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Journal of Bioactive and Compatible Polymers
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Anticancer Activity of Polyunsaturated Fatty Acid Emulsion Stabilized by Hydrophobized Polysaccharide

Hiroki Fukui

Laboratory of Materials Science of Polymers Department of Polymer Chemistry Kyoto University Sakyo-ku, Yoshida Hommachi, Kyoto 606, Japan

Kazunari Akiyoshi

Laboratory of Materials Science of Polymers Department of Polymer Chemistry Kyoto University Sakyo-ku, Yoshida Hommachi, Kyoto 606, Japan

Toshinori Sato

Laboratory of Materials Science of Polymers Department of Polymer Chemistry Kyoto University Sakyo-ku, Yoshida Hommachi, Kyoto 606, Japan

Junzo Sunamoto

Laboratory of Materials Science of Polymers Department of Polymer Chemistry Kyoto University Sakyo-ku, Yoshida Hommachi, Kyoto 606, Japan

Shigehiko Yamaguchi

Nippon Oil & Fats, Co., Ltd. Tsukuba Research Laboratory Tsukuba 300-26, Japan

Mituhiro Numata

Department of Bioactive Molecules National Institute of Health Shinjuku-ku, Tokyo, Japan

An oil-in-water emulsion of selectively cytotoxic {alpha}-linolenic acid (ALA, C18:3{omega}3) 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.

Journal of Bioactive and Compatible Polymers, Vol. 8, No. 4, 305-316 (1993)
DOI: 10.1177/088391159300800401
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