Nanoparticles have been extensively employed for early cancer diagnosis and treatment due to their favorable optical, magnetic, and radioactive properties. As carriers, they can also attain targeted delivery and controlled drug release, thus improving therapeutic efficacy. However, simultaneously reconciling tumor-targeting enrichment efficiency, tunable collective properties, and metabolic clearance remains a formidable challenge in tumor imaging and therapy. Recently, responsive assembly and disassembly strategies that exploit characteristics of the tumor microenvironment have opened new avenues to address this challenge. On the one hand, in vivo assembly and disassembly of nanoparticles can optimize their biodistribution and metabolism, sequentially promoting tumor-targeted accumulation and systemic clearance. On the other hand, the physicochemical properties of nanoparticles are precisely modulated by changes in size and structure during the assembly and disassembly process, thus improving tumor theranostic performance. Although several reviews on size-tunable nanomaterials were published, they mainly focused on how size variations of nanomaterials influence their biological effects, such as enhanced penetration, increased retention, and accelerated elimination. Little attention has been paid to the size-dependent changes in the intrinsic properties (e.g., optical, magnetic, and radioactive properties) of nanomaterials, particularly inorganic nanomaterials, and the biological application of such changes. In this work, we review the in vivo assembly and disassembly of several types of inorganic nanoparticles and their applications in tumor imaging and treatment.



