The development of pharmaceuticals is increasingly centred on delivery strategies that maximise therapeutic benefits while reducing adverse effects. Multiparticulate drug delivery systems appear to be particularly well-suited for producing controlled and delayed release oral formulations with less chance of dose dumping, according to recent developments. Biopharmaceutical benefits are provided by these oral multiparticulate drug delivery methods in terms of consistent and even distribution and transit inside the gastrointestinal tract. The process of pelletization is a revolutionary drug delivery technique that helps create a site-specific drug delivery system by turning tiny powder particles into pellets. The process known as pelletization makes it possible to create spherical beads or pellets, which typically have a mean diameter of between 0.5 and 2.0 mm. In general, unwanted qualities are eliminated and the physical or chemical properties of fine powders are improved by using pelletization and pellets to improve the flowability, appearance, and mixing capabilities. This prevents excessive dust and reduces segregation. Several methods, including extrusion and spheronization, rotogranulation, solution, suspension, or powder stacking, spray-drying, or spray-congealing, are used to make pellets. This chapter's goal is to provide an overview of some general information regarding pellets, pelletization, and certain widely utilized methods in the pharmaceutical sector.