Yang Lily, Mao Hui, Wang Y Andrew, Cao Zehong, Peng Xianghong, Wang Xiaoxia, Duan Hongwei, Ni Chunchun, Yuan Qingan, Adams Gregory, Smith Mark Q, Wood William C, Gao Xiaohu, Nie Shuming
Department of Surgery, Winship Cancer Institute, Emory University School of Medicine, Atlanta, GA 30322, USA.
Small. 2009 Feb;5(2):235-43. doi: 10.1002/smll.200800714.
Epidermal growth factor receptor (EGFR) targeted nanoparticle are developed by conjugating a single-chain anti-EGFR antibody (ScFvEGFR) to surface functionalized quantum dots (QDs) or magnetic iron oxide (IO) nanoparticles. The results show that ScFvEGFR can be successfully conjugated to the nanoparticles, resulting in compact ScFvEGFR nanoparticles that specifically bind to and are internalized by EGFR-expressing cancer cells, thereby producing a fluorescent signal or magnetic resonance imaging (MRI) contrast. In vivo tumor targeting and uptake of the nanoparticles in human cancer cells is demonstrated after systemic delivery of ScFvEGFR-QDs or ScFvEGFR-IO nanoparticles into an orthotopic pancreatic cancer model. Therefore, ScFvEGFR nanoparticles have potential to be used as a molecular-targeted in vivo tumor imaging agent. Efficient internalization of ScFvEGFR nanoparticles into tumor cells after systemic delivery suggests that the EGFR-targeted nanoparticles can also be used for the targeted delivery of therapeutic agents.
通过将单链抗表皮生长因子受体（EGFR）抗体（ScFvEGFR）与表面功能化的量子点（QD）或磁性氧化铁（IO）纳米颗粒偶联，开发出了表皮生长因子受体（EGFR）靶向纳米颗粒。结果表明，ScFvEGFR能够成功地与纳米颗粒偶联，形成紧密的ScFvEGFR纳米颗粒，该纳米颗粒能特异性结合表达EGFR的癌细胞并被其内化，从而产生荧光信号或磁共振成像（MRI）对比。将ScFvEGFR-QD或ScFvEGFR-IO纳米颗粒全身递送至原位胰腺癌模型后，证明了纳米颗粒在体内对人癌细胞的肿瘤靶向性和摄取。因此，ScFvEGFR纳米颗粒有潜力用作分子靶向体内肿瘤成像剂。全身递送后ScFvEGFR纳米颗粒高效内化进入肿瘤细胞，这表明EGFR靶向纳米颗粒也可用于治疗剂的靶向递送。
