Application of the double emulsion prepared by membrane-emulsification technique for drug delivery system

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We newly prepared a water-in-oil-in-water emulsion (W/O/W) for hepatic arterial injection chemotherapy for hepatocellular carcinoma (HCC). The emulsion consisted of iodinated poppy-seed oil (IPSO) microdroplets enclosing numerous vesicles of aqueous solution dissolving epirubicin. Two kinds of surfactant such as polyglycerol esters of polycondensed fatty acids of castor oil and polyoxyethlene 60 stearate (hydrogenated castor oil treated with ethylene oxide, 1 : 60, molar ratio) were used to attain adequate stability of the emulsion : separation of the oil arid water and changes in the size of IPSO microdroplets were not observed at least 40 days when stored in a vial at room temperature. From a series of experiments, it has been revealed that W/O/W which consists of IPSO microdroplets with a diameter of 70 mum and is prepared with 60 mg of epirubicin in total 10 ml of internal and external aqueous phase is applicable in clinical use because of its stability and efficacy. Using the W/O/W, we repeated hepatic arterial injection chemotherapy for 24 patients bearing recurrent HCC which occurred after hepatectomy. No fatal adverse effect originated in oil embolism or due to anticancer agent was encountered. The 3- and 5-year cumulative survival rates from the time of recurrence were 50 and 24%. As for the patients with four or more nodules, the 3-year cumulative survival rate was 50%.