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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.


To prepare 9-nitro-camptothecin (9-NC)-loaded folate-conjugated polymer micelles and investigate its characterization and antituomor activity in vitro.


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.


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% respectively. 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.


Xu JJ, Han X, Ni JM, Lu WY. Characterization and pharmacodynamic evaluation in vitro of 9-nitro-camptothecin-loaded folate-conjugated polymer micelles as tumor-targeted drug delivery system. Zhongguo Zuzhi Gongcheng Yanjiu yu Linchuang Kangfu. 2011;15(51): 9583-9586. [http://www.crter.cn]

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