Article
  • Preparation and Characterization of Deoxycholic Acid-Conjugated Low Molecular Weight Water-Soluble Chitosan Nanoparticles for Hydrophobic Antifungal Agent Carrier
  • Choi CY, Jung H, Nam JP, Park YK, Jang MK, Nah JW
  • 소수성 항진균제 전달체로 응용하기 위한 데옥시콜릭산이 결합된 저분자량 수용성 키토산 나노입자의 제조와 특성
  • 최창용, 정현, 남정표, 박윤경, 장미경, 나재운
Abstract
To develop the carrier of hydrophobic antifungal agents based on low molecular weight watersoluble chitosan (LMWSC), LMWSC was chemically modified with deoxycholic acid (DA) which is one of the bile acid as a hydrophobic group. The nanoparticles (WSCDA) using DA conjugated LMWSC were characterized using dynamic light scattering(DLS) and transmittance electron microscope (TEM). The particle size of WSCDA ranged from 250 to 350 nm and increased with the number of DA substitution. The loaded itraconazole as an antifungal agent WSCDA nanoparticles (WSCDA-ITCN) were prepared by solvent evaporation method. The drug content and the loading efficiency were investigated approximately 9∼10% and 61∼68% by UV spectrophotometer, respectively. The release of drug from nanoparticles was slow and showed sustained release characteristics. Based on the results of release study that the higher DA contents in WSCDA, the slower the releasing rate, the WSCDA-ITCN could be used as an excellent antifungal agent.

저분자량 수용성 키토산(LMWSC)을 소수성 항진균제 전달체로 응용하기 위하여, 데옥시콜릭산(deoxycholic acid, DA)을 이용하여 LMWSC를 화학적으로 개질하였다. DA가 결합된 LMWSC 나노입자(WSCDA)의 특성은 동적광산란기, 투과전자현미경을 이용하여 그 특성을 분석하였다. 제조되어진 나노입자의 크기는 250∼350 nm로 DA의 치환도가 증가함에 따라 입자의 크기가 증가하였다. 항진균제인 이트라코나졸(itraconazole)이 봉입된 WSCDA 나노입자(WSCDA-ITCN)는 소수성 상호작용을 이용한 용매 증발법으로 제조하였다. UV 분광광도계를 이용하여 약물의 함량 및 담지 효율을 측정한 결과 약물의 담지 효율은 61∼68%로 우수한 담지 효율을 보였다. 약물방출 거동에서 이트라코나졸이 봉입된 나노파티클의 DA의 함량이 많아질수록 약물이 천천히 방출되었다. 이상의 결과로부터 본 연구에서 제조한 DA가 결합된 저분자량 수용성 키토산 나노파티클이 항진균제 전달체로서 매우 높은 응용 가능성을 나타내고 있음을 확인하였다.

Keywords: LMWSC; deoxycholic acid; antifungal; itraconazole; drug

References
  • 1. Nah JW, Jang MK, J. Polym. Sci. A: Polym. Chem., 40(21), 3796 (2002)
  •  
  • 2. Ikeda I, Sugano M, Yoshida K, Sasaki E, Iwamoto Y, Hatano K, J. Agric. Food Chem., 41, 431 (1993)
  •  
  • 3. Muzzarelli RAA, Lough C, Emanuelli M, Caborhydr. Res., 8, 433 (1987)
  •  
  • 4. Sawayanagi Y, Nambu N, Nagai T, Chem. Pharm. Bull., 31, 2507 (1983)
  •  
  • 5. Paul W, Sharma CP, S. T. P. Phama Science, 10, 5 (2000)
  •  
  • 6. Lee M, Nah J, Kwon Y. Koh J, Ko K, Kim SW, Phamaceut. Res., 18, 427 (2001)
  •  
  • 7. Jang MJ, Kim DG, Jeong YI, Jang MK, Nah JW, Polym.(Korea), 31(6), 555 (2007)
  •  
  • 8. Behr JP, Acc. Chem. Res., 26, 274 (1993)
  •  
  • 9. Wagner E, Cotton M, Curr. Opin. Biotechnol., 4, 705 (1993)
  •  
  • 10. Chandy T, Sharma CP, Art Cells Art. Org., 18, 1 (1990)
  •  
  • 11. Park JS, Yang JC, Yuk SH, Shin HS, Rhee JM, Kim MS, Lee HB, Khang G, Polym.(Korea), 31(3), 189 (2007)
  •  
  • 12. Del Rosso JQ, Gupta AK, Today’s Therapeutic Trends, 15, 179 (1997)
  •  
  • 13. Del Rosso JQ, Zellis S, Gupta AK, J. Am. Osteopath. Assoc., 98, 497 (1998)
  •  
  • 14. Hickman JG, J. Am. Acad. Dermatol., 34, 785 (1996)
  •  
  • 15. Delescluse J, J. Am. Acad. Dermatol., 23, 551 (1990)
  •  
  • 16. Del Rosso JQ, Gupta AK, Int. J. Dermatol., 38, 28 (1999)
  •  
  • 17. Alcantara R, Garibay JM, Adv. Ther., 5, 26 (1998)
  •  
  • 18. Dongowski G, Fritzsch B, Giessler J, Hartl A, Kuhlmann O, Neubert RHH, Eur. J. Pharm. Biopharm., 60, 147 (2005)
  •  
  • 19. Maeda T, Takenaka H, Yamahira Y, Noguchi T, J. Pharm. Sci., 68, 1286 (1979)
  •  
  • 20. Chiba Y, Kohri N, Iseki K, Miyazaki K, Chem. Pharm. Bull., 39, 2158 (1991)
  •  
  • 21. Chae SY, Son S, Lee M, Jang MK, Nah JW, J. Control. Release, 109, 330 (2005)
  •  
  • 22. Kwon S, Park JH, Chung H, Kwon IC, Jeong SY, Kim IS, Langmuir, 19(24), 10188 (2003)
  •  
  • Polymer(Korea) 폴리머
  • Frequency : Bimonthly(odd)
    ISSN 0379-153X(Print)
    ISSN 2234-8077(Online)
    Abbr. Polym. Korea
  • 2023 Impact Factor : 0.4
  • Indexed in SCIE

This Article

  • 2009; 33(4): 389-395

    Published online Jul 25, 2009

  • Received on May 15, 2009
  • Accepted on Jun 9, 2009