Anticancer drug‐loaded nanoparticles have been explored extensively to decrease side effects while improving their therapeutic efficacy. However, due to the low drug loading content, premature drug release, nonstandardized carrier structure, and difficulty in predicting the fate of the carrier, only a few nanomedicines have been approved for clincial use. Herein, a carrier‐free nanoparticle based on the self‐assembly of the curcumin–erlotinib conjugate (EPC) is developed. The EPC nanoassembly exhibits more potent cell killing, better antimigration, and anti‐invasion effects for BxPC‐3 pancreatic cancer cells than the combination of free curcumin and erlotinib. Furthermore, benefiting from both passive and active tumor targeting effect, EPC nanoassembly can effectively accumulate in the tumor tissue in a xenograft pancreatic tumor mouse model. Consequently, EPC effectively reduces the growth of pancreatic tumors and extends the median survival time of the tumor‐bearing mice from 22 to 68 days. In addition, no systemic toxicity is detected in the mice receiving EPC treatment. Attributed to the uniformity of the curcumin–erlotinib conjugate and easiness of scaling up, it is expected that the EPC can be translated into a powerful tool in fighting against pancreatic cancer and other epidermal growth factor receptor positive cancers.

中文翻译：

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用于癌症靶向治疗的姜黄素-厄洛替尼缀合物的无载体纳米组装。

载有抗癌药物的纳米颗粒已被广泛探索，以减少副作用，同时提高其治疗效果。然而，由于载药量低、药物释放过早、载体结构不标准化、载体命运难以预测等问题，只有少数纳米药物被批准用于临床。在此，开发了一种基于姜黄素-埃洛替尼缀合物（EPC）自组装的无载体纳米颗粒。与游离姜黄素和厄洛替尼的组合相比，EPC纳米组装体对BxPC-3胰腺癌细胞表现出更有效的细胞杀伤作用、更好的抗迁移和抗侵袭作用。此外，受益于被动和主动肿瘤靶向作用，EPC纳米组装体可以在异种移植胰腺肿瘤小鼠模型中有效积聚在肿瘤组织中。因此，EPC 有效地减少了胰腺肿瘤的生长，并将荷瘤小鼠的中位生存时间从 22 天延长至 68 天。此外，在接受 EPC 治疗的小鼠中没有检测到全身毒性。由于姜黄素-厄洛替尼缀合物的均一性和易于扩大规模，预计 EPC 可以转化为对抗胰腺癌和其他表皮生长因子受体阳性癌症的强大工具。