氟尿嘧啶-壳寡糖/硒纳米微球的制备及抑制肿瘤细胞生长活性

doi:10.7503/cjcu20131141

高等学校化学学报 ›› 2014, Vol. 35 ›› Issue (7): 1603.doi: 10.7503/cjcu20131141

氟尿嘧啶-壳寡糖/硒纳米微球的制备及抑制肿瘤细胞生长活性

童春义, 唐凤霞, 刘斌, 廖红东, 刘选明()

湖南大学生物学院, 长沙 410082

收稿日期:2013-11-22 出版日期:2014-07-10 发布日期:2014-04-29
作者简介:联系人简介: 刘选明, 男, 博士, 教授, 博士生导师, 主要从事纳米药物载体研究. E-mail: xml05@126.com
基金资助:
国家自然科学基金青年基金(批准号: 31201074)和中央高校基本科研业务费专项资金(湖南大学, 批准号: 531107040020)资助

Preparation of Micro-spheres Co-carried Anti-tumor Drug and Sensitizer(5-Fu-COS/SeNP) and Their Inhibiting Tumorous Cellular Growths Activity^†

TONG Chunyi, TANG Fengxia, LIU Bin, LIAO Hongdong, LIU Xuanming^*()

College of Biology, Hunan University, Changsha 410082, China

Received:2013-11-22 Online:2014-07-10 Published:2014-04-29
Contact: LIU Xuanming E-mail:xml05@126.com
Supported by:
Supported by the National Natural Science Foundation of China for Young Scholars(No.31201074) and the Fundamental Research Funds for the Central Universities of China(Hunan University)(No.531107040020)

摘要/Abstract

摘要：

为研究抗肿瘤药物与辅药负载于同一药物载体的作用效果, 首先以壳寡糖和广谱抗肿瘤药物5-氟尿嘧啶(5-Fu)为原料通过化学键合合成氟尿嘧啶-壳寡糖前体, 然后以其为模板通过溶胶-凝胶法制备了同时负载氟尿嘧啶和硒纳米颗粒的壳寡糖微球. 采用透射电子显微镜(TEM)、 Zeta电位仪和红外光谱(IR)对制备的微球进行了表征, 结果表明, 微球粒径为433 nm, 硒纳米颗粒包裹在微球内; 对微球包裹药物进行检测发现, 5-Fu装载率为(8.2±0.3)%, 硒装载率为(7.96±0.34)%; 体外缓释检测和细胞实验结果证实, 微球能够缓慢释放2种药物, 其缓释作用能很好地抑制肝癌细胞SMMC-7721的生长.

关键词: 氟尿嘧啶, 硒纳米颗粒, 纳米微球, 抗肿瘤活性

Abstract:

5-Fu-COS/SeNP micro-spheres were prepared in two steps to study the antitumor drug load and auxiliary same effects as the drug carrier. First, the Fu-COS prodrug was synthesized with the broad-spectrum anti-tumor drug 5-fluorouracil(5-Fu) and chito-oligosaccharides(COS), then, Fu-COS was used as temples while 5-Fu-COS/SeNP was prepared by sol-gel method. 5-Fu-COS/SeNP was characterized by TEM, Zeta-sizer and IR, and its anti-tumor activity was detected by MTT method. The results showed that 5-Fu and Se were completely carried in 5-Fu-COS/SeNP, the size of 5-Fu-COS/SeNP was 433 nm, the drug-loading rate of 5-Fu and Se were (8.2±0.3)% and (7.96±0.34)%, respectively, and 5-Fu and nanose released slowly and had well inhibiting tumorous cellular growths activity. As time increases, release rate of the drug by Fu-COS/SeNP increased and the inhibition of cell enhanced. After 24 h, inhibition rate had exceeded the sum of 5-Fu and SeNP. After 48 h, the inhibition rate of Fu-COS/SeNP was less than the sum of the inhibition rate of 5-Fu and SeNP, but higher than that of 5-Fu or SeNP. These results indicated that the spheres have high drug loading efficiency and good drug release properties. This novel method to produce micro-spheres could expand the development of drug release research.

Key words: 5-Fluorouracil(5-Fu), Se nanoparticles, Nanomicro-spheres, Anti-tumor activity

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TrendMD:

童春义, 唐凤霞, 刘斌, 廖红东, 刘选明. 氟尿嘧啶-壳寡糖/硒纳米微球的制备及抑制肿瘤细胞生长活性. 高等学校化学学报, 2014, 35(7): 1603.

TONG Chunyi, TANG Fengxia, LIU Bin, LIAO Hongdong, LIU Xuanming. Preparation of Micro-spheres Co-carried Anti-tumor Drug and Sensitizer(5-Fu-COS/SeNP) and Their Inhibiting Tumorous Cellular Growths Activity^†. Chem. J. Chinese Universities, 2014, 35(7): 1603.

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氟尿嘧啶-壳寡糖/硒纳米微球的制备及抑制肿瘤细胞生长活性

Preparation of Micro-spheres Co-carried Anti-tumor Drug and Sensitizer(5-Fu-COS/SeNP) and Their Inhibiting Tumorous Cellular Growths Activity^†

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氟尿嘧啶-壳寡糖/硒纳米微球的制备及抑制肿瘤细胞生长活性

Preparation of Micro-spheres Co-carried Anti-tumor Drug and Sensitizer(5-Fu-COS/SeNP) and Their Inhibiting Tumorous Cellular Growths Activity†

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Preparation of Micro-spheres Co-carried Anti-tumor Drug and Sensitizer(5-Fu-COS/SeNP) and Their Inhibiting Tumorous Cellular Growths Activity^†