Qian Chenggen, Chen Yulei, Zhu Sha, Yu Jicheng, Zhang Lei, Feng Peijian, Tang Xin, Hu Quanyin, Sun Wujin, Lu Yue, Xiao Xuanzhong, Shen Qun-Dong, Gu Zhen
1. Department of Polymer Science & Engineering and Key Laboratory of High Performance Polymer Materials & Technology of MOE, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210023, China;; 2. Joint Department of Biomedical Engineering, University of North Carolina at Chapel Hill and North Carolina State University, Raleigh, NC 27695, USA;; 3. Division of Molecular Pharmaceutics and Center for Nanotechnology in Drug Delivery, Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA;
1. Department of Polymer Science & Engineering and Key Laboratory of High Performance Polymer Materials & Technology of MOE, Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210023, China;
Theranostics. 2016 Apr 28;6(7):1053-64. doi: 10.7150/thno.14843. eCollection 2016.
Stimuli-responsive and imaging-guided drug delivery systems hold vast promise for enhancement of therapeutic efficacy. Here we report an adenosine-5'-triphosphate (ATP)-responsive and near-infrared (NIR)-emissive conjugated polymer-based nanocarrier for the controlled release of anticancer drugs and real-time imaging. We demonstrate that the conjugated polymeric nanocarriers functionalized with phenylboronic acid tags on surface as binding sites for ATP could be converted to the water-soluble conjugated polyelectrolytes in an ATP-rich environment, which promotes the disassembly of the drug carrier and subsequent release of the cargo. In vivo studies validate that this formulation exhibits promising capability for inhibition of tumor growth. We also evaluate the metabolism process by monitoring the fluorescence signal of the conjugated polymer through the in vivo NIR imaging.
刺激响应性和成像引导的药物递送系统在提高治疗效果方面具有巨大潜力。在此,我们报告一种基于三磷酸腺苷(ATP)响应性和近红外(NIR)发射共轭聚合物的纳米载体,用于抗癌药物的控释和实时成像。我们证明,表面用苯基硼酸标签功能化作为ATP结合位点的共轭聚合物纳米载体,在富含ATP的环境中可转化为水溶性共轭聚电解质,这促进了药物载体的解体和随后货物的释放。体内研究证实,该制剂在抑制肿瘤生长方面具有良好的能力。我们还通过体内近红外成像监测共轭聚合物的荧光信号来评估代谢过程。