纳米药物的快速发展正在彻底改变癌症治疗的格局，而有效地将它们输送到实体瘤中仍然是一个艰巨的挑战。目前，监管部门批准的纳米药物与实验室报告的纳米颗粒之间的治疗反应存在巨大脱节。这种差异主要是由于未能利用纳米药物在肿瘤中的经典整体药代动力学行为来预测抗肿瘤功效。越来越多的证据表明，治疗效果主要依赖于纳米药物的瘤内时空分布。本综述重点关注全身化疗纳米药物在实体瘤中的时空分布。首先，详细描述了调节纳米药物时空分布的瘤内生物屏障。接下来重点分析纳米药物的空间分布和时间释放对抗肿瘤疗效的影响。然后，总结了当前评估纳米药物时空分布的方法。最后，全面回顾了积极调节纳米药物时空分布以实现最佳肿瘤治疗的先进策略。版权所有 © 2023。由 Elsevier B.V. 出版。

The rapid development of nanomedicines is revolutionizing the landscape of cancer treatment, while effectively delivering them into solid tumors remains a formidable challenge. Currently, there is a huge disconnect on therapeutic response between regulatory approved nanomedicines and laboratory reported nanoparticles. The discrepancy is mainly resulted from the failure of using the classic overall pharmacokinetics behaviors of nanomedicines in tumors to predict the antitumor efficacy. Increasing evidence has revealed that the therapeutic efficacy predominantly relies on the intratumoral spatiotemporal distribution of nanomedicines. This review focuses on the spatiotemporal distribution of systemically administered chemotherapeutic nanomedicines in solid tumor. Firstly, the intratumoral biological barriers that regulate the spatiotemporal distribution of nanomedicines are described in detail. Next, the influences on antitumor efficacy caused by the spatial distribution and temporal drug release of nanomedicines are emphatically analyzed. Then, current methodologies for evaluating the spatiotemporal distribution of nanomedicines are summarized. Finally, the advanced strategies to positively modulate the spatiotemporal distribution of nanomedicines for an optimal tumor therapy are comprehensively reviewed.Copyright © 2023. Published by Elsevier B.V.