With the rapid development of technology in the therapeutic field, metal-organic frameworks (MOFs)/coordination polymers (CPs) can be considered as a progressive drug carrier for biomedical applications in drug delivery systems (DDS). These materials have exhibited notable perspectives as in mint condition DDS due to their various identical properties, such as well-defined structures, tunable porosity, ultrahigh surface area, and easy chemical functionalization. The excellent thermal and chemical stabilities of these compounds are convenient for relevant applications. The DDSs allow the discharge of the active pharmaceutical component to perform a prayed therapeutic response. In past few years, there has been interpretative progress in many new sections of MOFs and CPs that have earned popularity over other unique identified systems through higher biocompatibility and versatile loading capabilities. This review presents and assesses the most recent research, findings, and challenges associated with the use of MOFs as DDSs. With the drastic development of synthetic methods, tailorable composition, and functionalization techniques, smart MOF-based nanocomposites with advanced bio-related properties have been designed to meet the growing demands of MOF materials for biomedical applications. Tangible care is given to the stimuli responsive MOF-based DDSs with great interest in the pandemic era for additive therapy and multimodal systems.