阿霉素脂质体的制备及抗肿瘤活性研究

doi:10.3969/j.issn.1006-7795.2015.02.001

首都医科大学学报 ›› 2015, Vol. 36 ›› Issue (2): 157-160.doi: 10.3969/j.issn.1006-7795.2015.02.001

阿霉素脂质体的制备及抗肿瘤活性研究

李飞阳¹, 崔纯莹¹, 王玉记², 吴建辉²

1. 首都医科大学化学生物学与药学院药剂学系, 北京 100069;
2. 首都医科大学化学生物学与药学院药物化学系, 北京 100069

收稿日期:2014-12-08 出版日期:2015-04-21 发布日期:2015-04-16
通讯作者: 吴建辉 E-mail:wujianhui01@126.com
基金资助:
"十二五"重大新药创制科技重大专项(2011ZX09302-007-01)。

Preparation and antitumor activity of a novel liposome of doxorubicin

Li Feiyang¹, Cui Chunying¹, Wang Yuji², Wu Jianhui²

1. Department of Pharmacy, School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China;
2. Department of Medicinal Chemistry, School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China

Received:2014-12-08 Online:2015-04-21 Published:2015-04-16
Supported by:
This study was supported by Significant New Drugs Creation "Five-year" Plan Special Science and Technology Major(2011ZX09302-007-01).

摘要/Abstract

摘要： 目的开发一种新型阿霉素脂质体制剂。方法采用膜分散法制备阿霉素脂质体;采用噻唑蓝比色法(MTT法)考察阿霉素和阿霉素脂质体对5种人类肿瘤细胞株增生的抑制作用;以荷S180小鼠为模型,考察阿霉素和阿霉素脂质体的抗肿瘤活性。结果膜分散法适用于制备阿霉素脂质体,其平均包封率高于95%;阿霉素制备成脂质体仍具备抑制肿瘤细胞株增生活性,并呈现时间依赖关系;动物实验表明,阿霉素脂质体的抗肿瘤活性比阿霉素强,毒性比阿霉素低。结论此法制备的阿霉素脂质体包封率高,简便易行,重现性好,并且显示了较好的抗肿瘤活性。

关键词: 阿霉素脂质体, 肿瘤细胞增生, 释放曲线, 抗肿瘤活性

Abstract: Objective To develop a novel preparation of liposomal doxorubicin. Methods The liposome was prepared by dispersion film assay, loaded doxorubicin by ammonium sulfate gradient method, the anti-proliferation activities of doxorubicin liposome and doxorubicin against cancer cells evaluated by MTT assay and the antitumor activities of doxorubicin liposome and doxorubicin on S180 mouse model were measured. Results The doxorubicin liposome encapsulation efficiency was more than 96.3% at different time points. Doxorubicin liposome effectively inhibited the proliferation of carcinoma cells. The in vivo anti-tumor activity and toxicity of doxorubicin liposome were significantly higher and lower than that of doxorubicin, respectively. Conclusion The method is practicable to prepare doxorubicin liposome having good antitumor potency in vivo.

Key words: doxorubicin liposome, cytotoxicity, releasing curve, anti-tumor activity in vivo

中图分类号:

R965.1

李飞阳, 崔纯莹, 王玉记, 吴建辉. 阿霉素脂质体的制备及抗肿瘤活性研究[J]. 首都医科大学学报, 2015, 36(2): 157-160.

Li Feiyang, Cui Chunying, Wang Yuji, Wu Jianhui. Preparation and antitumor activity of a novel liposome of doxorubicin[J]. Journal of Capital Medical University, 2015, 36(2): 157-160.

[1]	黄萍, 崔纯莹, 王玉记, 吴建辉. 聚乙二醇包裹表阿霉素脂质体的制备及评价[J]. 首都医科大学学报, 2015, 36(2): 166-172.
[2]	李雪梅, 王玉记, 吴建辉, 崔纯莹. RGD脂肪醇与17-AAG脂质体的制备及抗肿瘤活性研究[J]. 首都医科大学学报, 2015, 36(2): 172-177.
[3]	闫岩, 王玉记, 吴建辉, 崔纯莹. 17-AAG聚氰基丙烯酸正丁酯纳米粒的制备及抗肿瘤活性研究[J]. 首都医科大学学报, 2015, 36(2): 178-184.
[4]	史凡, 崔纯莹, 吴建辉, 王玉记. 多西紫杉醇-海豹油纳米结构脂质载体的抗肿瘤活性评价[J]. 首都医科大学学报, 2015, 36(2): 185-191.
[5]	蒋雪云, 张颖洁, 赵明. 超黄金治疗期的缺血性中风大鼠模型、治疗模式及疗效表述[J]. 首都医科大学学报, 2014, 35(1): 108-112.
[6]	张如意, 张丽, 吴燕川, 李林. 二苯乙烯苷对PD模型小鼠干预作用的观察及机制初探[J]. 首都医科大学学报, 2014, 35(6): 735-740.

阿霉素脂质体的制备及抗肿瘤活性研究

Preparation and antitumor activity of a novel liposome of doxorubicin

PDF

可视化

被引次数

摘要/Abstract

引用本文

使用本文

参考文献

相关文章 6

编辑推荐

Metrics

本文评价