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I- 标记的聚乙烯亚胺包埋金纳米粒子用于靶向肿瘤 SPECT/CT 成像和放射性核素治疗。

I-labeled polyethylenimine-entrapped gold nanoparticles for targeted tumor SPECT/CT imaging and radionuclide therapy.

机构信息

Department of Nuclear Medicine, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200080, People's Republic of China.

State Key Laboratory of Material-Oriented Chemical Engineering, School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing 211816, People's Republic of China.

出版信息

Int J Nanomedicine. 2019 Jun 11;14:4367-4381. doi: 10.2147/IJN.S203259. eCollection 2019.

DOI:10.2147/IJN.S203259
PMID:31354266
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6580422/
Abstract

Polyethylenimine (PEI) has been widely used as a versatile template to develop multifunctional nanosystems for disease diagnosis and treatment. In this study, we manufactured iodine-131 (I)-labeled PEI-entrapped gold nanoparticles (Au PENPs) as a novel nanoprobe for single-photon emission computed tomography/computed tomography (SPECT/CT) imaging and radionuclide therapy. PEI was PEGylated and sequentially conjugated with Buthus martensii Karsch chlorotoxin (BmK CT, a tumor-specific ligand which can selectively bind to MMP2), 3-(4'-hydroxyphenyl)propionic acid-OSu (HPAO), and fluorescein isothiocyanate to form the multifunctional PEI template for entrapment of Au NPs. Then, the PEI surface was radiolabeled with I via HPAO to produce the novel nanoprobe (BmK CT-Au PENPs-I). The synthesized multifunctional Au PENPs before and after I radiolabeling were well-characterized as follows: structure, X-ray attenuation coefficient, colloid stability, cytocompatibility, and radiochemical stability in vitro. Furthermore, BmK CT-Au PENPs-I were suitable for targeted SPECT/CT imaging and radionuclide therapy of tumor cells in vitro and in a xenograft tumor model in vivo. The developed multifunctional Au PENPs are a promising theranostic platform for targeted imaging and treatment of different MMP2-overexpressing tumors.

摘要

聚乙烯亚胺（PEI）已被广泛用作开发用于疾病诊断和治疗的多功能纳米系统的通用模板。在这项研究中，我们制造了碘-131（I）标记的聚乙烯亚胺包埋的金纳米颗粒（Au PENPs）作为用于单光子发射计算机断层扫描/计算机断层扫描（SPECT/CT）成像和放射性核素治疗的新型纳米探针。PEI 被聚乙二醇化，并依次与蝎子毒素（BmK CT，一种可以选择性结合 MMP2 的肿瘤特异性配体）、3-（4'-羟基苯基）丙酸-OSu（HPAO）和异硫氰酸荧光素缀合，形成用于包封 Au NPs 的多功能 PEI 模板。然后，通过 HPAO 将 PEI 表面放射性标记 I，以产生新型纳米探针（BmK CT-Au PENPs-I）。合成的多功能 Au PENPs 在进行 I 放射性标记前后均具有以下特征：结构、X 射线衰减系数、胶体稳定性、细胞相容性和体外放射化学稳定性。此外，BmK CT-Au PENPs-I 适用于体外肿瘤细胞的靶向 SPECT/CT 成像和放射性核素治疗以及体内异种移植肿瘤模型。开发的多功能 Au PENPs 是一种有前途的治疗诊断平台，可用于靶向成像和治疗不同 MMP2 过表达的肿瘤。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/f10f79f89359/IJN-14-4367-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/2cd77711e7bb/IJN-14-4367-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/81744be3f3c6/IJN-14-4367-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/e73e1a1c5561/IJN-14-4367-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/763db7505f9d/IJN-14-4367-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/49f364f75c4f/IJN-14-4367-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/3941ddf6f938/IJN-14-4367-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/f10f79f89359/IJN-14-4367-g0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/2cd77711e7bb/IJN-14-4367-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/81744be3f3c6/IJN-14-4367-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/e73e1a1c5561/IJN-14-4367-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/763db7505f9d/IJN-14-4367-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/49f364f75c4f/IJN-14-4367-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/3941ddf6f938/IJN-14-4367-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d77/6580422/f10f79f89359/IJN-14-4367-g0007.jpg

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