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Preparation and characterization of galactosylated glycol chitosan micelles and its potential use for hepatoma-targeting delivery of doxorubicin |
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| Authors: | Jing-Mou Yu Wei-Dong Li Lu Lu Xue-Yun Zhou Dian-Yuan Wang Hui-Min Li Xiao-Yuan Xu Jian Chen |
| Affiliation: | 1. Department of Pharmacy, College of Basic Medical Science, Jiujiang University, 17 Lufeng Road, Jiujiang, 332000, People’s Republic of China 2. Key Laboratory of Systems Biology Medicine of Jiangxi Province, College of Basic Medical Science, Jiujiang University, Jiujiang, 332000, People’s Republic of China 3. College of Science, Jiujiang University, Jiujiang, 332005, People’s Republic of China |
| Abstract: | This study aimed to develop novel galactosylated cholesterol modified-glycol chitosan (Gal-CHGC) micelles for targeting delivery of doxorubicin (DOX) in live cancer cells. Three kinds of Gal-CHGC conjugates were synthesized and characterized. The mean particle size and critical aggregation concentration of these polymeric micelles increased with the increase of galactose substitution degree. The DOX-loaded micelles were prepared by an o/w method. The mean diameters of DOX-loaded galactosylated micelles were in the range of 387–497 nm. DOX released from drug-loaded micelles displayed a biphasic way. Cellular uptake studies demonstrated that DOX-loaded galactosylated micelles could enhance the uptake of DOX into HepG2 cells. Moreover, the cytotoxicity of DOX-loaded galactosylated micelles against HepG2 cells significantly improved in contrast with free DOX and DOX-loaded micelles without galactosylation. These results suggested that Gal-CHGC micelles could be a potential carrier for hepatoma-targeting drug delivery. |
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