Abstract
We developed a novel w/o/w emulsion formulation containing medium-chain triglyceride (MCT) as an oily phase and lomeron 300 as an aqueous phase with functions of embolizing and sustaining drug-release in trans-catheter arterial embolization (TAE) therapy for hepatocellular carcinoma. The various formulations with various kinds of surfactants were applied to the MCT w/o/w emulsion to improve its stability. The most stable w/o/w emulsion was obtained when the mixture of HCO-10 and CO-3 (1 : 1) of 3% in oily phase and HCO-60 of 5% in aqueous phase were formulated. The stability of emulsion was also evaluated by a drug release test with Spin-Biodialyser™ Double-sided for the emulsions encapsulating epirubicin hydrochloride (EPI), doxorubicin hydrochloride (DOX) or Evans blue in an inner aqueous phase. The drug release profiles suggested the sustained drug release property of the emulsions. When normal rats were treated with the hepatic arterial injection of the MCT w/o/w emulsion encapsulating EPI, there was non dysfunction trans aminase of GOT and GPT in normal liver. The increased drug retention in liver after the arterial administration of EPI in a w/o/w emulsion form in rats bearing a hepatic tumor revealed the usefulness of this device for the drug targeting to the hepatic tumor.
