Antitumor Effect of 131I-Labeled Anti-VEGFR2 Targeted Mesoporous Silica Nanoparticles in Anaplastic Thyroid Cancer

Abstract

Anaplastic thyroid cancer (ATC) comprises approximately 2% of all thyroid cancers, and its median survival rate remains poor because of its resistance to conventional therapy. Vascular endothelial growth factor receptor (VEGFR)-targeted therapeutics-loaded mesoporous silica nanoparticles represent a major advance for angiogenesis imaging and inhibition in lethal cancers. In the present study, we aimed to assess whether ¹³¹I-labeled anti-VEGFR2 targeted mesoporous silica nanoparticles would have antitumor efficacy in an ATC tumor-bearing nude mouse model. Using in vitro and in vivo studies, we investigated the increased targeting ability and retention time in the anti-VEGFR2 targeted group using confocal microscopy and a γ counter. The tumor tissue radioactivity of the anti-VEGFR2 targeted group at 24 and 72 h after intratumoral injection was significantly higher than that of the non-targeted groups (all P < 0.05). Moreover, we found that radioactive accumulation was obvious even at 3 week post-injection in the anti-VEGFR2 targeted group via single-photon emission computed tomography/computed tomography, which was not seen at 3 day post-injection in the Na¹³¹I group. Meanwhile, compared with the non-targeted group, tumor growth in the targeted group was significantly inhibited, without causing apparent systemic toxic effects. Additionally, the median survival time in the targeted group (41 days) was significantly prolonged compared with that in the non-targeted (34 days) or Na¹³¹I (25 days) groups (both P < 0.01). Our data support the view that the as-developed ¹³¹I-labeled anti-VEGFR2 targeted mesoporous silica nanoparticles showed promising results in ATC tumor-bearing mouse model and such an approach might represent a novel therapeutic option for ATC.