| 叶酸修饰星型端氨基PEG-PLGA纳米胶束的制备及肿瘤细胞靶向作用 |
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| 引用本文： | 马桂蕾,赵顺新,金旭,陈旼旼,张政朴,宋存先.叶酸修饰星型端氨基PEG-PLGA纳米胶束的制备及肿瘤细胞靶向作用[J].高等学校化学学报,2012,33(8):1854-1859. |
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| 作者姓名： | 马桂蕾 赵顺新 金旭 陈旼旼 张政朴 宋存先 |
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| 作者单位： | 1. 中国医学科学院生物医学工程研究所, 天津市生物材料重点实验室, 天津 300192;
2. 南开大学高分子化学研究所, 功能高分子材料教育部重点实验室, 天津 300071;
3. 首都医科大学附属北京天坛医院, 北京 100050 |
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| 基金项目： | 国家自然科学基金,天津市自然科学基金,北京市自然科学基金 |
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| 摘 要： | 合成了星型多臂端氨基聚乙二醇(PEG)/聚乳酸-羟基乙酸(PLGA)两亲性嵌段共聚物(4s-PLGA-PEG-NH2), 并通过核磁共振和凝胶渗滤色谱法对其结构进行表征; 采用溶剂挥发法制备阿霉素载药纳米胶束, 利用EDC缩合法与叶酸偶联, 得到叶酸修饰的星型端氨基PEG-PLGA纳米胶束; 采用动态光散射、 紫外光谱及透射电镜等手段对纳米胶束进行了表征; 对载药纳米胶束在HeLa细胞中的摄取及细胞毒性进行了初步评价. 结果表明, 经叶酸修饰的星型多臂端氨基PEG-PLGA载药纳米胶束可有效提高HeLa细胞的摄取率以及对HeLa细胞的杀伤率, 表明其可作为一类新型的靶向抗肿瘤药物递送载体.
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| 关 键 词： | 星型聚合物 端氨基聚乙二醇-聚(乳酸-羟基乙酸) 纳米胶束 叶酸 靶向 |
| 收稿时间： | 2011-09-22 |
Folate-conjugated Micelles Based on Star-shaped PLGA-PEG-NH2 Copolymers as Novel Tumor-targeted Nanocarriers |
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| MA Gui-Lei
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ZHAO Shun-Xin
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JIN Xu
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CHEN Min-Min
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ZHANG Zheng-Pu
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SONG Cun-Xian.Folate-conjugated Micelles Based on Star-shaped PLGA-PEG-NH2 Copolymers as Novel Tumor-targeted Nanocarriers[J].Chemical Research In Chinese Universities,2012,33(8):1854-1859. |
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| Authors: | MA Gui-Lei ZHAO Shun-Xin JIN Xu CHEN Min-Min ZHANG Zheng-Pu SONG Cun-Xian |
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| Institution: | 1. Tianjin Key Laboratory of Biomaterials, Institute of Biomedical Engineering, Chinese Academy of Medical Sciences, Tianjin 300192, China;
2. Key Laboratory of Functional Polymer Materials, Ministry of Education, Institute of Polymer Chemistry, Nankai University, Tianjin 300071, China;
3. Capital Medical University Affiliated Beijing Tiantan Hospital, Beijing 100050, China |
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| Abstract: | A new type of folic acid(FA)-conjugated amphiphilic 4-arm star-shaped PLGA-PEG-NH2(4s-PLGA-PEG-NH2) micelles was prepared as a doxorubicin(DOX)-loaded nanocarrier for tumor-targeted drug delivery. The 4s-PLGA-PEG-NH2 micelles were prepared by a solvent evaporation method; then, FA was conjugated onto the surface of the micelles using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride(EDC) conjugation chemistry. The structure of the synthesized 4s-PLGA-PEG-NH2 copolymer was characterized by 1H NMR and gel permeation chromatography(GPC). The prepared micelles properties were determined by dynamic light scattering, UV spectra and TEM observation. The cellular uptake and cytotoxicity of FA-conjugated DOX-4s-PLGA-PEG-NH2 micelles were assessed using confocal laser scanning microscopy(CLSM) and the cell counting kit-8 assay. The results show that compared with the nontargeted DOX-micelles, FA-DOX-micelles have higher cellular uptake of DOX, and subsequently a higher cytotoxicity to tumor cells. In conclusion, the FA-conjugated 4s-PLGA-PEG-NH2 micelles could be an excellent nanocarrier to deliver anticancer drugs specifically inside the cell via FA-receptor-medicated endocytosis. |
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| Keywords: | Star-shaped copolymer PLGA-PEG-NH2" target="_blank">2')" href="#">PLGA-PEG-NH2 Nano-micelle Folic acid Targeted carrier |
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