近年来，DNA 纳米结构除了具有遗传功能外，还作为用于药物输送、生物传感和癌症治疗的新兴生物医学材料得到了广泛的研究。通过简单的自组装过程，多个精确设计的单链 DNA 可以被制造成复杂的三维 DNA 纳米结构。在所有合成的DNA纳米结构中，四面体DNA纳米结构（TDN）脱颖而出，成为最有前途的生物医学纳米材料。 TDNs由于其紧凑的结构和DNA来源而具有结构稳定性、细胞膜渗透性和天然生物相容性的优点。除了其固有的优势外，TDN 通过多种功能修饰在递送治疗剂方面具有巨大潜力。作为一种多功能材料，TDN 实现了创新的制药应用，包括抗菌治疗、抗癌治疗、免疫调节和软骨再生。鉴于 TDN 在生物医学领域的快速发展，了解如何成功生产和微调 TDN 的特性以满足特定的治疗需求和临床转化至关重要。本文深入探讨了 TDN 的合成和功能化，并总结了基于 TDN 的治疗递送方法及其在药剂学和纳米医学领域的广泛应用、挑战和未来方向。© 2024 美国化学会。

DNA nanostructures have been widely researched in recent years as emerging biomedical materials for drug delivery, biosensing, and cancer therapy, in addition to their hereditary function. Multiple precisely designed single-strand DNAs can be fabricated into complex, three-dimensional DNA nanostructures through a simple self-assembly process. Among all of the synthetic DNA nanostructures, tetrahedral DNA nanostructures (TDNs) stand out as the most promising biomedical nanomaterial. TDNs possess the merits of structural stability, cell membrane permeability, and natural biocompatibility due to their compact structures and DNA origin. In addition to their inherent advantages, TDNs were shown to have great potential in delivering therapeutic agents through multiple functional modifications. As a multifunctional material, TDNs have enabled innovative pharmaceutical applications, including antimicrobial therapy, anticancer treatment, immune modulation, and cartilage regeneration. Given the rapid development of TDNs in the biomedical field, it is critical to understand how to successfully produce and fine-tune the properties of TDNs for specific therapeutic needs and clinical translation. This article provides insights into the synthesis and functionalization of TDNs and summarizes the approaches for TDN-based therapeutics delivery as well as their broad applications in the field of pharmaceutics and nanomedicine, challenges, and future directions.© 2024 American Chemical Society.