Biotinylated Cyclen-Contained Cationic Lipids as Non-Viral Gene Delivery Vectors

Authors

  • Qiang Liu,

    1. Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu, China
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  • Wen-Jing Yi,

    1. Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu, China
    2. Laboratory of Genome Stability, Development and Stem Cell Institute, The West China Second Hospital, Sichuan University, Chengdu, China
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  • Yi-Mei Zhang,

    1. Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu, China
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  • Ji Zhang,

    1. Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu, China
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  • Liandi Guo,

    1. Laboratory of Genome Stability, Development and Stem Cell Institute, The West China Second Hospital, Sichuan University, Chengdu, China
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  • Xiao-Qi Yu

    Corresponding author
    1. Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu, China
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Abstract

A series of 1, 4, 7, 10-tetraazacyclododecane (cyclen)-based cationic lipids, namely 5a–c bearing a biotin moiety and a variety of end groups (cholesterol, diosgenin, and α-tocopherol) via biodegradable carbamate bond linkage were prepared and applied as non-viral gene delivery vectors. The liposomes formed from 5 and dioleoylphosphatidylethanolamine could bind and condense plasmid DNA into nanoparticles with appropriate size and zeta potentials. All biotinylated cyclen cationic lipids showed higher cell viability than commercially available lipofectamine 2000 even at high N/P ratios, while their transfection efficiency was relatively lower. Further, results indicate that among the three lipids, α-tocopherol-containing compound 5c has higher DNA-binding ability, lower cytotoxicity, and higher transfection efficiency. Transfection in two different cell lines revealed that these lipoplexes have higher gene delivery efficiency toward tumor cells.

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