In recent years, consumers' demand for cosmeceutical products with protective and therapeutic functions derived from natural sources have caused this industry to search for alternative active ingredients. Bioactive peptides have a wide spectrum of bioactivities, which make them ideal candidates for development of these cosmeceutical products. In vitro studies have demonstrated that bioactive peptides (obtained as extracts, hydrolysates, and/or individual peptides) exhibit biological properties including antioxidant, antimicrobial, and anti-inflammatory activities, in addition to their properties of inhibit aging-related enzymes such as elastase, collagenase, tyrosinase and hyaluronidase. Some studies report multifunctional bioactive peptides that can simultaneously affect, beneficially, multiple physiological pathways in the skin. Moreover, in vivo studies have revealed that topical application or consumption of bioactive peptides possess remarkable skin protection. These properties suggest that bioactive peptides may contribute in the improvement of skin health by providing specific physiological functions, even though the mechanisms underlying the protective effect have not been completely elucidated. This review provides an overview of in vitro, in silico and in vivo properties of bioactive peptides with potential use as functional ingredients in cosmeceutical field. It also describes the possible mechanisms involved as well as opportunities and challenges associated with their application.