Due to its abundance in nature and low cost, starch is one of the most relevant raw materials for replacing synthetic polymers in a number of applications. It is generally regarded as non-toxic, biocompatible, and biodegradable and, therefore, a safe option for biomedical, food, and packaging applications. In this review, we focused on studies that report the use of starch as a matrix for stabilization, incorporation, or release of bioactive compounds, and explore a wide range of applications of starch-based materials. One of the key application areas for bioactive compounds incorporated in starch matrices is the pharmaceutical industry, especially in orally disintegrating films. The packaging industry has also shown great interest in using starch films, especially those with antioxidant activity. Regarding food technology, starch can be used as a stabilizer in nanoemulsions, thus allowing the incorporation of bioactive compounds in a variety of food types. Starch also presents potential in the cosmetic industry as a delivery system. However, there are still several types of industry that could benefit from the incorporation of starch matrices with bioactive compounds, which are described in this review. In addition, the use of microbial bioactive compounds in starch matrices represents an almost unexplored field still to be investigated.