Department of pharmaceutics, PSG College of Pharmacy, Coimbatore 641 004, Tamil Nadu, India, Affiliated to TN Dr. M.G.R Medical University, Guindy, Chennai 600032, Tamil Nadu, India.
Department of pharmacology, PSG College of Pharmacy, Coimbatore 641 004, Tamil Nadu, India.
Curr Pharm Des. 2020;26(26):3141-3146. doi: 10.2174/1381612826666200316143239.
Silver nanoparticles (AgNPs) have attracted considerable interest in the medical industry due to their physicochemical properties, small size, and surface plasmon behavior. Their smaller particle size and instability in blood circulation leads to toxicity due to its aggregation as Ag+ ions and accumulation at the deepseated organ. In the present study, we aimed at reducing the toxicity of AgNPs by conjugation with an anticancer drug GEM and to improve their internalization through folate receptors-mediated endocytosis by capping the nanoparticles with folic acid (FA).
One-pot facile synthesis of FA capped silver nanoparticles (FA-AgNPs) has been achieved by using FA as a reducing agent. FA-AgNPs were mixed with Gemcitabine (GEM) to obtain tethered FA-GEM-AgNPs. Nanoparticles were characterized by Dynamic Light Scattering (DLS), UV-Visible spectroscopy, Transmission Electron Microscopy (TEM), Energy Dispersive X-ray Analysis (EDAX), Selected Area Electron Diffraction (SAED), and Atomic Absorption Spectroscopy (AAS). The 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was carried out to determine the cytotoxic effect of the prepared nanoformulations. The apoptotic cell death induced by FA-GEM-AgNPs in breast cancer cells were monitored with Acridine orange (AO)/Ethidium Bromide (EtBr) staining.
Compared to GEM and AgNPs, FA-GEM-AgNPs showed enhanced cytotoxic effect and internalization in MDA-MB-453 breast cancer cell line. FA-GEM-AgNPs could be an ideal candidate for targeting cancer cells via folate receptor-mediated endocytosis.
由于其物理化学性质、小尺寸和表面等离子体行为,银纳米粒子(AgNPs)在医学领域引起了相当大的兴趣。由于其在血液循环中的小颗粒尺寸和不稳定性,导致其聚集为 Ag+离子并在深部器官中积累,从而产生毒性。在本研究中,我们旨在通过与抗癌药物吉西他滨(GEM)结合来降低 AgNPs 的毒性,并通过叶酸受体介导的内吞作用将纳米颗粒用叶酸(FA)封端来提高其内化作用。
通过使用 FA 作为还原剂,一锅简便地合成了 FA 封端的银纳米粒子(FA-AgNPs)。将 FA-AgNPs 与 Gemcitabine(GEM)混合以获得键合的 FA-GEM-AgNPs。通过动态光散射(DLS)、紫外可见光谱、透射电子显微镜(TEM)、能量色散 X 射线分析(EDAX)、选区电子衍射(SAED)和原子吸收光谱(AAS)对纳米粒子进行了表征。通过 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐(MTT)测定法测定了制备的纳米制剂的细胞毒性作用。通过吖啶橙(AO)/溴化乙锭(EtBr)染色监测 FA-GEM-AgNPs 在乳腺癌细胞中诱导的凋亡细胞死亡。
与 GEM 和 AgNPs 相比,FA-GEM-AgNPs 在 MDA-MB-453 乳腺癌细胞系中显示出增强的细胞毒性作用和内化作用。FA-GEM-AgNPs 可能是通过叶酸受体介导的内吞作用靶向癌细胞的理想候选物。