화학공학소재연구정보센터
Journal of the Korean Industrial and Engineering Chemistry, Vol.11, No.2, 133-137, April, 2000
생분해성 고분자 마이크로겔 Microsphere의 약물방출 특성 및 항암효과
Drug Release Behaviors and Antitumor Effects of The Biodegradable Microgel Microspheres
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초록
폴리카프로락톤을 기초로 하여 용액증합방법으로 microgel을 합성하고, 용매증발법으로 모델 약물인 BSA와 5-fluorouracil (5-FU)이 담지된 microsphere를 제조하였다. Microgel을 제조함에 있어 가교제의 양과 pH 및 BSA와 5-FU의 담지량에 따른 약물의 방출속도를 in vitro 실험한 결과, BSA를 함유하는 microsphere가 5-FU를 함유하는 경우 보다 약물이 훨씬 빨라 방출되었다. 또한, 5-FU를 담지한 microsphere를 saecoma-180 asites 종양세포가 이식된 마우스에 투여하여 실험한 결과, 투여량에 따라 암종양세포에 대하여 현저한 연명효과를 나타내었다.
Biodegradable microsphere containing Bovine Serum Albumin (BSA) or 5-fluorouracil (5-FU) was prepared with the microgel based on poly(caprolactone diol) by a modified solvent evaporation method. The effects of the crosslinking degree of microgel, pH, the concentration of BSA and 5-FU of medium on the release properties were investigated in vitro. Drug release rate from the micorsphere containing BSA was relatively rapid than the microsphere containing 5-FU. Antitumor activities were tested against Sarcoma-180 asites in vivo. The rate of medium survival of treated mice to that of control mice was depend on injected amount of the microsphere containing 5-FU.
  1. Funke W, Walthe K, Polym. J. Jpn., 17, 179 (1985)
  2. Funke W, Brit. Polym. J., 21, 107 (1989)
  3. Kleiner B, Funke W, Makromol. Chem. Rapid Commun., 10, 345 (1989) 
  4. Graham NB, Mao J, UK Patent, GB 9506946-4 (1995)
  5. Graham NB, Brit. Polym. J., 10, 260 (1978)
  6. Pitt CG, Hendren RW, Schindler A, Woodward SC, J. Control. Release, 1, 3 (1984) 
  7. Nishioka Y, Kyotani S, Masui H, Okamura M, Miyazaki M, Okazaki K, Ohnishi S, Yamamoto Y, Ito K, Chem. Pharm. Bull., 37(11), 3074 (1989)
  8. Seki T, Kawaguchi T, Endoh H, Ishikawa K, Juni K, Nakano M, J. Pharm. Sci., 79(11), 985 (1990) 
  9. Hora MS, Rana RK, Nunberg JH, Tice TR, Gilley RM, Hudson ME, Pharm. Res., 7, 1190 (1990) 
  10. Jalil R, Nixon JR, J. Microencapsul., 7, 297 (1990)
  11. Ruiz JM, Busnel JP, Benoit JP, Pharm. Res., 7, 928 (1990) 
  12. Ogawa Y, Yamamoto M, Okada H, Yashiki T, Shimamoto T, Chem. Pharm. Bull., 36, 1095 (1988)
  13. O'Hagan DT, Jeffery H, Davis SS, Int. J. Pharm., 103, 37 (1994) 
  14. Alonso MJ, Cohen S, Park TW, Siber GR, Langer R, Pharm. Res., 10, 945 (1993) 
  15. Cohen S, Yoshioka T, Lucarelli M, Hwang LH, Langer R, Pharm. Res., 8(6), 713 (1991) 
  16. Kim KS, Graham NB, J. Ind. Eng. Chem., 4(3), 221 (1998) 
  17. Kim KS, Kang SH, Kim JM, J. Korean Ind. Eng. Chem., 9(4), 591 (1998)