Polymer(Korea), Vol.32, No.3, 263-269, May, 2008
소수성 항암제의 전달체로 응용하기 위한 리소콜릭산이 결합된 키토산 나노입자의 제조와 특성
Preparation and Characterization of Lithocholic Acid Conjugated Chitosan Oligosaccharide Nanoparticles for Hydrophobic Anticancer Agent Carriers
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초록
키토산에 기초한 소수성 항암제의 전달체를 개발하기 위하여, 젖산염 키토산을 소수성기로써 담즙산 중의 하나인 리소콜릭산(lithocholic acid, LA)을 이용하여 화학적으로 개질하였다. LA가 결합된 키토산 나노입자(COS-LA)의 물리화학적 특성을 1H-NMR, dynamic light scattering(DLS) 그리고 spectrofluorophotometer를 이용하여 조사하였다. 항암제로써 파클리탁셀(paclitaxel)이 봉입된 CLs-Tx(COS-LA-paclitaxel) 나노입자는 투석 방법을 이용하여 제조되었고 HPLC를 통하여 약물의 봉입량을 측정하였다. DLS를 이용하여 측정한 파클리탁셀이 봉입된 나노 입자의 크기는 약 300 nm를 나타내었다. 또한 임계미셀형성(CMC) 농도는 LA의 치환도에 의존한다는 것을 확인하였다. 이상의 결과로부터 본 연구에서 제조한 LA가 결합된 젖산염 키토산이 파클리탁셀 전달체로서 매우 높은 응용 가능성을 나타내고 있음을 확인하였다.
To develop carriers of hydrophobic anticancer agents based on chitosan, chitosan oligosaccharide lactate (COS) was chemically modified with lithocholic acid (LA) which is one of the bile acids as a hydrophobic group. The physicochemical properties of the lithocholic acid conjugated chitosan nanoparticles (COS-LA) were investigated using 1H-NMR spectroscopy, dynamic light scattering (DLS) and spectrofluorophotometer. COS-LA-paclitaxel (CLs-Tx) nanoparticles loading paclitaxel as an anticancer agent were prepared by a dialysis method and its loading efficiency was measured through HPLC. On the basis of DLS results, the estimated particle sizes of CLs-Tx were around 300 nm. Also, the critical micelle concentration (CMC) was proven to be dependent on the degree of substitution of lithocholic acid. It showed that the CLs-Tx has the superior potential for the application as a paclitaxel carrier.
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