Lipid‐Coated Gold Nanoparticles Functionalized by Folic Acid as Gene Vectors for Targeted Gene Delivery in vitro and in vivo

• DOI: 10.1002/cmdc.201700391
• Publication Date: 2017-10-02T02:28:36Z
• Authors: Baoji Du; Xiaoxiao Gu; Xu Han; Guanyu Ding; Yuling Wang; Dan Li; Erkang Wang; Jin Wang
• Keywords: Folate receptor; Lipofectamine

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