癌症治疗继续是一个巨大的挑战，因为大多数化疗药物对健康器官造成严重的不良反应，化疗药物缺乏选择性靶向作用，即使是现有的具有特异性靶向治疗也因为缺乏深入肿瘤微环境的分布而失败。纳米技术提供了多种优势，以应对传统疗法的局限性。然而，纳米治疗技术传递到肿瘤组织的效果多年来并未得到改善，部分原因是纳米治疗技术在更深的肿瘤区域的分布不足，导致耐药和复发。为了解决渗透问题，iRGD被探索并发现具有在改善癌症纳米医学传递方面极高的效果。临床前观察结果非常鼓舞人心，但是，临床转化还处于初期阶段。基于此，我们作出了详细的努力，详细介绍了iRGD在增加抗癌和肿瘤成像潜力方面的各种有希望的应用。重要的是，我们全面讨论了基于iRGD的治疗方法的临床转化所涉及的缺点和不确定性，以及未来的发展方向。 版权所有 ©2023 Elsevier B.V. 发表。

Cancer therapy continues to be a huge challenge as most chemotherapeutic agents exert serious adverse effects on healthy organs. Chemotherapeutic agents lack selective targeting and even the existing target specific therapies are failing due to poor distribution into the tumor microenvironment. Nanotechnology offers multiple advantages to address the limitations encountered by conventional therapy. However, the delivery of nanotherapeutics to tumor tissue has not improved over the years partly due to the poor and inadequate distribution of nanotherapeutics into deeper tumor regions resulting in resistance and relapse. To curb the penetration concerns, iRGD was explored and found to be highly effective in improving the delivery of cancer nanomedicine. The preclinical observations are highly encouraging; however, the clinical translation is at a nascent stage. Based on this, we have made an elaborative effort to give a detailed account of various promising applications of iRGD to increase anticancer and tumor imaging potential. Importantly, we have comprehensively discussed the shortcomings and uncertainties associated with the clinical translation of iRGD-based therapeutic approaches and future directions.Copyright © 2023. Published by Elsevier B.V.