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Nanoparticles of deoxycholic acid, polyethylene glycol and folic acid-modified chitosan for targeted delivery of doxorubicin

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Abstract

Chitosan (CS) was first modified hydrophobically with deoxycholic acid (DCA) and then with polyethylene glycol (PEG) to obtain a novel amphiphilic polymer (CS–DCA–PEG). This was covalently bound to folic acid (FA) to develop nanoparticles (CS–DCA–PEG–FA) with tumor cell targeting property. The structure of the conjugates was characterised using Fourier transform infrared and 1H nuclear magnetic resonance spectroscopy and X-ray diffraction. Based on self-aggregation, the conjugates formed nanoparticles with a low critical aggregation concentration of 0.035 mg/ml. The anti-cancer drug doxorubicin (DOX) was encapsulated into the nanoparticles with a drug-loading capacity of 30.2 wt%. The mean diameter of the DOX-loaded nanoparticles was about 200 nm, with a narrow size distribution. Transmission electron microscopy images showed that the DOX-loaded nanoparticles were spherical. The drug release was studied under different conditions. Furthermore, the cytotoxic activities of DOX in CS–DCA–PEG–FA nanoparticles against folate receptor (FR)-positive HeLa cells and FR-negative fibroblast 3T3 cells were evaluated. These results suggested that the CS–DCA–PEG–FA nanoparticles may be a promising vehicle for the targeting anticancer drug to tumor cells.

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Acknowledgments

This study is financially supported by the Natural Science Foundation of Guangdong (S2012040008003), Guangzhou Science and Technology Plan Project (No. 11C32070752), the Key Project of DEGP (cxzd1109), the Ph.D. Programs Foundation of Ministry of Education of China and the Fundamental Research Funds for the Central Universities (21612327). This research is financially supported by Guangzhou Science and Technology Plan Project (No. 11C32070752).

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Authors and Affiliations

  1. Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, Jinan University, Guangzhou, 510632, China

    Zhonggen Shi, Rui Guo, Weichang Li, Yi Zhang, Wei Xue, Yu Tang & Yuanming Zhang

  2. Department of Chemistry, Jinan University, Guangzhou, 510632, China

    Zhonggen Shi, Weichang Li, Yu Tang & Yuanming Zhang

  3. Department of Biomedical Engineering, Jinan University, Guangzhou, 510632, China

    Rui Guo, Yi Zhang & Wei Xue

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  1. Zhonggen Shi
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  2. Rui Guo
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  3. Weichang Li
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  4. Yi Zhang
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  5. Wei Xue
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  6. Yu Tang
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  7. Yuanming Zhang
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Correspondence to Rui Guo.

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Shi, Z., Guo, R., Li, W. et al. Nanoparticles of deoxycholic acid, polyethylene glycol and folic acid-modified chitosan for targeted delivery of doxorubicin. J Mater Sci: Mater Med 25, 723–731 (2014). https://doi.org/10.1007/s10856-013-5113-0

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  • DOI: https://doi.org/10.1007/s10856-013-5113-0

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