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Tc-PLA/PVA/Atezolizumab 纳米粒用于非小细胞肺癌诊断的生物分布。

Biodistribution of Tc-PLA/PVA/Atezolizumab nanoparticles for non-small cell lung cancer diagnosis.

机构信息

Ege University, Faculty of Pharmacy, Department of Radiopharmacy, 35040 Bornova, Izmir, Turkey.

Brazilian Nuclear Energy Commission, Nuclear Engineering Institute, Laboratory of Synthesis of Novel Radiopharmaceuticals and Nanoradiopharmacy, Rio de Janeiro 21941906, Brazil; Zona Oeste State University, Laboratory of Nanoradiopharmaceuticals and Radiopharmacy, Rio de Janeiro 23070200, Brazil.

出版信息

Eur J Pharm Biopharm. 2022 Jul;176:21-31. doi: 10.1016/j.ejpb.2022.05.006. Epub 2022 May 11.

DOI:10.1016/j.ejpb.2022.05.006
PMID:35568255
Abstract

Lung cancer (LC) is a common type of cancer, which is a leading cause of death around the world. There is an urgency for the development of new drugs that could diagnose the LC in the early stages and in a precise manner. In this direction, the development of nanoparticles radiolabeled with the diagnostic radioisotopes represent an important advance in the field of cancer imaging. In this study were developed PLA/PVA/Atezolizumab nanoparticles which were radiolabeled with Tc (Technetium-99m). The radiolabeled nanoparticles were evaluated in both: in-vitro (L-929 and A-549) as in-vivo (mice). The results showed no cytotoxicity effect in the healthy cells (L-929) and cytotoxicity effect in the tumor cells (A-549). The biodistribution assay demonstrated that Tc-PLA/PVA/Atezolizumab could reach the tumor site 14-folds higher than the nonparticulate atezolizumab. In conclusion, Tc-PLA/PVA/Atezolizumab nanoparticles showed to be a new drug which is able to precisely image the lung tumor, and it must be considered for clinical trials.

摘要

肺癌(LC)是一种常见的癌症,是全球主要的死亡原因之一。迫切需要开发新的药物,以便能够以精确的方式在早期诊断 LC。在这方面,用诊断放射性同位素标记的纳米粒子的开发代表了癌症成像领域的重要进展。在这项研究中,开发了 PLA/PVA/Atezolizumab 纳米粒子,并对其进行了 Tc(锝-99m)放射性标记。对放射性标记的纳米粒子进行了体内(L-929 和 A-549)和体外(L-929 和 A-549)评估。结果表明,在健康细胞(L-929)中没有细胞毒性作用,而在肿瘤细胞(A-549)中具有细胞毒性作用。生物分布试验表明,Tc-PLA/PVA/Atezolizumab 能够到达肿瘤部位的浓度比非颗粒型 atezolizumab 高 14 倍。总之,Tc-PLA/PVA/Atezolizumab 纳米粒子显示出是一种能够精确成像肺部肿瘤的新药,值得考虑进行临床试验。

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