中国组织工程研究与临床康复2011，Vol.15Issue(51)：9583-9586,4.DOI:10.3969/j.issn.1673-8225.2011.51.020
9-硝基喜树碱叶酸聚合物胶束肿瘤靶向给药系统的表征及体外药效评价
Characterization and pharmacodynamic evaluation in vitro of 9-nitro-camptothecin-loaded folate-conjugated polymer micelles as tumor-targeted drug delivery system
摘要
Abstract
BACKGROUND: Recently, the increasing attention has been focused on amphiphilic polymer micelles as carriers for poorly soluble drugs and folate-mediated tumor targeted drug delivery system in the field of pharmaceutics.OBJECTIVE: To prepare 9-nitro -camptothecin (9 -NC)-loaded folate-conjugated polymer micelles and investigate its characterization and antituomor activity in vitro .METHODS: The 9-NC-loaded folate-conjugated polymer micelles were prepared by film-hydration method; micelles size and drug loading capacity were determined by laser particle size analyzer and reversed-phase high-performance liquid chromatography respectively. The dialysis method was used in vitro release study. Pharmacodynamic evaluation in vitro was performed using cellular uptake and cell growth inhibition tests.RESULTS AND CONCLUSION: The diameter of the formulated 9-NC-loaded folate-conjugated micelles was about 24-26 nm. The encapsulation efficiency and drug loading capacity were 95.7% and 3.24% resp ectively. And the accumulative release percentage in 24 hours of drug-loaded micelles was about 90%. Besides, the folate-conjugated micelles had higher binding affinity with tumor cells and significantly stronger antitumor activity in vitro than normal micelles. The results indicated that the folate-conjugated micelles can provide a type of tumor-targeted nano drug delivery system with good prospect for insoluble drugs.关键词
聚合物胶束/9-硝基喜树碱/叶酸/肿瘤细胞靶向/抗肿瘤活性分类
医药卫生引用本文复制引用
徐金军,韩雪,倪京满,陆伟跃..9-硝基喜树碱叶酸聚合物胶束肿瘤靶向给药系统的表征及体外药效评价[J].中国组织工程研究与临床康复,2011,15(51):9583-9586,4.基金项目
国家重大科学研究计划(973 计划)资助项目(2010CB934000) （973 计划）
国家重大新药创制专项(2009ZX09310-006) （2009ZX09310-006）
上海市纳米专项基金资助项目(0953nm03300). （0953nm03300）
