Nanoparticles as drug delivery systems and diagnostic agents have gained much attention in recent
years, especially for cancer treatment. Nanocarriers improve the therapeutic efficiency and bioavailability of
antitumor drugs, besides providing preferential accumulation at the target site. Among different types of nanocarriers
for drug delivery assays, metal-organic frameworks (MOFs) have attracted increasing interest in the academic
community. MOFs are an emerging class of coordination polymers constructed of metal nodes or clusters
and organic linkers that show the capacity to combine a porous structure with high drug loading through distinct
kinds of interactions, overcoming the limitations of traditional drug carriers explored up to date. Despite the rational
design and synthesis of MOFs, structural aspects and some applications of these materials like gas adsorption
have already been comprehensively described in recent years; it is time to demonstrate their potential applications
in biomedicine. In this context, MOFs can be used as drug delivery systems and theranostic platforms due
to their ability to release drugs and accommodate imaging agents. This review describes the intrinsic characteristics
of nanocarriers used in cancer therapy and highlights the latest advances in MOFs as anticancer drug delivery
systems and diagnostic agents.