Octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles as potential carriers for targeted antitumor drug delivery

Zou Aifeng; Meirong Huo; Yong Zhang; Jianping Zhou; Xiaoqiang Yin; Chengli Yao; Qinnv Zhu

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Octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles as potential carriers for targeted antitumor drug delivery

Zou Aifeng ,Meirong Huo * #,Yong Zhang,Jianping Zhou,Xiaoqiang Yin,Chengli Yao,Qinnv Zhu

Department of Pharmaceutics, China Pharmaceutical University

*Correspondence author

#Submitted by

Subject:

Funding: Specialized Research Fund for the Doctoral Program of Higher Education of China （No.No.200803161017）, Key New Drug Innovation Project from the Ministry of Science and Technology of the People’s Republic of China （No.No.2009ZX09310004）

Opened online:13 October 2011

Accepted by: none

Citation: Zou Aifeng ,Meirong Huo,Yong Zhang.Octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles as potential carriers for targeted antitumor drug delivery[OL]. [13 October 2011] http://en.paper.edu.cn/en_releasepaper/content/4444776

Octreotide (OCT) was recently found to have high binding affinity to the positive tumor cells of somatostatin receptors (SSTRs). In this study, octreotide-polyethene glycol-stearic acid (OCT-Phe-PEG-SA) was first successfully synthesized and used as a targeting molecule for N-octyl-O, N-carboxymethyl chitosan (OCC). Doxorubicin (DOX) was loaded into OCT-modified OCC micelles (DOX-OCC-OCT). The drug-loaded micelles obtained exhibited spherical shape, small particle sizes and negative zeta potentials. The cytotoxicity of DOX-OCC-OCT micelles against MCF-7 cells (SSTRs expressing) was found to significantly increase with the increased amount of OCT modification, while no significant difference was observed against WI-38 cells (no SSTRs expressing). Results of flow cytometry, fluorescence microscopy and confocal laser scanning microscopy confirmed DOX-OCC-OCT micelles could remarkably increase the uptake of DOX in MCF-7 cells. All the results indicated that OCC-OCT micelles may be a promising intracellular targeting carrier for efficient delivery of antitumor drugs into tumor cells.

Keywords:Chitosan; Polymeric drug delivery system; Drug targeting; Micelle; Cancer chemotherapy

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