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KMID : 0525720130180040235
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Journal of Chitin and Chitosan
2013 Volume.18 No. 4 p.235 ~ p.242
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Evaluation of Folic Acid and Doxorubicin Conjugated O-carboxymethyl Chitosan for pH-sensitive Target Drug Delivery
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Kim Tae-Hun
Park Sun-Jeong
Nam Joung-Pyo
Park Seong-Cheol
Choi Chang-Yong
Jang Mi-Kyeong
Nah Jae-Woon
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Abstract
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In this study, target ligand and anticancer drug were conjugated with O-carboxymethyl chitosan (FPOCM-DOX). Targeting ligand was used folic acid (FA) for specific binding of FA receptor overexpressed cancer cell. Anticancer drug model was used doxorubicin (DOX). DOX was conjugated with 2, 3-dimethylmaleic anhydride (DMMA) (DMMA-DOX) for pH-sensitive drug release. The FPOCM-DOX of chemical structure was analyzed by 1 H-NMR and FT-IR. DLS study that the FPOCM-DOX was self-aggregated to an average diameter of 432 nm. In addition, the antitumor activity of FPOCM-DOX was demonstrated against HeLa cell by MTT assay. The IC50 of OCM-DOX and FPOCM-DOX were confirmed 11.25 μg, 5.6 μg in HeLa cell. The antitumor activity considered that FPOCM-DOX might be increased antitumor activity by receptor mediate endocytosis. The result suggested that FPOCM-DOX might be a promised anticancer drug carrier for cancer therapy.
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KEYWORD
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pH-sensitive, Doxorubicin, Folic acid, Folic acid receptor
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