The development of nanomedicine has recently achieved several breakthroughs in the field of cancer treatment; however, biocompatibility and targeted penetration of these nanomaterials remain as limitations, which lead to serious side effects and significantly narrow the scope of their application. The self-assembly of intermediate filaments with arginine–glycine–aspartate (RGD) peptide (RGD-IFP) was triggered by the hydrophobic cationic molecule 7-amino actinomycin D (7-AAD) to synthesize a bifunctional nanoparticle that could serve as a fluorescent imaging probe to visualize tumor treatment. The designed RGD-IFP peptide possessed the ability to encapsulate 7-AAD molecules through the formation of hydrogen bonds and hydrophobic interactions by a one-step method. This fluorescent nanoprobe with RGD peptide could be targeted for delivery into tumor cells and released in acidic environments such as endosomes/lysosomes, ultimately inducing cytotoxicity by arresting tumor cell cycling with inserted DNA. It is noteworthy that the RGD-IFP/7-AAD nanoprobe tail-vein injection approach demonstrated not only high tumor-targeted imaging potential, but also potent antitumor therapeutic effects in vivo. The proposed strategy may be used in peptide-driven bifunctional nanoparticles for precise imaging and cancer therapy.

纳米医学的发展最近在癌症治疗领域取得了多项突破；然而，这些纳米材料的生物相容性和靶向渗透性仍然存在局限性，这会导致严重的副作用并显着缩小其应用范围。中间丝与精氨酸-甘氨酸-天冬氨酸 (RGD) 肽 (RGD-IFP) 的自组装由疏水性阳离子分子 7-氨基放线菌素 D (7-AAD) 触发以合成可用作荧光的双功能纳米颗粒成像探头可视化肿瘤治疗。设计的RGD-IFP肽具有通过一步法形成氢键和疏水相互作用来封装7-AAD分子的能力。这种带有 RGD 肽的荧光纳米探针可以靶向递送到肿瘤细胞中并在酸性环境中释放，例如内体/溶酶体，最终通过插入 DNA 阻止肿瘤细胞循环来诱导细胞毒性。值得注意的是，RGD-IFP/7-AAD纳米探针尾静脉注射方法不仅表现出高肿瘤靶向成像潜力，而且具有强大的抗肿瘤治疗效果在体内。所提出的策略可用于肽驱动的双功能纳米粒子，用于精确成像和癌症治疗。