Department of Radiology & Nuclear Medicine, Erasmus MC, 's-Gravendijkwal 230, 3015 CE Rotterdam.
Department of Radiation Science and Technology, Delft University of Technology, Mekelweg 15, 2629 JB Delft, The Netherlands; Institut Charles Sadron, University of Strasbourg, CNRS UPR 22, 23 rue du Loess, 67034 Strasbourg, cedex 2, France; Department of Chemical Engineering, Delft University of Technology, van der Maasweg 9, 2629 HZ, 2628 BL Delft, The Netherlands.
Nanomedicine. 2017 Oct;13(7):2179-2188. doi: 10.1016/j.nano.2017.04.015. Epub 2017 May 20.
Pluronics P94 are block-copolymer showing prolonged circulation time and tumor-cell internalization in vitro, suggesting a potential for tumor accumulation and as a drug carrier. Here we report the results of the radiolabeled-P94 unimers (P94-In-DTPA) on tumor uptake/retention and biodistribution after intravenous and intratumoral injection to tumor-bearing mice. Intravenous administration results in a high radioactive signal in the liver; while in tumor and other healthy tissues only low levels of radioactivity could be measured. In contrast, the intratumoral injection of P94 resulted in elevated levels of radioactivity in the tumor and low levels in other organs, including the liver. Independently from the injection route, the tumor tissue presented long retention of radioactivity. The minimal involvement of off-target tissues of P94, together with the excellent tracer retention over-time in the tumor designates Pluronic P94 copolymer as a highly promising carrier for anti-tumor drugs.
泊洛沙姆 P94 是一种嵌段共聚物，具有延长的循环时间和体外肿瘤细胞内化作用，提示其具有肿瘤蓄积和作为药物载体的潜力。本文报道了放射性标记的 P94 单体（P94-In-DTPA）经静脉和肿瘤内注射到荷瘤小鼠后的肿瘤摄取/保留和生物分布的结果。静脉给药后，肝脏中放射性信号很高；而在肿瘤和其他健康组织中，只能测量到低水平的放射性。相比之下，P94 的肿瘤内注射导致肿瘤中放射性水平升高，而其他器官（包括肝脏）中的放射性水平较低。与注射途径无关，肿瘤组织中放射性的保留时间较长。泊洛沙姆 P94 对非靶组织的最小参与，以及在肿瘤中随时间延长的优异示踪剂保留，将 Pluronic P94 共聚物指定为抗肿瘤药物的极具前景的载体。
