Preparation of new lipiodol-emulsion containing water soluble anticancer agent by membrane emulsification technique.

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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.
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