Size of Lipid Microdroplets Effects Results of Hepatic Arterial Chemotherapy with an Anticancer Agent in Water-in-Oil-in-Water Emulsion to Hepatocellular Carcinoma

We have initially prepared a new drug delivery system for hepatocellular carcinoma (HCC). Using sonication and a detergent, iodinated poppy seed oil (IPSO) can be mixed with an aqueous solution of epirubicin to make a water-in-oil emulsion. The water-in-oil emulsion is further passed through a microporous glass membrane and split into saline to make a long-term inseparable water-in-oil-in-water emulsion (W/O/W) that consists of IPSO microdroplets. To investigate the effect of the size of IPSO microdroplets on the efficacy of injection chemotherapy with W/O/W in patients with HCC, 32 HCC patients were randomly assigned and treated with W/O/W of small IPSO microdroplets (30 μm in diameter) containing 60 mg of epirubicin ( n = 16, group A) or W/O/W of large IPSO microdroplets (70 μm) containing the same amounts of epirubicin ( n = 16, group B). Effects were assessed by measuring the percentage of decline of the α-fetoprotein (AFP) level in a week from the AFP level immediately before the treatment. The decline was significantly larger in group B (50.5 ± 19.8, mean ± S.D.) compared with group A (18.9 ± 33.1; p < .005). The size of IPSO microdroplets injected into the hepatic artery determines the decrease of serum AFP levels of the patients with HCC.