Chinese Journal of Tissue Engineering Research ›› 2011, Vol. 15 ›› Issue (51): 9583-9586.doi: 10.3969/j.issn.1673-8225.2011.51.020

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Characterization and pharmacodynamic evaluation in vitro of 9-nitro-camptothecin-loaded folate-conjugated polymer micelles as tumor-targeted drug delivery system

Xu Jin-jun1, Han Xue2, Ni Jing-man1, Lu Wei-yue2   

  1. 1Institute of Pharmacy, Pharmaceutical School of Lanzhou University, Lanzhou  730000, Gansu Province, China
    2Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai  201203, China
  • Received:2011-05-10 Revised:2011-07-14 Online:2011-12-17 Published:2011-12-17
  • Contact: Ni Jing-man, Doctor, Professor, Institute of Pharmacy, Pharmaceutical School of Lanzhou University, Lanzhou 730000, Gansu Province, China lynjm2004@hotmail.com Correspondence to: Lu Wei-yue, Professor, Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 201203, China wylu@shmu.edu.cn
  • About author:Xu Jin-jun★, Studying for master’s degree, Institute of Pharmacy, Pharmaceutical School of Lanzhou University, Lanzhou 730000, Gansu Province, China xjj619@gmail.com
  • Supported by:

    China Ministry of Science and Technology under Contract, No. 2010CB934000*; Program of National Key New Drug Creation, No. 2009ZX09310-006*; Shanghai Nanotechnology Program, No. 0953nm03300*

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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.

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