As one of the most promising and effective delivery systems for targeted controlled-release drugs, nanocarriers (NCs) have been widely studied. Although the development of nanoparticle preparations is very prosperous, the safety and effectiveness of NCs are not guaranteed and cannot be precisely controlled due to the unclear processes of absorption, distribution, metabolism, and excretion (ADME), as well as the drug release mechanism of NCs in the body. Thus, the approval of NCs for clinical use is extremely rare. This paper reviews the research progress and challenges of using NCs in vivo based on a review of several hundred closely related publications. First, the ADME of NCs under different administration routes is summarized; second, the influences of the physical, chemical, and biosensitive properties, as well as targeted modifications of NCs on their disposal process, are systematically analyzed; third, the tracer technology related to the in vivo study of NCs is elaborated; and finally, the challenges and perspectives of nanoparticle research in vivo are introduced. This review may help readers to understand the current research progress and challenges of nanoparticles in vivo, as well as of tracing technology in nanoparticle research, to help researchers to design safer and more efficient NCs. Furthermore, this review may aid researchers in choosing or exploring more suitable tracing technologies to further advance the development of nanotechnology.

作为靶向控释药物最有前途和最有效的传递系统之一，纳米载体（NCs）已被广泛研究。尽管纳米颗粒制剂的发展非常繁荣，但由于吸收，分布，代谢和排泄（ADME）的过程不清楚，以及纳米粒的药物释放机制，NCs的安全性和有效性无法得到保证，也无法得到精确控制。体内的NC。因此，非常少有NC用于临床的批准。本文综述了在体内使用NC的研究进展和挑战基于对数百篇密切相关的出版物的评论。首先，总结了不同给药途径下NCs的ADME。其次，系统地分析了物理，化学和生物敏感性特性的影响，以及对NCs的有针对性的修改对其处置过程的影响；第三，阐述了与NCs体内研究有关的示踪技术。最后，介绍了体内纳米颗粒研究的挑战和前景。这篇综述可以帮助读者了解纳米粒子在体内的最新研究进展和挑战以及纳米颗粒研究中的追踪技术，可帮助研究人员设计更安全，更高效的NC。此外，本综述可帮助研究人员选择或探索更合适的示踪技术，以进一步推动纳米技术的发展。