肝动脉栓塞用吡柔比星-碘油微乳的组方筛选和细胞毒作用评价.pdfVIP

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 1,2 1 1 1 2 1* 杨蕾 ，刘韬 ，陈倩超，潘莹，叶丽卡，黄红兵 （1.华南肿瘤学国家重点实验室,中山大学附属肿瘤医院,广东广州 510060； 2.广州医学院第二附属医院，广东广州， 510260） 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。 关键词：吡柔比星 碘化油 微乳 伪三元相图 稳定性 毒性作用 Preparation and Research on the Anti-Tumor Activity of Pirarubicin- Lipiodol Microemulsion for Transcatheter Arterial Chemoembolization 1,2 1 1 1 2 1* YANG Lei , LIU Tao , CHEN Qian-chao , PAN Ying , YE Li-ka , HUANG Hong-bing (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) 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-L