中药成分自组装是中药同类或异类成分在特定条件下，经非共价键作用自发构筑纳?微米级功能聚集体的过程。该过程既可保留各组分原有生物活性，又能通过协同效应赋予体系新功能。围绕“自上而下”与“自下而上”2种核心研究策略，系统阐述中药自组装行为。前者从中药复方或单味药中拆分天然存在的自组装纳米聚集体，后者通过分子定向组装构建纳米聚集体；阐明pH、温度、浓度及炮制等关键因素对自组装过程的调控作用。重点探讨中药自组装在诠释中药配伍理论、创新药物剂型与靶向递药系统、推动中药复方现代化研究中的应用价值。针对当前领域在机制解析、稳定性、安全性及临床转化方面的挑战，展望未来发展方向，旨在为中药复杂体系现代化研究提供新范式。

Self-assembly of traditional Chinese medicine components refers to the process in which similar or different components of traditional Chinese medicine, under specific conditions, spontaneously form functional aggregates at the nanometer-micron scale through non-covalent bonding. This process not only retains the original biological activity of each component but also endows the system with new functions through synergistic effects. This paper focuses on two core research strategies, “top-down” and “bottomup”, to systematically describe the self-assembly behavior of traditional Chinese medicine: the former splits the naturally existing selfassembling nano-aggregates from traditional Chinese medicine compound or single herbs, while the latter builds nano-aggregates through molecular directional assembly; it clarifies the regulatory effects of key factors such as pH, temperature, concentration, and processing on the self-assembly process; and it mainly explores the application value of traditional Chinese medicine self-assembly in interpreting traditional Chinese medicine compatibility theory, innovating drug formulations and targeted drug delivery systems, and promoting the modernization research of traditional Chinese medicine compound. In response to the current challenges in the field regarding mechanism analysis, stability, safety, and clinical translation, this paper looks forward to future development directions, aiming to provide a new paradigm for the modernization research of complex traditional Chinese medicine systems.

R283.6

国家自然科学基金资助项目(82204595); 国家自然科学基金项目联合基金资助项目(U23A20517); 山西省基础研究计划资助项目(202303021221070); 中国博士后基金资助项目(340903); 山西省中医药科技创新工程资助项目(2025kjzy006)