Department of Pharmaceutical Technology, Anna University, BIT Campus, Tiruchirappalli 620024, Tamilnadu, India.
Central Leather Research Institute, Council of Scientific and Industrial Research, Adyar, Chennai 20, Tamilnadu, India.
Carbohydr Polym. 2015 Sep 5;128:63-74. doi: 10.1016/j.carbpol.2015.04.010. Epub 2015 Apr 20.
In this study, green synthesis of gold nanoparticles (AuNPs) was achieved using the extract of eggplant as a reducing agent. Hyaluronic acid (HA) serves as a capping and targeting agent. Metformin (MET) was successfully loaded on HA capped AuNPs (H-AuNPs) and this formulation binds easily on the surface of the liver cancer cells. The synthesized nanoparticles were characterized by UV-Vis spectrophotometer, HR-TEM, particle size analyser and zeta potential measurement. Toxicity studies of H-AuNPs in zebra fish confirmed the in vivo safety of the AuNPs. The in vitro cytotoxicity results showed that the amount of MET-H-AuNPs enough to achieve 50% inhibition (IC50) was much lower than free MET. Flow cytometry analysis showed the significant reduction in G2/M phase after treatment with MET-H-AuNPs, and molecular level apoptosis were studied using western blotting. The novelty of this study is the successful synthesis of AuNPs with a higher MET loading and this formulation exhibited better targeted delivery as well as increased regression activity than free MET in HepG2 cells.
在这项研究中，使用茄子提取物作为还原剂实现了金纳米粒子（AuNPs）的绿色合成。透明质酸（HA）作为封端和靶向剂。二甲双胍（MET）成功加载到 HA 封端的 AuNPs（H-AuNPs）上，这种制剂很容易结合到肝癌细胞表面。所合成的纳米粒子通过紫外-可见分光光度计、高分辨率透射电子显微镜、粒度分析仪和zeta 电位测量进行了表征。斑马鱼中的 H-AuNPs 毒性研究证实了 AuNPs 的体内安全性。体外细胞毒性结果表明，达到 50%抑制（IC50）所需的 MET-H-AuNPs 量远低于游离 MET。流式细胞术分析表明，用 MET-H-AuNPs 处理后 G2/M 期明显减少，并用 Western blot 研究了分子水平的细胞凋亡。本研究的新颖之处在于成功合成了具有更高 MET 负载量的 AuNPs，并且该制剂在 HepG2 细胞中表现出比游离 MET 更好的靶向递送以及更高的回归活性。
