Wang Dongxin, Li Yingqi, Tian Zhimei, Cao Ruixia, Yang Binsheng
Key Laboratory of Chemical Biology & Molecular Engineering of Ministry of Education, Institute of Molecular Science, Shanxi University, Taiyuan, 030006, PR China.
Ther Deliv. 2014 May;5(5):511-24. doi: 10.4155/tde.14.17.
PEGylated fluorescent nanodiamond (FND) conjugated with Tf (FND-PEG-Tf) was investigated for targeted drug delivery.
MATERIALS & METHODS: Human hepatoma (HepG2) and normal (L-02) cell lines were used to investigate the difference in cellular uptake of FND-PEG-Tf and its loading drug system. Nanoparticle uptake was evaluated by flow cytometry and laser scanning confocal microscopy.
FND-PEG-Tf showed highly specific TfR-mediated uptake by HepG2 cells, relative to negative controls (L-02 cell), which was a strong correlation among TfR density on the cell surface. The mechanism of TfR-mediated uptake was attested by free Tf with Fe³⁺ as a competitive agent. The difference in cell viability between L-02 and HepG2 cells treated with doxorubicin hydrochloride (DOX) nanoparticles (FND-PEG-Tf-DOX) can be explained by FND-PEG-Tf, which can target drug delivery to cancer cells.
FND-PEG-Tf can potentially be utilized in targeted cancer cell imaging and effective drug delivery for cancer therapy.
研究与转铁蛋白（Tf）偶联的聚乙二醇化荧光纳米金刚石（FND）（FND-PEG-Tf）用于靶向给药。
用人肝癌（HepG2）细胞系和正常（L-02）细胞系研究FND-PEG-Tf及其载药系统在细胞摄取方面的差异。通过流式细胞术和激光扫描共聚焦显微镜评估纳米颗粒的摄取情况。
相对于阴性对照（L-02细胞），FND-PEG-Tf显示出由HepG2细胞高度特异性介导的转铁蛋白受体（TfR）摄取，这与细胞表面TfR密度之间存在强相关性。以游离Tf与Fe³⁺作为竞争剂证实了TfR介导摄取的机制。用盐酸阿霉素（DOX）纳米颗粒（FND-PEG-Tf-DOX）处理的L-02细胞和HepG2细胞之间的细胞活力差异可以用FND-PEG-Tf来解释，它可以将药物靶向递送至癌细胞。
FND-PEG-Tf有可能用于靶向癌细胞成像以及癌症治疗的有效给药。
