5-Fluorouracil 전달을 위한 리포산이 결합된 키토산 공중합체

이선영; 김영진; Sun Young Lee; Young Jin Kim

Polymer(Korea), Vol.36, No.2, 149-154, March, 2012

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5-Fluorouracil 전달을 위한 리포산이 결합된 키토산 공중합체

Lipoic Acid Conjugated Chitosan Copolymer for the Delivery of 5-Fluorouracil

이선영, 김영진 ^†

충남대학교 공과대학 바이오응용화학과

Sun Young Lee, and Young Jin Kim^†

Department of Applied Chemistry and Biological Engineering, Chungnam National University, 220 Gung-dong, Yuseong-gu, Daejeon 305-764, Korea

E-mail:

초록

생체적합성을 가진 키토산과 강력한 항산화제로 알려진 리포산을 합성하여 만든 양친매성 고분자를 이용하여 약물전달시스템으로서의 응용 가능성을 알아보았다. 수용액 상에서 자기조립의 성질을 가지는 양친매성 고분자는 나노입자를 형성하고 이 입자 안에 항암제로 널리 쓰이는 5-fluorouracil을 고체분산법을 이용하여 봉입하였다. 최적의 약물전달체를 얻기 위하여 키토산에 결합된 리포산의 비율을 조절하여 입자크기 및 약물봉입률을 비교하였다. DLS를 이용하여 측정한 나노입자는 약 250 nm 정도의 크기를 가졌고 그 봉입률은 10% 내외로 측정되었다. 42%의 리포산 치환율을 가지는 공중합체가 약물전달체로서 가장 우수한 성능을 보여주었다.

The amphiphilic copolymer by the conjugation of biocompatible chitosan and antioxidant lipoic acid was studied as a drug delivery carrier. The amphiphilic copolymer was self-assembled to form nanoparticles in the aqueous solution. 5-Fluorouracil widely used as an anticancer drug was encapsulated inside the nanoparticles by a solid dispersion method. The degree of branching of lipoic acid on chitosan was controlled to obtain the optimal condition for the drug delivery carrier. The sizes of nanoparticles were about 250 nm by the dynamic light scattering. The encapsulation efficiency of nanoparticles were about 10%. The copolymer with 42% degree of branching showed the best performance as a drug delivery carrier.

Keywords:chitosan;lipoic acid;5-fluorouracil;amphiphilic polymer;drug delivery system.

[References]

Park JH, Saravanakumar G, Kim K, Kwon IC, Adv. Drug Deliv. Rev., 62, 28 (2010)
Kwon IC, Kim K, Kim S, Chung H, Jeong SY, Polym. Sci. Technol., 15(4), 396 (2004)
Kim JH, Kim YS, Park K, Lee S, Nam HY, Min KH, Jo HG, Park JH, Choi K, Jeong SY, Park RW, Kim IS, Kim K, Kwon IC, J. Control. Release., 127, 41 (2008)
Yih TC, Al-Fandi M, J. Cell. Biochem., 97, 1184 (2006)
Mu L, Feng SS, J. Control. Release., 86, 33 (2003)
Maeda H, Wu J, Sawa T, Matsumura Y, Hori K, J.Control. Release., 65, 271 (2000)
Winzenburg G, Schmidt C, Fuchs S, Kissel T, Adv.Drug Deliv. Rev., 56, 1453 (2004)
Wang YS, Liu LR, Jiang Q, Zhang QQ, Eur. Polym. J., 43, 43 (2007)
Agnihotri SA, Mallikarjuna NN, Aminabhavi TM, J. Control. Release., 100, 5 (2004)
Liu ZH, Jiao YP, Wang YF, Zhou CR, Zhang ZY, Adv. Drug Deliv. Rev., 60, 1650 (2008)
Yue W, Yao PJ, Wei YN, Li SQ, Lai F, Liu XM, Food Chem., 108, 1082 (2008)
Zhang Y, Huo MR, Zhou JP, Yu D, Wu YP, Carbohydr. Polym., 77, 231 (2009)
Bustamante J, Lodge JK, Marcocci L, Tritschler HJ, Packer L, Rihn BH, Free Radical Biol. Med., 24, 1023 (1998)
Biewenga GP, Haenen GRMM, Bast A, Gen. Pharmacol., 29, 315 (1997)
Dozio E, Ruscica M, Passaparo L, Dogliotti G, Steffani L, Marthyn P, Pagani A, Demartini G, Esposti D, Fraschini F, Magni P, Eur. J. Pharmacol., 641, 29 (2010)
Park EJ, Kim YJ, Polym.(Korea), 32(6), 544 (2008)
Kwon SK, Kim SW, Kim YJ, Polym.(Korea), 34(6), 501 (2010)

[Related Articles]

[1] Park JH, Saravanakumar G, Kim K, Kwon IC, Adv. Drug Deliv. Rev., 62, 28 (2010)

[2] Kwon IC, Kim K, Kim S, Chung H, Jeong SY, Polym. Sci. Technol., 15(4), 396 (2004)

[3] Kim JH, Kim YS, Park K, Lee S, Nam HY, Min KH, Jo HG, Park JH, Choi K, Jeong SY, Park RW, Kim IS, Kim K, Kwon IC, J. Control. Release., 127, 41 (2008)

[4] Yih TC, Al-Fandi M, J. Cell. Biochem., 97, 1184 (2006)

[5] Mu L, Feng SS, J. Control. Release., 86, 33 (2003)

[6] Maeda H, Wu J, Sawa T, Matsumura Y, Hori K, J.Control. Release., 65, 271 (2000)

[7] Winzenburg G, Schmidt C, Fuchs S, Kissel T, Adv.Drug Deliv. Rev., 56, 1453 (2004)

[8] Wang YS, Liu LR, Jiang Q, Zhang QQ, Eur. Polym. J., 43, 43 (2007)

[9] Agnihotri SA, Mallikarjuna NN, Aminabhavi TM, J. Control. Release., 100, 5 (2004)

[10] Liu ZH, Jiao YP, Wang YF, Zhou CR, Zhang ZY, Adv. Drug Deliv. Rev., 60, 1650 (2008)

[11] Yue W, Yao PJ, Wei YN, Li SQ, Lai F, Liu XM, Food Chem., 108, 1082 (2008)

[12] Zhang Y, Huo MR, Zhou JP, Yu D, Wu YP, Carbohydr. Polym., 77, 231 (2009)

[13] Bustamante J, Lodge JK, Marcocci L, Tritschler HJ, Packer L, Rihn BH, Free Radical Biol. Med., 24, 1023 (1998)

[14] Biewenga GP, Haenen GRMM, Bast A, Gen. Pharmacol., 29, 315 (1997)

[15] Dozio E, Ruscica M, Passaparo L, Dogliotti G, Steffani L, Marthyn P, Pagani A, Demartini G, Esposti D, Fraschini F, Magni P, Eur. J. Pharmacol., 641, 29 (2010)

[16] Park EJ, Kim YJ, Polym.(Korea), 32(6), 544 (2008)

[17] Kwon SK, Kim SW, Kim YJ, Polym.(Korea), 34(6), 501 (2010)