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Synthesis and characterization of a hyperbranched grafting copolymer PEI-g-PLeu for gene and drug co-delivery

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Abstract

L-Leucine (Leu) is a hydrophobic natural amino acid and can polymerize into poly-L-Leucine (PLeu) to be an excellent biocompatible material. In this paper, a hyperbranched copolymer polyethyleneimine-g-poly-L-leucine (PEI-g-PLeu) was synthesized by ring-opening polymerization with leucine NCA as monomer and PEI as initiator, which will be used as drug and gene co-delivery system for cancer therapy. To characterize the transfection efficiency in vitro, pGL3 as the reporter gene was loaded in PEI-g-PLeu to form complexes. Doxorubicin (DOX) with cis-aconitic anhydride linker (CAD) and calf thymus DNA (as model DNA) were co-loaded in PEI-g-PLeu to obtain PEI-g-PLeu/DNA/CAD nanoparticles to measure Zeta potentials and particle sizes. Lastly, CAD and modified Bc12-shRNA(as therapeutic gene) were co-loaded in PEI-g-PLeu to get PEI-g-PLeu/CAD/DNA complexes. Our finding revealed when PEI and PLeu with the molar ratio of 1:240, and PEI-g-PLeu and DNA with the mass ratio of 1:5, PEI-g-PLeu/CAD/DNA had negligible cytotoxicity with equivalent gene transfaction efficiency compared with PEI25k. As a result, PEI-g-PLeu/CAD/DNA was a promising drug and gene co-delivery system.

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Authors and Affiliations

  1. School of Materials Science and Engineering, Changchun University of Science and Technology, Changchun, 130022, China

    Yanhui Li, Xue Zhang, Jingpeng Zhang, Xin Mu & Qian Duan

  2. Key Laboratory of Polymer Ecomaterials,Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, 130022, China

    Xue Zhang, Jingpeng Zhang, Xin Mu & Huayu Tian

  3. Changchun Chaoyang People’s Hospital, Changchun, 130022, China

    Tinghong Wang

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  1. Yanhui Li
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Correspondence to Yanhui Li or Huayu Tian.

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Li, Y., Zhang, X., Zhang, J. et al. Synthesis and characterization of a hyperbranched grafting copolymer PEI-g-PLeu for gene and drug co-delivery. J Mater Sci: Mater Med 29, 47 (2018). https://doi.org/10.1007/s10856-018-6057-1

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  • DOI: https://doi.org/10.1007/s10856-018-6057-1

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