Research Papers:

Anti-cancer efficacy of biotinylated chitosan nanoparticles in liver cancer

Mingrong Cheng, Weiping Zhu _, Qing Li, Dejian Dai and Yiming Hou

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Oncotarget. 2017; 8:59068-59085. https://doi.org/10.18632/oncotarget.19146

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Mingrong Cheng1,2,*, Weiping Zhu3,5,*, Qing Li4,*, Dejian Dai2 and Yiming Hou5

1Department of General Surgery, Pudong New Area District Zhoupu Hospital, Shanghai 201318, China

2Department of General Surgery, Shanghai Tianyou Hospital, Tongji University, Shanghai 200000, China

3Department of Hepatic Surgery, Fudan University Shanghai Cancer Center, Shanghai Medical College, Fudan University, Shanghai 200032, China

4Department of Medical Clinic, Pujiang Community Health Service Center, Shanghai 201112, China

5Department of General Surgery, Shanghai Fifth People’s Hospital, Fudan University, Shanghai 200240, China

*These authors have contributed equally to this work

Correspondence to:

Weiping Zhu, email: [email protected]

Dejian Dai, email: [email protected]

Keywords: biotin chitosan, curative effect, drug delivery system, liver cancer, nanoparticles

Received: August 08, 2016    Accepted: June 02, 2017    Published: July 10, 2017


The present study investigated the synthesis of biotinylated chitosan (Bio-CS) from chitosan using a nanomaterial skeleton with biotin and the successful targeting of the formulation in liver cancer cells. Bio-CS was validated by fourier transformed infrared spectroscopy and hydrogen-1 nuclear magnetic resonance spectroscopy. Bio-CS and plasmid DNA were used to construct Bio-CS/plasmid DNA nanoparticles according to the optimal molar ratio of 1:1 and the optimal pH-value of 5.5. Under these conditions, the parameters mean particle size, potential, encapsulation rate and drug loading, were 82.9 nm, +21.8 mV, 85.7% and 35.4%, respectively. Bio-CS exhibited an apparent liver cancer targeting effect in vitro and in vivo, as demonstrated by confocal laser scanning, green fluorescent protein transfection, and in vivo imaging assays. In addition, the Bio-CS/plasmid DNA nanoparticles significantly increased the survival period of the orthotropic liver cancer mouse model compared with the plasmid DNA, with no apparent side effects on the cells. Bio-CS nanomaterials stimulated an immune response in hepatoma cells via increased expression of GM-CSF, IL-21 and Rae-1 markers. The data suggest that Bio-CS increased the inhibition of liver cancer cell proliferation in vitro and the activation of the cellular immunity in vivo.

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