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放射性标记的光敏剂连接牛血清白蛋白纳米颗粒的合成与生物学评价作为肿瘤成像剂。

Synthesis and biological evaluation of radiolabeled photosensitizer linked bovine serum albumin nanoparticles as a tumor imaging agent.

机构信息

Department of Nuclear Applications, Institute of Nuclear Science, Ege University, Bornova TR-35100, Izmir, Turkey.

出版信息

Int J Pharm. 2012 Jan 17;422(1-2):472-8. doi: 10.1016/j.ijpharm.2011.11.013. Epub 2011 Nov 15.

Abstract

In this study, we reported on the synthesis and biological evaluation of radiolabeled fluorescent dye conjugated bovine serum albumin nanoparticles within the size range 190-210 nm. The bovine serum albumin nanoparticles (BSANPs) were prepared using a desolvation method, and chemical cross-linking was performed using gluteraldehyde. Furthermore, pheophorbide-a (PH-A) was loaded on the BSANPs. The results obtained from dynamic light scattering and electron microscopy have proved that nanoparticles are highly monodisperse and near-spherical shaped. The photo-physical properties of the PH-A-BSANPs were obtained using the spectrophotometric techniques. According to the results, PH-A and BSANPs show high non-covalent interaction. PH-A loaded nanoparticles were labeled with (99m)Tc and the radio-labeling efficiency was determined as 90 ± 1.2%. Biodistribution studies of (99m)Tc labeled PH-A-BSANPs and PH-A were carried out using female Albino Wistar rats, and (99m)Tc-PH-A-BSANPs showed a significantly higher uptake in the breast and uterus than (99m)Tc-PH-A. Cell culture study was carried out in MCF-7 cell line (human breast adenocarcinoma cell line). According to the cell culture studies, (99m)Tc-PH-A-BSANPs showed a higher uptake than (99m)Tc-PH-A. Moreover, PH-A-BSANPs demonstrated good photo-physical properties and BSANPs increased the uptake of PH-A on to the MCF-7 cell line. These results confirm that (99m)Tc labeled PH-A-BSANPs could be utilized for radioimaging.

摘要

在这项研究中,我们报告了在 190-210nm 范围内合成和生物评价放射性标记荧光染料偶联牛血清白蛋白纳米粒子。牛血清白蛋白纳米粒子(BSANPs)是使用去溶剂化法制备的,并且使用戊二醛进行了化学交联。此外,叶啉-a(PH-A)被加载到 BSANPs 上。动态光散射和电子显微镜的结果证明了纳米粒子具有高度单分散性和近球形。使用分光光度技术获得了 PH-A-BSANPs 的光物理性质。结果表明,PH-A 和 BSANPs 表现出很强的非共价相互作用。负载 PH-A 的纳米粒子被标记上(99m)Tc,放射性标记效率确定为 90±1.2%。使用雌性白化 Wistar 大鼠进行了(99m)Tc 标记的 PH-A-BSANPs 和 PH-A 的生物分布研究,(99m)Tc-PH-A-BSANPs 在乳房和子宫中的摄取明显高于(99m)Tc-PH-A。在 MCF-7 细胞系(人乳腺癌腺癌细胞系)中进行了细胞培养研究。根据细胞培养研究,(99m)Tc-PH-A-BSANPs 的摄取量高于(99m)Tc-PH-A。此外,PH-A-BSANPs 表现出良好的光物理性质,BSANPs 增加了 PH-A 在 MCF-7 细胞系上的摄取。这些结果证实(99m)Tc 标记的 PH-A-BSANPs 可用于放射性成像。

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