Formulation of w/o/w lipiodol emulsion encapsulating epirubicin hydrochloride for the transcatheler arterial embolization therapy for hepatocellular carcinoma

Abstract

Lipiodol (LPD) is widely used as an oily contrast medium and an embolizing material for transcathether arterial embolization (TAE) therapy for hepatocellular carcinoma. Most of the anticancer drug is water-soluble such as epirubicin hydrochloride (EPI), so that it is used as an emulsion form with LPD. A w/o/w emulsion of LPD encapsulating the drug is a useful drug carrier to accumulate the water-soluble drug (EPI) in the carcinoma. We developed the LPD w/o/w emulsion encapsulating EPI by using a two-step pumping emulsification procedure. This procedure is easily carried out even in operation under sterilized condition. It was found that a large amount of the aqueous drug solution was encapsulated in the resultant w/o/w emulsion and the drug release profile from emulsion showed a sustained release pattern. The hemolysis induced by the w/o/w emulsion was much depressed compared to the EPI solution or the conventional o/w emulsion used for the TAE therapy. Therefore, the present w/o/w emulsion prepared by us is a desirable formulation for the TAE therapy and now under investigating with human subject.