Theranostic nanoparticles are integrated systems useful for simultaneous diagnosis and imaging guided delivery of therapeutic drugs, with wide ranging potential applications in the clinic. Here we developed a theranostic nanoparticle (~ 24 nm size by dynamic light scattering) p-FE-PTX-FA based on polymeric micelle encapsulating an organic dye (FE) fluorescing in the 1,000-1,700 nm second near-infrared (NIR-II) window and an anti-cancer drug paclitaxel. Folic acid (FA) was conjugated to the nanoparticles to afford specific binding to molecular folate receptors on murine breast cancer 4T1 tumor cells. In vivo, the nanoparticles accumulated in 4T1 tumor through both passive and active targeting effect. Under an 808 nm laser excitation, fluorescence detection above 1,300 nm afforded a large Stokes shift, allowing targeted molecular imaging tumor with high signal to background ratios, reaching a high tumor to normal tissue signal ratio (T/NT) of (20.0 ± 2.3). Further, 4T1 tumors on mice were completed eradicated by paclitaxel released from p-FE-PTA-FA within 20 days of the first injection. Pharmacokinetics and histology studies indicated p-FE-PTX-FA had no obvious toxic side effects to major organs. This represented the first NIR-II theranostic agent developed.

中文翻译：

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第二种近红外窗口中的肿瘤治疗剂，用于癌症治疗和成像。

Theranostic纳米颗粒是集成系统，可用于同时诊断和指导治疗药物的成像引导，在临床上具有广泛的潜在应用。在这里，我们基于聚合物胶束开发了一种治疗型纳米颗粒（通过动态光散射可达到约24 nm的尺寸）p-FE-PTX-FA，该聚合物胶束在1,000-1,700 nm的第二个近红外（NIR-II）中发出了荧光的有机染料（FE）。窗口和抗癌药紫杉醇。将叶酸（FA）偶联到纳米颗粒上，以提供与鼠类乳腺癌4T1肿瘤细胞上的分子叶酸受体的特异性结合。在体内，纳米颗粒通过被动和主动靶向作用在4T1肿瘤中积累。在808 nm激光激发下，在1,300 nm以上的荧光检测提供了较大的斯托克斯位移，可以使靶向分子成像的肿瘤具有高的信噪比，达到（20.0±2.3）的高肿瘤与正常组织信号比（T / NT）。此外，在第一次注射后的20天内，通过从p-FE-PTA-FA释放的紫杉醇根除了小鼠的4T1肿瘤。药代动力学和组织学研究表明，p-FE-PTX-FA对主要器官没有明显的毒副作用。这代表了第一个开发的NIR-II治疗试剂。