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A Potential Targeting Gene Vector Based on Biotinylated Polyethyleneimine/Avidin Bioconjugates

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Abstract

Purpose

To improve the gene delivery efficiency and safety of non-viral vector in liver cells, avidin, which exhibited good biocompatibility and remarkable accumulation in liver, was bioconjugated with biotinylated polyethylenimine to obtain a novel gene vector.

Materials and methods

Biotinylated polyethyleneimine/avidin bioconjugate (ABP) was synthesized through grafting biotin to high molecular weight branched polyethylenimine (PEI, 25 kDa) and then bioconjugating with avidin by the biotin-avidin interaction. Physiochemical characteristics of ABP/pDNA complexes were analyzed, and in vitro cytotoxicity and transfection of ABP were also evaluated in HepG2, Hela and 293 T cells by using 25 kDa PEI as the control.

Results

It was found that ABP was able to condense pDNA efficiently at N/P ratio of 4. The particle sizes of ABP/pDNA complexes were less than 220 nm, and the average surface charges were around 27 mV at the N/P ratio ranging from 2 to 60. Among three different cell lines, ABP and its DNA complexes demonstrated much lower cytotoxicity and higher transfection efficacy in HepG2 cells as compared with 25 kDa PEI.

Conclusion

ABP presented higher transfection efficacy and safety in HepG2 cells due to the biocompatibility of avidin and the specific interactions between avidin and HepG2 cells.

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Acknowledgement

Acknowledgement is made to National Natural Science Foundation of China (50633020), National Key Basic Research Program of China (2005CB623903) and Ministry of Education of China (Cultivation Fund of Key Scientific and Technical Innovation, Project 707043).

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Authors and Affiliations

  1. Key Laboratory of Biomedical Polymers of Ministry of Education & Department of Chemistry, Wuhan University, Wuhan, 430072, People’s Republic of China

    Xuan Zeng, Yun-Xia Sun, Xian-Zheng Zhang, Si-Xue Cheng & Ren-Xi Zhuo

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  1. Xuan Zeng
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  2. Yun-Xia Sun
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  3. Xian-Zheng Zhang
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  4. Si-Xue Cheng
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  5. Ren-Xi Zhuo
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Correspondence to Xian-Zheng Zhang or Ren-Xi Zhuo.

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Zeng, X., Sun, YX., Zhang, XZ. et al. A Potential Targeting Gene Vector Based on Biotinylated Polyethyleneimine/Avidin Bioconjugates. Pharm Res 26, 1931–1941 (2009). https://doi.org/10.1007/s11095-009-9920-4

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  • DOI: https://doi.org/10.1007/s11095-009-9920-4

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