| 王彦妹，李娜梅，刘格莎，贺冬秀，唐国涛，雷小勇，严奉祥，喻翠云*.载药果胶基纳米粒子体外HepG2肝癌细胞的靶向性研究[J].南华大学学报(自然科学版),2013,27(1):69~74.[WANG Yan mei，LI Na mei，LIU Ge sha，HE Dong xiu，TANG Guo tao，LEI Xiao yong，YAN Feng xiang，YU Cui yun*.In vitro Evaluation of Pectin Nanoparticles Targeting Effect for Hepatocellular Carcinoma Cells[J].Journal of University of South China(Science and Technology),2013,27(1):69~74.] |
| 载药果胶基纳米粒子体外HepG2肝癌细胞的靶向性研究 |
| In vitro Evaluation of Pectin Nanoparticles Targeting Effect for Hepatocellular Carcinoma Cells |
| 投稿时间：2013-01-15 |
| DOI： |
| 中文关键词: 果胶基纳米粒子 HepG2 ASGPR 靶向给药体系 |
| 英文关键词:pectin nanoparticles HepG2 ASGPR TDD |
| 基金项目:国家自然科学基金资助项目(20774070)；湖南省教育厅基金资助项目(10C1179)；博士启动基金资助项目(2010XQD37) |
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| 中文摘要: |
| 具有良好的生物相容性且生物可降解天然多糖，一直作为药物传递体系，具有如下优点：可延长药物的生物半衰期，减轻药物的毒副作用.本实验旨在制备一种果胶基载5 氟脲嘧啶（5-Fluorouracil，5-FU）纳米粒子（P-5-FU）载药系统，探讨果胶基纳米载药体系本身带有大量的半乳糖残基这种天然靶头对人肝癌细胞 HepG2 的靶向效果.MTT法测定载药果胶基纳米粒子对HepG2和A549细胞的增殖抑制作用，MTT结果显示P-5-FU对HepG2细胞的增殖具有明显抑制作用，呈剂量依赖性，且作用较5-FU强；而P-5-FU对 A549 细胞增殖亦有明显抑制作用，呈剂量依赖性，但与5-FU 相比无明显差别；高效液相色谱法（HPLC）对两种细胞对载药纳米粒子的摄取情况和靶向性进行了测定.细胞摄取结果显示HepG2细胞对 P-5-FU的摄取量较5-FU明显增多，而A549细胞对P-5-FU和5-FU的摄取量没有明显的差别.半乳糖饱和ASGPR结合位点后两种细胞对 P-5-FU和5-FU的摄取量都没有明显的差别.结果表明果胶基纳米载药粒子可特异性靶向高表达的细胞. |
| 英文摘要: |
| Natural polysaccharide with good biocompatibility and biodegradability is always used as drug delivery system which offered numerous advantages，including reducing side effects，prolonging duration time，retaining drug bioactivity，and thus improving the therapeutic efficiency.This study aimed to propose a targeting human hepatocellular carcinoma cells (HepG2) drug delivery system based on pectin nanoparticles whose chains have a large number of galactose residues and evaluate their targeting effect on HepG2 cells.Cytotoxicity study（MTT） in HepG2 and A549 cell lines demonstrates that the resulting 5-Fluorouracil (5-FU) loaded nanoparticles are more potent in killing cancer cells with over expressed asialoglycoprotein receptor (ASGPR) on their surface，compared to free drug.While 5-FU loaded nanoparticles can also inhibit the proliferation of A549 cells in a dose dependent way，but there is no significant difference compared with free 5-FU.Cellular uptake of 5-FU and P-5-FU by HepG2，A549 cells was detected by High Performance Liquid Chromatography (HPLC).The HPLC results illustrate that the HepG 2 cells can uptake more P-5-FU than free 5-FU，while co incubated with galactose the HepG 2 cells has a relatively low uptake rate compared with P-5-FU and was closely comparable to that of free 5-FU.But the amount of 5-FU and P-5-FU in A549 cells was almost the same，when co incubated with galactose for 2h the amount of uptake of the two cell line also has no significant difference.The results indicate that the additional galactose competes with the “galactose residues” in the pectin based nanoparticles for binding to HepG2 cells，thus affects significantly the targeting efficacy of nanoparticles.However，no obvious difference was observed for A549 cells under the same condition.The overall results confirm the targeting efficacy of pectin based nanoparticles towards HepG2 cells. |
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