;加药量为2 mg时载药量最高,为(7.26±0.16)%,包封率达(72.6±0.7)%。优化工艺制备的VCR-SiNPs平均粒径为(102.4±1.65)nm,对人乳腺癌细胞MDA-MB-231半数抑制率(IC50)为5.4μmol/L,是游离药物的56.25%。结论制备的VCR-SiNPs可缓释药物,抗癌效果明显优于游离药物。Objective To prepare vincristine sulfate（VCR） loaded silica nanoparticles（VCR-SiNPs）.Methods The modified water in oil microemulsion method was used to study the impact of catalyzer ratio and amount of VCR on nanoparticles＇s size,drug loading efficiency and encapsulation efficiency,dialysis method was used to evaluate the drug release and the cytotoxicity of VCR-SiNPs was investigated by MTT assay.Results The size increased with the catalyzer ratio increasing,when VCR weight in the formulation reached 2 mg,the VCR entrapment efficiency reached（72.6±0.7）% and the drug loading efficiency achieved（7.26±0.16）%.The IC50 value of VCR-SiNPs was 5.4 μM,56.25% as free VCR and encapsulated VCR demonstrated significant stability.Conclusion VCR-SiNPs can make the drug release steadly and slowly.In comparison with free VCR,the thermal toxicity of VCR-SiNPs against the MDA-MB-231 cells is significantly enhanced.

关 键 词：硫酸长春新碱 硅壳 纳米颗粒 缓释 

分 类 号：R944.9[医药卫生—药剂学]