In tabletized nanomedicine, the dynamic interplay between nanoformulations and the complex environment of the gastrointestinal tract plays a pivotal role, particularly in relation to the luminal, mucosal, and epithelial cells. This work describes the perspectives and opportunities of nanoformulations for the development of tabletized nanomedicine, including the integration of nanomedicine within tablet formulations to support the controlled release of drugs, biomolecules, and agents for improved therapeutic response. It also explores current trends in nanomedicine technology, such as bacteriophage, probiotic, and oligonucleotide tabletized nanomedicine, as well as the combination of nanomedicine with imaging agents, known as nanotheranostics.