Targeted drug delivery, also known as smart drug delivery or active drug delivery, is a subcategory of nanomedicine. Using this strategy, the medication is delivered into the infected organs in the patient's body or to the targeted sites inside the cells. In order to improve therapeutic efficiency and pharmacokinetic characteristics of the active pharmaceutical agents, conjugation of biomacromolecules such as proteins, nucleic acids, monoclonal antibodies, aptamers, and nanoparticulate drug carriers, has been mostly recommended by scientists in the last decades. Several covalent conjugation pathways are used for biomacromolecules coupling with nanomaterials in nanomedicine including carbodiimides and "click" mediated reactions, thiol-mediated conjugation, and biotin-avidin interactions. However, choosing one or a combination of these methods with suitable coupling for application to advanced drug delivery is essential. This review focuses on new and high impacted published articles in the field of nanoparticles and biomacromolecules coupling studies, as well as their advantages and applications.
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