**Abstract**

There has been substantial progress in the field of metal–organic frameworks (MOFs) and their nanoscale counterparts (NMOFs), in recent years. Their exceptional physicochemical properties are being constantly and actively exploited for various applications such as energy harvesting, gas storage, gas separation, catalysis, etc. Due to their porous framework, large surface area, tunability and easy surface functionalization, MOFs and NMOFs have also emerged as useful tools for biomedical applications, specifically for drug delivery. As drug carriers, they offer high drug loading capacity and controlled release at the target site. This chapter aims to give a panorama of the use of these MOFs as drug delivery agents. A brief overview of the structure and composition of MOFs, along with various methods and techniques to synthesize NMOFs suitable for drug delivery applications are mentioned. In addition, the most commonly employed strategies to associate drugs with these NMOFs are highlighted and methods to characterize them are also briefly discussed. The last section summarizes the applications of MOFs and NMOFs as carriers of therapeutic drugs, biomolecules, and other active agents.

**Keywords:** metal–organic frameworks, synthesis, drug encapsulation, characterization, drug delivery, biomolecules, photosensitizers
