Facile in situ synthesis of ultrasmall near-infrared-emitting gold glyconanoparticles with enhanced cellular uptake and tumor targeting
Facile in situ synthesis of ultrasmall near-infrared-emitting gold glyconanoparticles with enhanced cellular uptake and tumor targeting
复制标题
轻松原位合成超小型近红外发射金糖纳米粒子，增强细胞摄取和肿瘤靶向性
DOI：
10.1039/c9nr03821c
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发表时间：
2019
期刊：
影响因子：
6.7
通讯作者：
Liu Jinbin
中科院分区：
文献类型：
--
作者：
Wang Yaping;Ma Shufeng;Dai Zhiyi;Rong Zhili;Liu Jinbin
同时拥有高肿瘤靶向效率、长血液循环和低正常组织保留是未来临床可翻译纳米药物的关键。在此，我们报道了一种简单的原位糖缀合策略，用于在金前驱体存在的情况下，使用1-硫代-β- d -葡萄糖作为表面配体和还原剂合成近红外（NIR）发射金糖纳米颗粒（AuGNPs, ~ 2.4 nm）。超小AuGNPs表现出与肾可清除的超小非糖纳米颗粒相似的低健康器官保留率，但在体外和体内肿瘤靶向效率分别高出约10倍和2.5倍。研究发现，超小AuGNPs这种简单的糖缀合策略对癌细胞中的葡萄糖转运蛋白具有活性，并通过肾脏和肝胆清除途径延长血液循环，从而协同增强了超小AuGNPs的肿瘤靶向性。这一发现为提高超小NPs的肿瘤靶向性提供了一种明智的策略，并进一步加强了我们对糖缀合作用在设计未来临床可翻译纳米药物方面的理解。
The simultaneous possession of high tumor-targeting efficiency, long blood circulation, and low normal-tissue retention is critical for future clinically translatable nanomedicines. Herein, we reported a facile in situ glycoconjugation strategy for the synthesis of near-infrared (NIR)-emitting gold glyconanoparticles (AuGNPs, ∼2.4 nm) using 1-thio-β-D-glucose as both the surface ligand and the reducing agent in the presence of a gold precursor. The ultrasmall AuGNPs showed similar low healthy organ retention to that of the renal-clearable ultrasmall nonglyconanoparticles, but ∼10 and 2.5 times higher in vitro and in vivo tumor-targeting efficiencies, respectively, were observed. This facile glycoconjugation strategy of ultrasmall AuGNPs was found to show activity towards glucose transporters in the cancer cells and prolonged blood circulation with both renal and hepatobiliary clearance pathways, which synergistically enhanced the tumor targeting of the ultrasmall AuGNPs. This discovery provides a smart strategy for the improvement in tumor targeting by ultrasmall NPs and further strengthens our understanding of glycoconjugation in designing future clinically translatable nanomedicines.