Orally absorbable gold nanoparticles (AuNP) having cancer ablation therapy is strongly demanded to treat glioblastoma multiforme (GBM) for patients with its highest incidence rate. Here, we develop a milk protein lactoferrin-conjugated AuNP for its oral absorption and targeting to the GBM through the interaction between lactoferrin (Lf) and lactoferrin receptor (LfR) that is highly expressed in the intestine, blood-brain barrier and GBM. For stability and long circulation of AuNP, glutathione and polyethylene glycol (PEG) is introduced, which is called to Lf-PEG-AuNP. When Lf-PEG-AuNP are orally administered to orthotopic GBM-bearing mice, 11-fold and 8-fold higher concentrations of AuNP are measured in bloodstreams and GBM in the brain, respectively, compared with unconjugated-AuNP. Therefore, orally administered Lf-PEG-AuNP exhibit an outstanding temperature rise in GBM by irradiating laser and significantly reduce tumor volume. Collectively, we suggest that the Lf-PEG-AuNP can fundamentally target GBM in the brain through oral absorption, and that its efficient photothermal therapy is possible.

对于发病率最高的多形性胶质母细胞瘤（GBM）患者来说，强烈需要具有癌症消融疗法的口服可吸收金纳米颗粒（AuNP）。在此，我们开发了一种乳蛋白乳铁蛋白缀合的 AuNP，用于口服吸收，并通过乳铁蛋白 (Lf) 和在肠道、血脑屏障和 GBM 中高表达的乳铁蛋白受体 (LfR) 之间的相互作用靶向 GBM。为了保证AuNP的稳定性和长循环性，引入了谷胱甘肽和聚乙二醇（PEG），称为Lf-PEG-AuNP。当 Lf-PEG-AuNP 口服给予原位 GBM 小鼠时，与未结合的 AuNP 相比，在血流和 GBM 中测得的 AuNP 浓度分别高出 11 倍和 8 倍。因此，口服 Lf-PEG-AuNP 通过激光照射使 GBM 表现出显着的温升，并显着减小肿瘤体积。总的来说，我们认为 Lf-PEG-AuNP 可以通过口服吸收从根本上靶向大脑中的 GBM，并且其有效的光热疗法是可能的。