Nanoscale metal-organic frameworks (NMOFs) are a promising class of hybrid materials for biomedical applications, offering advantages such as structural and chemical diversity, high loading capacity, and intrinsic biodegradability. These materials can be synthesized under mild conditions as either crystalline or amorphous structures, and their properties can be tuned by adjusting composition, size, and morphology. NMOFs have been used for delivering imaging contrast agents and therapeutic agents, including paramagnetic metal ions like Gd³⁺ and Mn²⁺ for magnetic resonance imaging (MRI), and high-Z elements for X-ray computed tomography (CT). They can also carry anticancer drugs, such as cisplatin, with high efficiency. Surface modifications, such as silica coatings or organic polymer coatings, enhance stability, functionality, and targeting capabilities. NMOFs have shown potential for multimodal imaging and drug delivery, with applications in MRI, optical imaging, and CT. They can be functionalized with targeting ligands to improve cellular uptake and specificity. Despite their promise, further research is needed to optimize in vivo performance, including prolonged blood circulation, evasion of the reticuloendothelial system, and improved tissue specificity. NMOFs represent a promising platform for nanomedicine, with potential for incorporating a wide range of imaging and therapeutic agents.Nanoscale metal-organic frameworks (NMOFs) are a promising class of hybrid materials for biomedical applications, offering advantages such as structural and chemical diversity, high loading capacity, and intrinsic biodegradability. These materials can be synthesized under mild conditions as either crystalline or amorphous structures, and their properties can be tuned by adjusting composition, size, and morphology. NMOFs have been used for delivering imaging contrast agents and therapeutic agents, including paramagnetic metal ions like Gd³⁺ and Mn²⁺ for magnetic resonance imaging (MRI), and high-Z elements for X-ray computed tomography (CT). They can also carry anticancer drugs, such as cisplatin, with high efficiency. Surface modifications, such as silica coatings or organic polymer coatings, enhance stability, functionality, and targeting capabilities. NMOFs have shown potential for multimodal imaging and drug delivery, with applications in MRI, optical imaging, and CT. They can be functionalized with targeting ligands to improve cellular uptake and specificity. Despite their promise, further research is needed to optimize in vivo performance, including prolonged blood circulation, evasion of the reticuloendothelial system, and improved tissue specificity. NMOFs represent a promising platform for nanomedicine, with potential for incorporating a wide range of imaging and therapeutic agents.