Evaluation of acute toxicity of epirubicin hydrochloride-encapsulating w/o/w emulsion administered to rat for the transcatheter embolization therapy for hepatocellular carcinoma

Abstract

The toxicity of lipiodol (LPD) w/o/w emulsions encapsulating epirubicin hydrochloride (FARM) after iv administration to rat was investigated compared to the conventional o/w emulsions used for transcathether arterial embolization (TAE) therapy for hepatocellular carcinoma. Survival time of the rat administered w/o/w emulsion was longer than that of the o/w emulsion. The rats administered o/w emulsion (≥1.5 ml/kg) were deceased within 2 days by pulmonary edema caused by embolism with fine oil droplets. The edema was not found in the lungs of the rats administered w/o/w emulsion. The toxicity of the FARM, ie, size reduction of thymus gland and ulceration in the stomach, was reduced by encapsulating the drug in the w/o/w emulsion. The present w/o/w emulsion prepared by us proved a desirable formulation for the TAE therapy because of reducing toxicities of oil droplets and drug.