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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% 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.

RESULTS AND CONCLUSION:

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.cnhttp://en.zglckf.com]

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