肝动脉栓塞用吡柔比星-碘油微乳的组方筛选及细胞毒作用评价  

Preparation of Pirarubicin-Lipiodol Microemulsion for Transcatheter Arterial Chemoembolization and Its Anti-Tumor Activity

作　　者：杨蕾[1,2] 刘韬[1] 陈倩超[1] 潘莹[1] 叶丽卡[2] 黄红兵[1] 

机构地区：[1]华南肿瘤学国家重点实验室,中山大学附属肿瘤医院,广州510060 [2]广州医学院第二附属医院,广州510260

出　　处：《中国药学杂志》2010年第23期1837-1841,共5页Chinese Pharmaceutical Journal

基　　金：吴孟超医学科技基金资助项目(GZL-2007051)

摘　　要：目的研制肝动脉栓塞用吡柔比星-碘油微乳并对其体外抗肿瘤活性进行研究。方法采用伪三元相图法研究不同表面活性剂、助表面活性剂和Km值形成微乳的能力及区域,优选微乳处方,制备吡柔比星-碘油微乳,并对微乳的物理性质、稳定性进行研究;采用MTT法对吡柔比星-碘油微乳体外抗肿瘤活性进行考察。结果碘化油/大豆磷脂/无水乙醇/水形成的微乳粒径小、黏度低,初步稳定性实验表明,4℃下放置药物含量和粒径均无显著变化。MTT实验结果表明,吡柔比星-碘油微乳对人肝癌细胞有明显抑制作用,空白微乳对肝癌细胞HepG-2抑制作用弱。结论吡柔比星-碘油微乳制备简单,工艺重复性良好,质量稳定,体外抗肿瘤活性较强,为肝动脉栓塞给药剂型的改进提供了依据。OBJECTIVE To study the preparation of pirarubicin-lipiodol microemulsion for transcatheter arterial chemoembolization and its anti-tumor activity in-vitro.METHODS Pseudo-ternary phase diagrams developed by water titration method were used to select the suitable surfactant,co-surfactantand and their proportion.Physico-chemical property and stability of pirarubicin-lipiodol microemulsion were evaluated.MTT method was used to detect the toxicity of THP microemulsion against human hepatoma cell（HepG-2）.RESULTS Pirarubicin-lipiodol microemulsion prepared with Lipiodol/Lipoid S100/ ethyl alcohol/water was with small droplet size and low viscosity.The preliminary stability test showed that the drug content and droplet size of pirarubicin-lipiodol microemulsion were stable at 4 ℃.MTT assay showed that pirarubicin-lipiodol microemulsion apparently inhibited the proliferation of HepG-2 cell.Blank microemulsion had little cytotoxicity on HepG-2 cell.CONCLUSION The pirarubicin-lipiodol microemulsion is easy to prepare,its quality is stable,and it shows a high anti-tumor activity in vitro,which provide the basis for the optimizing of the dosage form for TACE.

关 键 词：吡柔比星 碘化油 微乳 伪三元相图 稳定性 毒性作用 

分 类 号：R944[医药卫生—药剂学]