Preparation and Antitumor Activities of Poly(polyethylene glycol methacrylate-co-methacryloyloxymethyl-5-fluorouracil) Prodrug

Suk Hyung Cho; Kong Soo Kim

Macromolecular Research, Vol.11, No.5, 317-321, October, 2003

Suk Hyung Cho^†, and Kong Soo Kim¹

Division of High-Tech Material and Eectronics, Hyejeon College, Hongsung-eup 350-800, Korea
¹Divison of Chemical Engineering, Chungbuk National University, CheongJu 360-763, Korea

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In order to prepare a prodrug, poly(polyethylene glycol ethacrylate-co-methacryloyloxymethyl-5-fluorouracil) (poly(PEGM-co-MAOFU)) prodrug particles were prepared by precipitation polymerization of MAOFU and PEGM in polyacrylic acid solution. The size of prodrug particles were 0.2-0.35 μm. The antitumor activity of prodrugs against sarcoma-180 tumor cell in mice was demonstrated and the polymer particles themselves showed low toxicity and good biocompatibility when they were administrated into mice.

Keywords:antitumor activity;poly(PEGM-co-MAOFU);prodrug;5-fluorouracil

[References]

Ahmad S, Ozaki S, Nagase T, Ligo M, Hoshi A, Chem. Pharm. Bull., 35, 4137 (1987)
Hasida M, Sato A, Kojima T, Muranishi S, Sezaki H, Tanigawa N, Satomura K, Hikasan Y, Jpn. J. Cancer Res., 72, 226 (1981)
Onishi H, Gawaguchi T, Nagai T, Chem. Pharm. Bull., 35, 3370 (1987)
Ouchi T, Yuyama H, J. Macromol. Sci.-Chem., A24, 1011 (1987)
Yang T, Zhno R, Polym. J., 22, 572 (1990)
Akashi M, Miyauchi N, Morita N, Minota T, J. Bioact. Compat. Polym., 2, 232 (1987)
Ozaki S, Watanabe Y, Hoshico T, Nagase T, Ogasawara T, Furukawa H, Uemura A, Ishikawa K, Mori M, Iigo M, Tokuzen R, Chem. Pharm. Bull., 34, 150 (1986)
Cho SH, Kim KS, Kang JK, Cho BH, Polym.(Korea), 18(5), 877 (1994)
Yong F, Zhuo R, Polym. J., 22, 572 (1990)
Tusukuda Y, Okawa K, Hibi N, Cancer Res., 47, 4293 (1987)
Ozaki S, Ohnishi J, Watanabe Y, Nohda T, Nagase T, Akiyama T, Uehara N, Hoshi A, Polym. J., 19, 955 (1987)
Kita Y, Imaki Y, Takemoto K, J. Polym. Sci. A: Polym. Chem., 18, 427 (1981)
Endo N, Umemoro N, Koto Y, Hara T, J. Immunol. Methods, 101, 253 (1987)
Ozaki S, Ohnishi J, Akiyama T, Nagase T, Uehara N, Hoshi A, Polym. J., 22, 689 (1990)
Yokoyama M, Miyauchi M, Yamada N, Okano T, Sakurai Y, Kataoka K, Cancer Res., 50, 1695 (1990)
Cho SH, Kim KS, Macromol. Res., in press (2003)
Gawaguchi T, Tsugane A, Higashide K, J. Pharm. Sci., 81, 508 (1992)
Sbarra AJ, Shirley W, Bardowil WA, Nature, 194, 255 (1962)
Duncan R, Kopecek J, Adv. Polym. Sci., 57, 51 (1984)

[Referenced By]

[1] Ahmad S, Ozaki S, Nagase T, Ligo M, Hoshi A, Chem. Pharm. Bull., 35, 4137 (1987)

[2] Hasida M, Sato A, Kojima T, Muranishi S, Sezaki H, Tanigawa N, Satomura K, Hikasan Y, Jpn. J. Cancer Res., 72, 226 (1981)

[3] Onishi H, Gawaguchi T, Nagai T, Chem. Pharm. Bull., 35, 3370 (1987)

[4] Ouchi T, Yuyama H, J. Macromol. Sci.-Chem., A24, 1011 (1987)

[5] Yang T, Zhno R, Polym. J., 22, 572 (1990)

[6] Akashi M, Miyauchi N, Morita N, Minota T, J. Bioact. Compat. Polym., 2, 232 (1987)

[7] Ozaki S, Watanabe Y, Hoshico T, Nagase T, Ogasawara T, Furukawa H, Uemura A, Ishikawa K, Mori M, Iigo M, Tokuzen R, Chem. Pharm. Bull., 34, 150 (1986)

[8] Cho SH, Kim KS, Kang JK, Cho BH, Polym.(Korea), 18(5), 877 (1994)

[9] Yong F, Zhuo R, Polym. J., 22, 572 (1990)

[10] Tusukuda Y, Okawa K, Hibi N, Cancer Res., 47, 4293 (1987)

[11] Ozaki S, Ohnishi J, Watanabe Y, Nohda T, Nagase T, Akiyama T, Uehara N, Hoshi A, Polym. J., 19, 955 (1987)

[12] Kita Y, Imaki Y, Takemoto K, J. Polym. Sci. A: Polym. Chem., 18, 427 (1981)

[13] Endo N, Umemoro N, Koto Y, Hara T, J. Immunol. Methods, 101, 253 (1987)

[14] Ozaki S, Ohnishi J, Akiyama T, Nagase T, Uehara N, Hoshi A, Polym. J., 22, 689 (1990)

[15] Yokoyama M, Miyauchi M, Yamada N, Okano T, Sakurai Y, Kataoka K, Cancer Res., 50, 1695 (1990)

[16] Cho SH, Kim KS, Macromol. Res., in press (2003)

[17] Gawaguchi T, Tsugane A, Higashide K, J. Pharm. Sci., 81, 508 (1992)

[18] Sbarra AJ, Shirley W, Bardowil WA, Nature, 194, 255 (1962)

[19] Duncan R, Kopecek J, Adv. Polym. Sci., 57, 51 (1984)