<p>Metal–organic frameworks (MOFs) represent a high-class of versatile materials, distinguished by their porous structures and chemical tunability. The unique combination of MOF properties has positioned them as promising candidates for myriad biomedical applications, ranging from targeted drug delivery and controlled release systems to advanced diagnostic materials. Despite their potential, the widespread application of MOFs in biomedicine relies on overcoming significant challenges in their synthesis and characterization. Traditional methodologies for MOF synthesis often fail to address the complex requirements of biomedical applications, such as biocompatibility, stability under physiological conditions, and precise control over functionalization. This review illuminates the technological advancements in synthesizing and characterizing MOFs and/or MOF-based nanomaterials, aiming to bridge the gap between the intrinsic properties of MOFs and their biomedical applications. We explore emerging synthesis techniques that offer improved controllability, scalability, and environmental benignity alongside novel characterization methods that provide deeper insight into MOF structures and interactions with biological systems. The state-of-the-art developments in MOF-based nanomaterials, encompassing synthesis, characterization, and biomedical applications, are comprehensively discussed. By highlighting recent breakthroughs and the potential for future innovations, this review not only aspires to carry through interdisciplinary collaboration but also accelerate the integration of MOFs or MOF-based nanomaterials into the next generation of biomedical solutions.</p>