Development and application of novel w/o/w emulsion for the chemoembolization therapy of hepatocellular carcinoma

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W/o/w emulsion (WOWE) encapsulating water-soluble anticancer agent (epirubicin hydrochloride, EPI) was prepared by two-step amulsification method. Aqueous and oil phases used were nonionic (iohexol) and oily (lipiodol) contract media, respectively. The agents added in inner and outer aqueous phases were polyoxyethylene hydrated caster oil 60 and gelatin, respectively.The WOWE was stable emulsion which could encapsulate large amount of EPI and the viscosity was small. The hemolysis percentage was less than that of the o/w emulsion (OWE) used for transcatheter chemoembolization therapy (TAE) conventionally.The acute toxicities of WOWE and OWE were investigated. The emulsions with and without EPI were administered to the tail vein of rats. The rats administered OWE (*1.5 ml/kg) were deceased within 2 days by pulmonary edema. The rats administered WOWE (*2.0 ml/kg) encapsulating EPI were deceased 7-9 days after administration by the toxicity of EPI.Bleeding and ulcer in the stomach and size reduction of thymus gland were observed in these deceased rats. These pathological damage in the stomach and thymus gland were observed in the rats administered less amounts of OWE than WOWE.This result suggests that the encapsulation of EPI in the WOWE droplets reduced the acute toxicity of EPI.Therefore, the WOWE newly prepared by us was safer than OWE and desirable formulation for TAE.The effectiveness of WOWE is investigated now and the possible clinical application of WOWE is under investigation.