In studies on wound-dressing materials, bioactive materials have been developed rapidly to accelerate wound healing. In recent years, scientists have studied arginine as a bioactive component due to its excellent biosafety, antimicrobial properties and therapeutic effects on wound healing. Surprisingly, arginine therapy is also used under specific pathological conditions, such as diabetes and trauma/hemorrhagic shock. Due to the broad utilization of arginine-assisted therapy, we present the unique properties of arginine for healing lesions of damaged tissue and examined multiple arginine-based systems for the application of wound healing. This review shows that arginine-based therapy can be separated in two categories: direct supplemental approaches of free arginine, and indirect approaches based on arginine derivatives in which modified arginine can be released after biodegradation. Using these two pathways, arginine-based therapy may prove to be a promising strategy in the development of wound curative treatments.