Assembly and Disassembly of Nanoparticles for Antitumor Applications: Mechanisms, Strategies, and Functions

ABSTRACT

Nanoparticles (NPs) demonstrate tremendous potential in tumor therapy, diagnostic imaging, and precision medicine. Their performance is regulated by their assembly and disassembly, which influence drug delivery, therapeutic efficacy, and biosafety. However, existing reviews are confined to single therapeutic modalities, specific assembly strategies, or isolated functional optimization approaches, and do not systematically examine of NP assembly‐disassembly processes and their biological functions. Accordingly, this review first discusses the driving forces behind NP assembly and disassembly, including hydrophobic, electrostatic, hydrogen bonding, and π–π interactions. Subsequently, the NP assembly strategies, covering ex situ and in situ self‐assembly, are summarized, and the applications by which assembled NP extend blood circulation residence time, enhance tumor accumulation, protect therapeutic cargo, and potentiate therapeutic efficacy are examined. The major NP disassembly pathways, including bond cleavage, carrier degradation, coordination dissociation, supramolecular dissociation, and phase transition, are subsequently discussed, highlighting their involvement in drug release, intracellular trafficking, and molecular imaging. Finally, a trade‐off‐based assembly and disassembly discussion outlines the key challenges for clinical translation, aiming to guide the development of more effective NP‐based therapeutic systems.