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Preparation and characterization of m PEG grafted chitosan micelles as 5-fluorouracil carriers for effective anti-tumor activity

查看全文 作  者:Dong-Jun [1]Fu;Yu [1]Jin;Mu-Qing [1]Xie;Ya-Jing [1]Ye;Dong-Dong [1]Qin;Kai-Yan [1,2,3]Lou;Yan-Zuo [1]Chen;Feng [1,2,3]Gao 高影响力作者 机构地区:[1]Department of Pharmaceutics, School of Pharmacy, East China University of Science and Technology;[2]Shanghai Key Laboratory of Functional Materials Chemistry, East China University of Science and Technology;[3]Shanghai Key Laboratory of New Drug Design, East China University of Science and Technology高影响力机构 出  处:《Chinese Chemical Letters》索引2014年第25卷第11期,共6页高影响力期刊 基  金:support from the Fundamental Research Funds for the Central Universities(No.WY1213013ECUST);supported by Science and Technology Commission of Shanghai Municipality(STCSM,contract Nos.11DZ2260600 and 10DZ2220500) 摘  要:The objective of this study was to investigate the potential of methoxy polyethylene glycol(m PEG)grafted chitosan(m PEG-g-CS) to be used as a drug carrier. m PEG-g-CS was successfully synthesized by one-step method with formaldehyde. The substitution degree of m PEG on chitosan was calculated by elemental analysis and was found to be(3.23 0.25)%. m PEG-g-CS self-assembled micelles were prepared by ultrasonic method with the controlled size of 178.5–195.1 nm and spherical morphology. Stable dispersion of the micelles was formed with the zeta potential of 2.3–30.2 m V. 5-Fluorouracil(5-FU), an anticancer chemotherapy drug, was used as a model drug to evaluate the efficiency of the new drug delivery carrier. The loading efficiency of 5-FU was(4.01 0.03)%, and the drug-loaded m PEG-g-CS self-assembled micelle showed a controlled-release effect. In summary, the m PEG-g-CS self-assembled micelle is proved to be a promising carrier with controlled particle size and controlled-release effect. Therefore, it has great potential for the application as 5-FU carriers for effective anti-tumor activity. 关 键 词:5-氟尿嘧啶 药物载体 抗肿瘤活性 壳聚糖 PEG 胶束 接枝 制备
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