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首页> 外文期刊>Journal of industrial and engineering chemistry >Cyclic RGDfK- and Sulfo-Cy5.5-functionalized mPEG-PCL theranostic nanosystems for hepatocellular carcinoma
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Cyclic RGDfK- and Sulfo-Cy5.5-functionalized mPEG-PCL theranostic nanosystems for hepatocellular carcinoma

机译：循环RGDFK-和磺酸硫化的MPEG-PCL Theranostic纳米系统用于肝细胞癌

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Sorafenib (SF) is a standard, clinically-recognized therapy for treating hepatocellular carcinoma (HCC) patients. However, as a multikinase inhibitor, SF causes a systemic side effect. Therefore, there is an urgent need to selectively deliver the optimum dose of SF to the tumor site. The present study aimed to selectively target SF to HCC using a biocompatible drug carrier to increase the therapeutic efficacy, in turn, minimize the adverse effects. To this end, methoxy polyethylene glycol-polycaprolactone (mPEG-PCL) di-block copolymer was selected as an amphiphilic carrier for SF that hydrophobic PCL core can encapsulate SF through self-assembly. Cyclic RGDfK (cRGD) was conjugated to the end of PEG-PCL (cRGD-PEG-PCL) for HCC targeting. Sulfo-Cyanine5.5 (S-Cy5.5) was also incorporated to PEG-PCL (S-Cy5.5-PEG-PCL) for near-infrared fluorescence (NIRF) imaging. The composition, morphology and size distribution of nanoparticles (NPs) were characterized by H-1 NMR, transmission electron microscopy (TEM) and dynamic light scattering (DLS), respectively. In addition, the ability of the integrin-mediated targeting of NPs for the selective delivery of SF was systemically investigated with Hep3B cell line and a nude mouse xenograft model. Consequently, it was found that S-Cy5.5-cRGD-PEG-PCL leads to the selective accumulation of SF into the tumor site and improve anticancer activity against HCC. (C) 2021 The Korean Society of Industrial and Engineering Chemistry. Published by Elsevier B.V. All rights reserved.
机译：索拉非尼（SF）是一种标准的、临床公认的治疗肝细胞癌（HCC）患者的疗法。然而，作为一种多激酶抑制剂，SF会引起全身副作用。因此，迫切需要选择性地将最佳剂量的SF输送到肿瘤部位。本研究旨在使用生物相容性药物载体选择性地将SF靶向HCC，以提高治疗效果，进而将不良反应降至最低。为此，选择甲氧基聚乙二醇-聚己内酯（mPEG-PCL）双嵌段共聚物作为SF的两亲性载体，疏水性PCL核可以通过自组装来封装SF。环RGDfK（cRGD）与PEG-PCL（cRGD-PEG-PCL）末端结合用于HCC靶向。磺基氰5。5（S-Cy5.5）也被并入PEG-PCL（S-Cy5.5-PEG-PCL）中用于近红外荧光（NIRF）成像。分别用H-1核磁共振、透射电镜和动态光散射对纳米颗粒的组成、形貌和尺寸分布进行了表征。此外，利用Hep3B细胞系和裸鼠异种移植模型系统研究了整合素介导的靶向NPs选择性递送SF的能力。因此，发现S-Cy5。5-cRGD-PEG-PCL导致SF选择性积聚到肿瘤部位，并提高抗肝癌活性。（2021）韩国工业和工程化学学会。由爱思唯尔B.V.出版。版权所有。

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