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。
Abstract
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
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Key words
pirarubicin /
lipiodol /
microemulsion /
pseudo-ternary phase diagram /
stability
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杨蕾 刘韬 陈倩超 潘莹 叶丽卡 黄红兵.
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[J]. 中国药学杂志, 2010, 45(23): 1837-1841
YNG Lei;LIU To;CHEN Qin-cho;PN Ying;YE Li-k;HUNG Hong-ing.
Preparation of Pirarubicin-Lipiodol Microemulsion for Transcatheter Arterial Chemoembolization and Its Anti-Tumor Activity[J]. Chinese Pharmaceutical Journal, 2010, 45(23): 1837-1841
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参考文献
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脚注
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