Amino acids are natural compounds that can be safely used in pharmaceutical applications. Considering the great interest in the amino acids used in the pharmaceutical industry, this article presents an overview of investigations reported in recent years. In this regard, the first sections begin with an introductory description of the properties, classification and safety of amino acids, while in the other sections the most common methods for the preparation of amino acids formulations and their application on solubilization, permeation and stabilization of several active pharmaceutical ingredients are described. Furthermore, available data about the multicomponent systems approach is included. Lastly, the impact of amino acids formulations on therapeutic efficacy is explored. The advantages illustrated suggest that amino acids are capable of improving the biopharmaceutical properties of drugs.