The field of regenerative medicine is vastly growing, with its applications ranging from many acute to chronic disease conditions. While the body’s natural regenerative and healing properties play a vital function as a part of the defense mechanism, external influence to boost the body’s regenerative traits has gained significant traction in recent years. The incorporation of nanoparticles in regenerative drug delivery aims to enhance bioavailability, improve biological barrier crossing, create sustained drug release, and deliver compounds to desired sites. Numerous polymeric, organic, and inorganic nanomaterials are explored due to their wide applicability and significant success in delivering biomolecules. The range of nanomaterials to choose from also allows the delivery of a diverse list of molecules, such as small biomolecules, peptides, and genes for tissue engineering and regeneration. Here, we discuss a repertoire of nanocarriers designated for tissue regeneration and their extensive therapeutic applications in this field. We also explore further the current trends in using various nanocarriers based on their physicochemical characteristics and compatibility with the therapeutic molecules for tissue engineering and regeneration.