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Original Research

Antitumor activity of folate-targeted, paclitaxelloaded polymeric micelles on a human esophageal EC9706 cancer cell line

, , , , , , , , & show all
Pages 3487-3502 | Published online: 06 Jul 2012
 

Abstract

Background

Esophageal cancer is recognized as one of the most refractory pernicious diseases. In addition, it is an aggressive malignancy with a propensity for local progression and distant dissemination. Because of the poor long-term prognosis for patients with esophageal cancer, increasing attention has focused on the integration of targeted agents into current therapeutics. Nevertheless, there have been few studies reported concerning the therapeutic efficacy of paclitaxel-conjugated polymeric micelles in human esophageal cancer in vivo. Therefore, the aim of this research was to investigate the tumor inhibition effect of composite micelles containing folic acid and paclitaxel on the human esophageal EC9706 cancer cell line.

Methods and results

Intravenous administration of folate-targeted, paclitaxel-loaded micelles was demonstrated to be more efficient in inhibiting subcutaneous xenograft tumors and extending the survival rate of tumor-bearing nude mice than free paclitaxel and plain paclitaxel micelles at an equivalent paclitaxel dose of 20 mg/kg, which was further backed up by flow cytometry, TUNEL, and expression of apoptosis-related proteins, including Bax, Bcl2, and caspase 3 in this study.

Conclusion

The folate-mediated paclitaxel-loaded polymeric micelle is a promising agent for the treatment of human esophageal cancer.

Acknowledgments

The authors acknowledge the financial support of the National Natural Science Foundation of China (20674084, 21004062, 51103148) and the Ministry of Science and Technology of China (973 Project 2009CB930102, 863 Project 2007AA03Z535).

Disclosure

The authors report no conflict of interest in this work.

Suplementary table

Table S1 Characteristics of M(PTX) and FA-M(PTX)