【作者】 杨蕾； 刘韬； 陈倩超； 潘莹； 叶丽卡； 黄红兵；

【Author】 YANG Lei1,2,LIU Tao1,CHEN Qian-chao1,PAN Ying1,YE Li-ka2,HUANG Hong-bing1(1. State Key Laboratory of Oncology in South China,Tumor Hospital Affiliated to SunYat-Sen University,Guangdong Guangzhou 510060,China; 2.The Second Affiliated Hospital of Guangzhou Medical University,Guangdong Guangzhou 510260,China)

【机构】 华南肿瘤学国家重点实验室中山大学附属肿瘤医院； 广州医学院第二附属医院；

【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、粘度低,初步稳定性实验表明,4°C下放置药物含量和粒径均无显著变化。MTT试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。更多还原

【Abstract】 OBLECTIVE 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, 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 could apparently inhibit 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 shows a high anti-tumor activity in vitro, which provide the basis for the optimizing of the dosage form for TACE.更多还原