College of Food and Drug, Luoyang Normal University, Luoyang, China.
Institute of Combined Injury, State Key Laboratory of Trauma, Burns and Combined Injury, Chongqing Engineering Research Center for Nanomedicine, College of Preventive Medicine, Third Military Medical University, Chongqing, China.
J Biomed Mater Res A. 2020 Sep;108(9):1816-1823. doi: 10.1002/jbm.a.36946. Epub 2020 Apr 18.
IR808, an IR780 derivative, is capable of fluorescently imaging and photodynamic therapy in vitro and in vivo. However, its application is greatly hampered by hydrophobicity, toxicity and nonspecific delivery to the targeting tissue and that causes accumulation in the liver and kidney. In order to overcome these limitations, we prepared IR808-PEG-FA from IR808, amino-terminated poly(ethylene glycol) (NH -PEG-NH , denoted as PEG) and folate (FA). PEG, an accepted hydrophilic medicinal agent, was introduced to improve hydrophobicity, and FA was used to increase targeting ability of the conjugate. The obtained product provides a good water solubility and stronger light intensity in near infrared (NIR)-imaging, and CCK-8 test demonstrated which had no appreciable toxicity. In addition, the cell uptake results indicated that IR808-PEG-FA was specifically targeted to positive tumors cells with folate receptor (FR) compared with IR808, and thus it may be used as a novel diagnostic agent or imaging-guided agent for cancer treatment. So this article provides a way to improve hydrophobicity, optical stability and targeting ability in the field of nano-probe for fluorochromes.
IR808 是 IR780 的衍生物，能够在体外和体内进行荧光成像和光动力治疗。然而，由于其疏水性、毒性和对靶向组织的非特异性递送，导致其在肝脏和肾脏中的积累，其应用受到了极大的阻碍。为了克服这些限制，我们从 IR808、氨基末端聚乙二醇（NH 2 -PEG-NH 2 ，表示为 PEG）和叶酸（FA）制备了 IR808-PEG-FA。PEG 是一种公认的亲水性药物，被引入以提高疏水性，FA 被用于增加缀合物的靶向能力。所得产物提供了良好的水溶性和在近红外（NIR）成像中更强的光强度，CCK-8 测试表明其毒性可忽略不计。此外，细胞摄取结果表明，与 IR808 相比，IR808-PEG-FA 特异性靶向具有叶酸受体（FR）的阳性肿瘤细胞，因此它可能被用作癌症治疗的新型诊断剂或成像引导剂。因此，本文为改善荧光染料纳米探针领域的疏水性、光学稳定性和靶向能力提供了一种方法。
