Anticancer Activity of Polyunsaturated Fatty Acid Emulsion Stabilized by Hydrophobized Polysaccharide

An oil-in-water emulsion of selectively cytotoxic ±-linolenic acid (ALA, C18:3ω3) was stabilized with cholesterol-bearing pullulan (CHP-55-2.1), and the in vivo anticancer effect of the O/W-emulsion was investigated. The O/W-emulsion was prepared by ultrasonication of a mixture of CHP and ALA in the presence or absence of trioctanoylglyceride (TriC8). The colloidal stabil ity of the CHP/ALA-emulsion was largely improved by adding TriC8. Intraperi toneal injection of the CHP/ALA-emulsion effectively prolonged the survival time of C3H/He mice which received an intraperitoneal transplantation of MM46 mammary tumor cells. The growth of these tumor cells subcutaneously transplanted in C3H/He mice was also significantly suppressed without any loss of body weight when CHP/ALA/TriC8-emulsion was intravenously injected. By using this colloidally stable O/W emulsion, it is possible to systemically ad minister a lipophilic liquid drug.