叶酸偶联纳米紫杉醇的制备

doi:10.3969/j.issn.1006-7795.2012.05.002

首都医科大学学报 ›› 2012, Vol. 33 ›› Issue (5): 565-568.doi: 10.3969/j.issn.1006-7795.2012.05.002

叶酸偶联纳米紫杉醇的制备

佟玲霞, 李红霞

首都医科大学附属北京世纪坛医院妇产科,北京 100038

收稿日期:2012-06-18 修回日期:1900-01-01 出版日期:2012-10-21 发布日期:2012-10-21
通讯作者: 李红霞

Preparation of folic acid coupled nano-paclitaxel drug

TONG Ling-xia, LI Hong-xia

Department of Obstetrics and Gynecology, Beijing Shijitan Hospital, Capital Medical University, Beijing 100038, China

Received:2012-06-18 Revised:1900-01-01 Online:2012-10-21 Published:2012-10-21

摘要/Abstract

摘要： 目的制备磷脂酰乙醇胺-聚乙二醇2000-叶酸(folic acid monomethoxy-polyethylene glycol 2000-distearoyl phosphatidyle thanolamine,ESPE-PEG2000-FA)修饰的紫杉醇纳米脂质体并考察其性质。方法采用超声乳化-溶剂挥发法制备DSPE-PEG2000-FA胶束;采用薄膜分散-挤压法制备紫杉醇脂质体;两者共同孵育形成DSPE-PEG2000-FA修饰的紫杉醇纳米脂质体;并测定修饰前后脂质体的粒径,包封率。结果叶酸偶联纳米紫杉醇药物的粒径(140.5±10.3)nm,多分散指数0.263±0.061,与原料药物纳米紫杉醇的粒径［(121.6±12.7)nm］和多分散指数(0.262±0.031)相比,差异无统计学意义。叶酸-紫杉醇纳米脂质体药物的包封率高达97%,与原料药紫杉醇纳米脂质体的包封率99%相比,差异无统计学意义,保证了药物的纯度和有效性。结论本研究报道了一种靶向叶酸偶联纳米紫杉醇的新剂型及制备方法。该剂型有良好的药物包封率和胶体稳定性。

关键词: 磷脂酰乙醇胺-聚乙二醇2000-叶酸, 脂质体, 紫杉醇, 粒径, 包封率

Abstract: Objective To prepare the folic acid coupled nano-paclitaxel drug for targeted tumor therapy. Methods Nano-paclitaxel was prepared by polycarbonate membrane dispersion-extrusion. The method of ultrasonic emulsification-solvent evaporation was adopted to prepare DSPE-PEG2000-FA micelle. Co-incubation method was used to prepare DSPE-PEG2000-FA modified folic acid coupling nano-paclitaxel. The mean diameter of folic acid coupling nano-paclitaxel drugs and the encapsulation efficiency were determined by zetasizer and elution curve of drug. Results Compared with the diameter of nano-paclitaxel particle［(121.6±12.7) nm］and polydispersity index (PDI) (0.262±0.031), the mean diameter of folic acid coupling nano-paclitaxel drugs ［(140.5±10.3) nm］ and PDI (0.263±0.061) were slightly larger, but the difference was not statistically significant (t=2.013; P=0.114). In contrast to the encapsulation efficiency of the crude drugs (nano-paclitaxel drugs) 99%, the encapsulation efficiency of folic acid coupling nano-paclitaxel drugs was as high as 97% with no significant decline, which ensures purity and effectiveness of the drugs. Conclusion The novel formulation of FR-targeted folic acid coupling nano-paclitaxel is reported. This formulation has good drug loading properties, drug encapsulation efficiency, and exhibits excellent colloidal stability.

Key words: folic acid monomethoxy-polyethylene glycol 2000-distearoyl phosphatidylethanolamine, nano-liposomes, paclitaxel, particle size, encapsulation

中图分类号:

R 94

佟玲霞;李红霞. 叶酸偶联纳米紫杉醇的制备[J]. 首都医科大学学报, 2012, 33(5): 565-568.

TONG Ling-xia;LI Hong-xia. Preparation of folic acid coupled nano-paclitaxel drug[J]. Journal of Capital Medical University, 2012, 33(5): 565-568.

[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.
[2]	魏丽艳, 崔纯莹, 吴建辉, 王玉记. 以海豹油为基质的多西紫杉醇脂肪乳的制备及其抗肿瘤活性研究[J]. 首都医科大学学报, 2015, 36(2): 192-198.
[3]	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.
[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]	王晶;赵灵芝;克晓燕. 制备淋巴瘤多基因肿瘤疫苗的方法学探索[J]. 首都医科大学学报, 2008, 29(2): 118-123.
[6]	张利群;陈杭薇;王四海;辛庆红;杜玉国;尤兰华. 人呼吸道合胞病毒转录调节基因转染PAa和A549肺腺癌细胞系[J]. 首都医科大学学报, 2005, 26(6): 733-736.
[7]	王红霞;杨慧;郝刚;曾翔俊;芦玲巧;江瑛;朱宪;姚兴海;张立克. 脂质体作为溶栓药物载体靶向抗血栓的实验研究[J]. 首都医科大学学报, 2004, 25(3): 290-293.
[8]	赵春礼;郑少鹏;王珂;鲁强;田竟生;徐群渊. 脂质体介导的骨骼肌细胞的基因转移[J]. 首都医科大学学报, 1996, 17(3): 165-167.

叶酸偶联纳米紫杉醇的制备

Preparation of folic acid coupled nano-paclitaxel drug

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 8

编辑推荐

Metrics

本文评价