In recent times, metal nanoparticles, especially gold nanoparticles (GNPs), have attracted considerable interest in bone regeneration and expanded many folds. Their eminence is governed by the ease in fabrication, stability, controllable size, high surface area, easy functionalization, and multifunctionality. [3] In bone tissue engineering, GNPs can extend their multifunctionality to different dimensions in modulating the fundamental elements of tissue engineering like scaffolds, cells, and bioactive cues. GNPs can improve the scaffolds' physicochemical properties, making them more suitable for bone regeneration. They also stimulate cellular functionality by enhancing adhesion, proliferation, migration, and differentiation. GNPs have already been explored for their capability in controlled delivery of the bioactive cues providing eminent therapeutic potential. Besides controlling the osseous tissue functionality, they also regulate the immunological and vascularization process propounding the tissue repair mechanism adding to extensive neo-bone formation. Gold has been considered the most stable and nontoxic metal, but its reduction to nanometric ranges changes the surface properties making them more reactive and functional than its bulk counterpart. [4] Many studies have been conducted to determine the toxicity of GNPs in biological systems. Nevertheless, mainly being safe, gold in nanometric range can exhibit toxicity depending on their size, shape, surface charge, and functionalization. Therefore, it becomes crucial to extensively study the cytocompatibility of these nanoparticles for every biological activity conferred by them.The current review focuses on exploring the multiple potentials of GNPs, which are revolutionizing the field of bone tissue engineering as regenerative therapy. The first part of the review deals with the involvement of nanoparticles in the areas of osteogenesis and how they help in remodeling the osseous tissues. The second part extensively defines the bone regenerative mechanism of GNPs through different dimensions ranging from the modulation of scaffold properties to the development of vascular networks and their interplay studies. Finally, the last part of the review unfolds the toxicological aspects of GNPs explored so far and the associated future opportunities rendered by them in bone tissue engineering.Osseous tissue repair has advanced due to the introduction of tissue engineering. The key elements required while engineering new tissues involve scaffolds, cells, and bioactive cues. The macrostructural to the nanostructural framework of such complex tissue has engrossed the intervention of nanotechnology for efficient neo-bone formation. Gold nanoparticles (GNPs) have recently gained interest in bone tissue regeneration due to their multimodal functionality. They are proven to modulate the properties of scaffolds and the osteogenic cells significantly. GNPs also influence different metabolic functions within the body, which directly or indirectly govern the mechanism of bone reg...