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The aspect of human life, making nanotechnology an exciting field for biomedical applications. Over the years, metal nanoparticles, such as silver, have attracted a lot of attention because of their extraordinary optical, electrical, and antibacterial qualities. Unfortunately, those nanoparticles' aggregation and toxicity have restricted their employment in more advantageous applications. Choosing therapeutically active bimolecular judiciously to functionalize the surface of these particles would undoubtedly improve their biological applicability and biocompatibility. In addition to providing an overview of the current approaches being used to biofunctionalize silver nanoparticles for certain purposes, the current review the distinct size-dependent properties of nanoscale materials have had a significant impact on every aims to highlight the application areas of these particles. Nanotechnology is a promising subject for biomedical applications because of the distinctive size-dependent features of materials at the nanoscale that have greatly touched all aspects of human life. Because of their exceptional optical, electrical, and antibacterial qualities, metal nanoparticles—like silver—have attracted a lot of attention over time. However, their employment in highly optimized applications has been limited due to their poisonous nature and tendency to aggregate. The biocompatibility and biological applicability of these particles are certain to be improved by the logical selection of therapeutically active bimolecular to functionalize their surface. The present review endeavors to emphasize the various application areas of silver nanoparticles while providing an overview of the current approaches entailed in biofunctionalizing these particles for particular uses.