The knowledge of a drug’s biopharmaceutical profile is of paramount importance to design dosage forms able to overcome the countless drug delivery challenges. To this purpose, control over the way the drug is released from the pharmaceutical form is fundamental, along with the insightful understanding of all pathophysiological factors that strongly influence the drug’s bioavailability and fate in the body. Although generally well addressed, many biopharmaceutical aspects remain challenging and require a continuous learning effort.