ChemMedChem
ChemMedChem
5 years ago

Lipid-coated gold nanoparticles functionalized by folic acid as gene vector for targeted gene delivery in vitro and in vivo

Yuling Wang, Baoji Du, Dan Li, Erkang Wang, Jin Wang, Xiaoxiao Gu, Guanyu Ding, Xu Han
Lipid-based nanoparticles as gene vectors attracted considerable attention for their high gene transfection efficiency and low cell toxicity. In our previous work, we have synthesized gold nanoparticles/dimethyldioctadecylammonium bromide (DODAB)/dioleoylphosphatidylethanolamine (DOPE) (GDD) as anionic lipid- and pH-sensitive gene vector. To further realize the targeted gene transfection, a series of gold nanoparticles/DODAB/DOPE/DOPE-folic acid (DOPE-FA) with different ratios of DOPE-FA were prepared and named as GDD-FA. The gene transfection efficiency mediated by GDD-FA (2.5%) can reach to about 85% for MCF-7 (FA receptor-positive cell), higher than those of negative control (GDD, 35%) and positive control (Lipofectamine 2000, 65%). However, the GDD-FA (2.5%) cannot further promote the gene transfection in A549 (FA receptor-negative cell). The higher gene transfection efficiency for MCF-7 can be attributed to the enhanced cellular uptake efficiency mediated by the FA target ability. Furthermore, the GDD-FA (2.5%) was also accumulated at the specific tumor site and showed the enhanced gene delivery ability in vivo. In addition, there was no significant harm for main tissues of the mice after treated by GDD-FA (2.5%). Therefore, the GDD-FA (2.5%) with the target ability and improved transfection efficiency facilitates its usability in gene therapy for the tumor cells overexpressing FA receptors. We believe this study will find more broad applications in gene therapy.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/cmdc.201700391

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