Preparation of pH-Responsive Micelle Based on Hyaluronic Acid for Drug Delivery
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R944.9

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    Abstract:

    To prepare the CD44-targeted hyaluronic acid-deoxycholic acid(HAAD) amphiphile to form micelles for the encapsulation of model anticancer drug doxorubicin(DOX),and its properties and anticancer activity were characterized. The boronate derived deoxycholic acid was synthesized via amidation reaction. Afterwards,HAAD was prepared by conjugating hyaluronic acid and boronate derived deoxycholic acid via boronate ester bond. The DOX encapsulated HAAD micelles were prepared and their properties,such as encapsulation efficiency(EE),drug loading level(DL) of DOX,in vitro drug release behavior were characterized. The cytotoxicity and cellular internalization were evaluated against model tumor cells(MCF-7) and normal cells(COS7). HAAD was successfully prepared and could self assemble into micelles with DOX loaded inside. The DL value of DOX was 9.15%. Moreover,the DOX-loaded HAAD micelles could show pH-responsive drug release behavior,the drug release rate was faster at acidic milieu. The flow cytometry analysis demonstrated the DOX-loaded HAAD micelles could be internalized by CD44-overexpressed MCF-7 cells more effectively. Additionally,the cytotoxicity assay showed DOX-loaded HAAD micelles had less toxicity against normal cells than that of tumor cells,showing selectivity.

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SONG Jiahong, XU Shanshan, ZHANG Manyue, LIU Xiao, XU Feige, ZHU Dongqi, CHEN Jingxiao, CHEN Jinghua. Preparation of pH-Responsive Micelle Based on Hyaluronic Acid for Drug Delivery[J]. Journal of Food Science and Biotechnology,2019,38(3):32-38.

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  • Online: June 21,2019
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