In recent years, the Pharmaceutical industry has witnessed remarkable advancements in drug delivery technologies, a trend expected to continue. Among the various dosage forms, tablets remain one of the most preferred options due to their practicality, ease of administration, and patient compliance. Innovations in tablet formulations have opened doors to enhanced customization of therapeutic agents, optimizing their effectiveness. Numerous novel drug delivery systems have been developed, providing improved therapeutic outcomes and addressing challenges associated with traditional formulations. This review highlights one such innovative approach, tablet-in-tablet systems. These systems offer significant advantages, such as sustained release of active pharmaceutical ingredients (APIs) and improved safety profiles, while ensuring better patient adherence. By transforming conventional drug delivery methods, such as injectables or oral solid dosage forms, into advanced formulations, tablet-in-tablet technology holds immense potential to revolutionize drug administration practices.