“…A major advantage of nanostructures in biomedical applications is their multifunctional capacity, which is particularly important for the treatment of complex diseases. − By integrating a limited number of functional blocks into a nanostructure, a multifunctional nanoformulation can be established to simultaneously achieve several tasks. − In general, these multifunctional nanomedicines were constructed by integrated means of covalent modification, self-assembly, coordination, physical embedding, and biotechnology. ,, The obtained multifunctionality includes, but is not limited to, therapeutics, diagnosis, imaging, delivery, and targeting. , The cooperativity of various pharmacophores is promising to manifest a satisfactory diagnostic and therapeutic index for many complex diseases. − Although significant achievements have been obtained in recent decades, multifunctional nanomedicines still face two formidable challenges: too much complexity and not enough reproducibility. , To achieve multifunctionality, nanostructures generally comprise complex components and require complicated preparation procedures, which cannot warrant the batch-to-batch consistency of construction and even function.…”