Octreotide-modified N-octyl-O, N-carboxymethyl chitosan micelles as potential carriers for targeted antitumor drug delivery
✍ Scribed by Aifeng Zou; Meirong Huo; Yong Zhang; Jianping Zhou; Xiaoqiang Yin; Chengli Yao; Qinnv Zhu; Min Zhang; Jinshan Ren; Qiang Zhang
- Publisher
- John Wiley and Sons
- Year
- 2012
- Tongue
- English
- Weight
- 654 KB
- Volume
- 101
- Category
- Article
- ISSN
- 0022-3549
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✦ Synopsis
Octreotide (OCT) was recently found to have high binding affinity to the positive tumor cells of somatostatin receptors (SSTRs). In this study, octreotide-Phe-polyethylene glycol-stearic acid 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, whereas no significant difference was observed against WI-38 cells (no SSTRs expressing). Results of flow cytometry, fluorescence microscopy, and confocal laser scanning microscopy confirmed that 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.