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Decreasing acute toxicity and suppressing colorectal carcinoma using Sorafenib-loaded nanoparticles

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journal contribution
posted on 03.02.2020 by Ningxi Li, Yan Chen, Huimin Sun, Tingwenli Huang, Tianyu Chen, Yichun Jiang, Qian Yang, Xiaoyan Yan, Min Wu

Objective: A polymer-based nanoparticle was constructed to target sorafenib delivery to colorectal carcinoma cells and decrease the side effects of the drug.

Methods: Sorafenib-loaded nanoparticles (S-NPs) based on PEG-PLGA were prepared using a double emulsion solvent evaporation method. The properties of S-NPs were evaluated and then their effects on the viability of colorectal cancer cells and normal human cells were assessed. The mechanism of S-NP internalization was explored using cellular uptake assays and in vitro fluorescence confocal imaging. Acute toxicity of sorafenib on its own or within S-NPs was assessed in mice.

Results: S-NPs showed high drug loading and entrapment efficiencies, they did not cause extensive hemolysis, and they efficiently inhibited growth of colorectal cancer cell lines and human umbilical vein endothelial cells. S-NPs showed lower acute toxicity than the free drug.

Conclusions: Loading sorafenib into nanoparticles can enhance its uptake by colorectal cancer cells and decrease its acute toxicity.


This work was supported by the Hospital Independently Funded Project of Sichuan [CYFY16DL-01], Chengdu Medical University [CYCG17-01], Cadre Health Care Research Project of Sichuan [2019-801], and the Zambon Pharmaceutical Scientific Research Foundation of the Chengdu Pharmaceutical Association [201905].