Lipid-coated gold nanoparticles functionalized by folic acid as gene vectors for targeted gene delivery invitro and invivo

Baoji Du, Xiaoxiao Gu, Xu Han, Guanyu Ding, Yuling Wang, Dan Li*, Erkang Wang, Jin Wang

*Corresponding author for this work

    Research output: Contribution to journalArticlepeer-review

    29 Citations (Scopus)

    Abstract

    Lipid-based nanoparticles as gene vectors have attracted considerable attention for their high gene transfection efficiency and low cytotoxicity. In our previous work, we synthesized gold nanoparticles/dimethyldioctadecylammonium bromide (DODAB)/dioleoylphosphatidylethanolamine (DOPE) (GDD) as anionic lipid- and pH-sensitive gene vectors. To further realize targeted gene transfection, a series of gold nanoparticles/DODAB/DOPE/DOPE-folic acid (DOPE-FA) with various ratios of DOPE-FA were prepared and termed as GFn (for which n=1.0, 2.5, 5.0, 7.5, or 10.0%). The gene transfection efficiency mediated by GF2.5 can reach about 85% for MCF-7 (FA-receptor-positive cells), higher than those of the negative control (GDD, 35%) and positive control (Lipofectamine 2000, 65%). However, GF2.5 does not further promote gene transfection into A549 (FA-receptor-negative cells). The higher gene transfection efficiency for MCF-7 cells can be attributed to enhanced cellular uptake efficiency mediated by the FA targeting ability. Furthermore, GF2.5 was also found to accumulate at the specific tumor site and showed enhanced invivo gene delivery ability. In addition, no significant harm was observed for the main tissues of the mice after treatment with GF2.5. Therefore, GF2.5, with the targeting ability and improved transfection efficiency, shows promise for its utility in gene therapy for tumor cells that overexpress FA receptors. We believe the results of this study will find more broad applications in gene therapy.

    Original languageEnglish
    Pages (from-to)1768–1775
    Number of pages8
    JournalChemMedChem
    Volume12
    Issue number21
    Early online date12 Oct 2017
    DOIs
    Publication statusPublished - 8 Nov 2017

    Keywords

    • Folic acid
    • Gene vectors
    • Gold nanoparticles
    • Liposomes
    • Targeted gene transfection
    • targeted gene transfection
    • gold nanoparticles
    • liposomes
    • folic acid
    • gene vectors

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