Cell penetrating peptides (CPPs) are commonly utilized for intracellular delivery of functional materials to circumvent biomembrane barrier. However, further application of CPPs is hindered by lacking selectivity toward targeted cells. The spider venom peptide, lycosin-I, is a CPP with potent cytotoxicity to cancer cells, which might enable lycosin-I to deliver functional materials into cancer cells selectively. In this study, we demonstrated that the lycosin-I-conjugated spherical gold nanoparticles (LGNPs) not only exhibited efficient cellular internalization efficiency toward cancer cells but also displayed unprecedented selectivity over noncancerous cells. Although LGNPs were removed from the living circulatory system via reticuloendothelial system-dominant clearance modes without noticeable adverse effects to animals, they actually displayed active tumor-targeting effects and efficient accumulation in tumors in vivo. Furthermore, the potential application of this platform for cancer therapy was explored by lycosin-I-conjugated gold nanorods (LGNRs). LGNRs exhibited selective intracellular translocation towards cancer cells and efficient photothermal effect under near infrared (NIR, 808 nm) irradiation, which consequently killed cancer cells in vitro and in vivo effectively. Therefore, the established LGNPs and LGNRs possessed great potential in cancer-targeting delivery and photothermal therapy.

中文翻译：

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蜘蛛毒素肽Lycosin-I功能化的纳米金在体内肿瘤靶向和治疗。

细胞穿透肽（CPP）通常用于功能性材料的细胞内递送，以规避生物膜屏障。但是，由于缺乏对靶细胞的选择性，阻碍了CPP的进一步应用。蜘蛛毒肽，lycosin-I，是一种对癌细胞具有强细胞毒性的CPP，它可能使lycosin-I选择性地将功能性物质传递到癌细胞中。在这项研究中，我们证明了溶血素I共轭球形金纳米颗粒（LGNPs）不仅对癌细胞具有有效的细胞内在化效率，而且对非癌细胞具有前所未有的选择性。尽管LGNPs是通过网状内皮系统以清除方式从活体循环系统中清除的，但对动物没有明显的不良影响，体内。此外，通过溶血素-I共轭的金纳米棒（LGNRs）探索了该平台在癌症治疗中的潜在应用。LGNRs表现出选择性的向癌细胞内转移，并在近红外（NIR，808 nm）辐射下具有有效的光热效应，从而在体内和体外有效杀死癌细胞。因此，已建立的LGNPs和LGNRs在靶向癌症的治疗和光热疗法方面具有巨大的潜力。