Green solvents such as ionic liquids (ILs) unlock possibilities for developing
innovative biomedical and pharmaceutical solutions. ILs are the most investigated solvents for
compound extractions, as reaction media and/or catalysts, and a desired eco-friendly solvent to
process biomacromolecules for biomaterial production. Investigations demonstrate that the
tunable nature and physicochemical features of ILs are also beneficial for building up delivery
systems through their combination with bioactive compounds. Bioactive compounds from
synthetic origins, like ibuprofen, ketoprofen, and natural sources such as curcumin, flavonoids,
and polyphenols are essential starting points as preventive and therapeutic agents for treating
diseases. Therefore, the association of those compounds with ILs opens up windows of
opportunities in this research field. This Review assesses some of the main and important
recent information and the current challenges concerning delivery platforms based on ILs
combined with bioactive compounds of both natural and synthetic origins. Moreover, the
chemistry, bioavailability, and biological functions of the main bioactive compounds used in
the ILs-based delivery platforms are described. These data are presented and are discussed,
together with the main delivery routes of the systems.