The skin presents several advantages as an administration route, including the possibility of localizing drugs in the tissue and overcoming the first-pass effect. However, its use is limited by the barrier function of the tissue, which is provided mainly (but not exclusively) by the stratum corneum. Various strategies to overcome this layer, have been considered over the years, ranging from the use of physical methods such as iontophoresis to wellknown conventional chemical penetration enhancers like oleic acid and DMSO. However, delivery of hydrophilic and large compounds remains a challenge. More recently, selected groups of peptides have attracted increasing attention due to their ability to penetrate into the skin promoting the transport of small and large molecules, including nanodispersed systems. Here, we will discuss the properties and application to cutaneous (into the skin) and transdermal (across the skin) delivery of three groups of peptides, namely protein-transduction domains, phage-displayed peptides and antimicrobial peptides.