高等学校化学学报

高等学校化学学报 ›› 2011, Vol. 32 ›› Issue (2): 416.

• 研究论文 • 上一篇    

甘草次酸修饰PEG-PLGA纳米粒的制备及与肝癌细胞亲和性

黄微,王平,王蔚,张玥,张闯年,田秦,王秀华,刘媛,袁直   

  1. 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
  • 收稿日期:2010-03-16 修回日期:2010-04-22 出版日期:2010-02-10 发布日期:2011-02-23
  • 通讯作者: 袁直 E-mail:zhiy@nankai.edu.cn
  • 基金资助:

    国家自然科学基金(批准号: 50873048)和天津市自然科学基金(批准号: 07JCZDJC00700) 资助.

Preparation of Glycyrrhetinic Acid-modified PEG-PLGA Nanoparticles and the Affinity Evaluation on Hepatoma Cells

HUANG Wei, WANG Ping, WANG Wei, ZHANG Yue, ZHANG Chuang-Nian, TIAN Qin, WANG Xiu-Hua, LIU Yuan, YUAN Zhi*   

  1. Key Laboratory of Functional Polymer Materials, Ministry of Education, Institute of Polymer Chemistry, Nankai University, Tianjin 300071, China
  • Received:2010-03-16 Revised:2010-04-22 Online:2010-02-10 Published:2011-02-23
  • Contact: YUAN Zhi E-mail:zhiy@nankai.edu.cn
  • Supported by:

    国家自然科学基金(批准号: 50873048)和天津市自然科学基金(批准号: 07JCZDJC00700) 资助.

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被引次数

33

摘要： 肝靶向药物载体材料是目前研究的热点. 本文将肝靶向分子甘草次酸偶联至聚乙二醇-聚(乳酸-羟基乙酸)(PEG-PLGA)嵌段共聚物上. 以聚乙二醇维生素E (TPGS)为稳定剂，采用溶剂挥发法制备肝靶向纳米粒，通过核磁、红外、激光光散射、透射电镜等方法对共聚物及纳米粒的理化性质进行表征；运用噻唑蓝(MTT)比色法评价纳米粒作为药物载体的安全性，并通过荧光显微镜初步考察了纳米粒与肝癌细胞的亲和能力.结果表明纳米粒子粒径128.2 nm，电势-16.2 mV，在电解质溶液中具有较高稳定性. 细胞实验结果显示该纳米粒无明显细胞毒性，且甘草次酸的引入能显著增加肝癌细胞对纳米粒的摄取几率，显示出其作为肝靶向药物载体的潜在价值.

关键词: 甘草次酸, 聚乙二醇-聚(乳酸-羟基乙酸), 聚乙二醇维生素E, 肝靶向药物载体.

Abstract: In this study, glycyrrhetinic acid-modified PEG-PLGA copolymer was fabricated, and was formed into nanoparticles (NPs) via solvent evaporation method with D-α-tocopheryl poly(ethylene glycol) succinate (TPGS) as a stabilizer. The physicochemical properties of the present system were investigated by NMR, IR, DLS, Ztea and TEM measurements. The cytotoxicity against hepatoma cells was studied based on MTT assay, and the affinity between the cells and the NPs were preliminarily evaluated by fluorescence microscopy. The results showed that the NPs were regularly spherical in shape with a hydrodynamic diameter around 128.2 nm, and the ztea potential of the NPs was about -16.2 mv. Besides, the NPs exhibited good stability against electrolyte solution. MTT result suggested that the NPs almost had no cytotoxicity on cells. Furthermore, the in vitro cell uptake result indicated that GA-modified NPs had a high affinity with hepatoma cells, and could be a promising liver targeted material.

Key words: Glycyrrhetinic acid, PEG-PLGA, D-α-tocopheryl poly(ethylene glycol) succinate (TPGS), Liver targeted material.

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