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Both FA- and mPEG-conjugated chitosan nanoparticles for targeted cellular uptake and enhanced tumor tissue distribution

Zhenqing Hou1, Chuanming Zhan1, Qiwei Jiang1, Quan Hu1, Le Li1, Di Chang1, Xiangrui Yang1, Yixiao Wang1, Yang Li1, Shefang Ye1, Liya Xie2*, Yunfeng Yi3* and Qiqing Zhang14

Author Affiliations

1 Research Center of Biomedical Engineering, Material College, Xiamen University, Xiamen 361005, China

2 First Hospital, Xiamen University, Xiamen, 361003, China

3 Southeast Hospital, Xiamen University, Zhangzhou, 363000, China

4 Tianjin Key Laboratory of Biomedical Materials, Tianjin 300192, China

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Nanoscale Research Letters 2011, 6:563  doi:10.1186/1556-276X-6-563

Published: 25 October 2011


Both folic acid (FA)- and methoxypoly(ethylene glycol) (mPEG)-conjugated chitosan nanoparticles (NPs) had been designed for targeted and prolong anticancer drug delivery system. The chitosan NPs were prepared with combination of ionic gelation and chemical cross-linking method, followed by conjugation with both FA and mPEG, respectively. FA-mPEG-NPs were compared with either NPs or mPEG-/FA-NPs in terms of their size, targeting cellular efficiency and tumor tissue distribution. The specificity of the mPEG-FA-NPs targeting cancerous cells was demonstrated by comparative intracellular uptake of NPs and mPEG-/FA-NPs by human adenocarcinoma HeLa cells. Mitomycin C (MMC), as a model drug, was loaded to the mPEG-FA-NPs. Results show that the chitosan NPs presented a narrow-size distribution with an average diameter about 200 nm regardless of the type of functional group. In addition, MMC was easily loaded to the mPEG-FA-NPs with drug-loading content of 9.1%, and the drug releases were biphasic with an initial burst release, followed by a subsequent slower release. Laser confocal scanning imaging proved that both mPEG-FA-NPs and FA-NPs could greatly enhance uptake by HeLa cells. In vivo animal experiments, using a nude mice xenograft model, demonstrated that an increased amount of mPEG-FA-NPs or FA-NPs were accumulated in the tumor tissue relative to the mPEG-NPs or NPs alone. These results suggest that both FA- and mPEG-conjugated chitosan NPs are potentially prolonged drug delivery system for tumor cell-selective targeting treatments.

chitosan; nanoparticles; drug delivery; mitomycin C