The pharmaceutical industry is at the forefront of a technological revolution, with researchers concentrating on creating new methods of oral medication delivery. Tablets and capsules are examples of conventional dose forms; however, these forms are linked to issues such as low bioavailability, adverse effects, frequent administration, and patient noncompliance. Instead of relying on antiquated methods, researchers explored new avenues for the administration of medicine. Current methods of drug delivery can shield bioactive compounds—including plant-based substances, proteins, and peptides—from the enzymes found in bodily fluids and other potentially harmful physical and chemical factors, thereby increasing the therapeutic index and the efficacy of pharmaceuticals. In this chapter, the most recent developments in the design of novel delivery methods for bioactive molecules, proteins, peptides, and extracts from plants, with the aim of overcoming the aforementioned obstacles has been discussed in detail. Additionally, a wide range of potential uses and upcoming developments has also been emphasized.