Preparation of new lipiodol-emulsion containing water soluble anticancer agent by membrane emulsification technique.
Preparation of new lipiodol-emulsion containing water soluble anticancer agent by membrane emulsification technique.
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膜乳化技术制备新型水溶性抗癌剂碘油乳剂
DOI：
10.2745/dds.8.59
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发表时间：
1993
影响因子：
--
通讯作者：
T. Setoguchi
中科院分区：
文献类型：
--
作者：
S. Higashi;M. Shimizu;T. Setoguchi
采用可控孔玻璃膜的膜乳化技术，在碘油滴(油)中制备了含有抗癌药物表阿霉素和卡铂的新型水包油乳剂(W/O/W)。表阿霉素(10 Mg)或卡铂(150 Mg)分别溶于5ml 0.58%葡萄糖溶液或15ml 0.75%生理盐水中。每个溶液与含有5wt%的酯交换蓖麻油酸四甘油酯的碘化油混合。对混合物进行超声波处理，形成含有其中一种抗癌剂的亚微米级油包水乳液(W/O)。W/O在54kPa的压力下通过膜进入葡萄糖溶液，形成新的W/O/Ws。膜的平均粒径分别为25μm和8μm，孔径分别为4.2μm和1.4μm。制备后油滴的稳定性保持在40天以上。显微镜观察和激光反射颗粒分析仪对液滴大小的测量证实了这一点。在恒流的5%葡萄糖溶液中用透析法测定表柔比星在外水中的溶解速度，9天后计算为15%。W/O/W将用于肝细胞癌的化疗栓塞术，或一般的靶向化疗。
We prepared new water-in-oil-in-water emulsions (W/O/W), containing water-soluble anti-cancer drugs, epirubicin and carboplation, in the lipiodol droplets(oil) by the membrane emulsification technique with controlled pore glass membrane. Epirubicin(10 mg) or carbopiatin(150 mg)was dissolved in 5 ml of 0.58% glucose solution or 15 ml of 0.75% saline, respectively. Each solution was mixed with lipiodol containing 5 wt% of tetraglycerol esters of interesterified ricinoleic acid. The mixture was sonicated to form a submicron particle sized water-in-oil-emulsion (W/O) containing one of the anticancer agent. W/O was permeated through the membrane at a pressure of 54 kPa into glucose solution forming new W/O/Ws. Mean particle size of the oil droplet was about 25 μm and 8 μm when prepared with 4.2 μm pore sized membrane and 1.4 μm, respectively. Stability of oil droplets was maintained over 40 days after preparations. This was confirmed by microscopic observations and by measurements of droplet size with laser reflection particle analyser. Dissolution rate of epirubicin from the droplet into outer water is measured by dialysis in the constant flow of 5% glucose solution, which was, after 9 days, calculated to be 15%. The W/O/W will be used in the field of chemoembolization for hepatocellular carcinoma, or in general, targeting chemotherapy.