文献：225 Ac标记的生物相容性共轭聚合物纳米粒子用于*内放射*

链接：https://www.sciencedirect.com/science/article/abs/pii/S0968089623003656

作者：陈希 建 ，冉熙梁  ，刘伟豪  ，欢 妈 ，白 赤 耀，姚 雄 ，涂 兰 啊，廖嘉丽  ，杨元友  ，杨继军，李菲泽  ，刘宁

摘要：

近年来，基于锕-225（225 Ac）的腔内放射*引起了越来越多的关注，这是因为它的α粒子可以对癌细胞产生*大的杀伤力，同时*大限度地减少对健康组织不必要的辐射影响。在此，我们开发了一种用两亲聚合物DSPE-PEG-DOTA包裹的111 In/ 225 Ac放射性标记的共轭聚合物纳米粒子（CPN），作为核成像引导下的癌症腔内放射*的新型可注射纳米放射性药物。使用111 In-DOTA-PEG-CPN作为纳米探针的单光子发射计算机断层扫描/计算机断层扫描（SPECT/CT）表明放射性标记纳米载体的保留时间延长，这与直接放射分析检查的体内生物分布一致。与接受PBS或DOTA-PEG-CPN*的小鼠相比，接受225 Ac-DOTA-PEG-CPN*的小鼠4T1模型中观察到*生长显著抑制。225 Ac-DOTA-PEG-CPN组在24天内无一例死亡，中位生存期显著延长至35天，而所有接受PBS或DOTA-PEG-CPN*的小鼠均在注射后20天死亡。此外，组织病理学研究表明，225 Ac-DOTA-PEG-CPN*后对健康组织无明显副作用。所有这些结果表明，新型225 Ac标记DOTA-PEG-CPN有望成为腔内放射*的典范。

Abstract

Recently, endoradiotherapy based on actinium-225 (225Ac) has attracted increasing attention, which is due to its α particles can generate maximal damage to cancer cells while minimizing unnecessary radiation effects on healthy tissues. Herein, 111In/225Ac-radiolabeled conjugated polymer nanoparticles (CPNs) coated with amphiphilic polymer DSPE-PEG-DOTA have been developed as a new injectable nano-radiopharmaceuticals for cancer endoradiotherapy under the guidance of nuclear imaging. Single photon emission computed tomography/computed tomography (SPECT/CT) using 111In-DOTA-PEG-CPNs as nano probe indicates a prolonged retention of radiolabeled nanocarriers, which was consistent with the in vivo biodistribution examined by direct radiometry analysis. Significant inhibition of tumor growth has been observed in murine 4T1 models treated with 225Ac-DOTA-PEG-CPNs when compared to mice treated with PBS or DOTA-PEG-CPNs. The 225Ac-DOTA-PEG-CPNs group experienced no single death within 24 days with the median survival considerably extended to 35 days, while all the mice treated with PBS or DOTA-PEG-CPNs died at 20 days post injection. Additionally, the histopathology studies demonstrated no obvious side effects on healthy tissues after treatment with 225Ac-DOTA-PEG-CPNs. All these results reveal that the new 225Ac-labeled DOTA-PEG-CPNs is promising as paradigm for endoradiotherapy.

西安齐岳生物提供相关产品：

DSPE-PEG-CTT2

DSPE-PEG-CPP

DSPE-PEG-octreotide

DSPE-PEG-SP94

DSPE-PEG-CCK8

DSPE-PEG2000-GE11

DSPE-PEG2K-YIGSR

DSPE-PEG2K-RVG29

DSPE-PEG2K-MMPs

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