Niosomes are vesicular nanocarriers and are receiving much attention as potential transdermal drug delivery systems due to properties such as enhanced drug penetration, local depot for sustained drug release, and a rate-limiting membrane for modulation of systemic absorption of drugs via the skin. Several mechanisms have been proposed to explain the ability of niosomes to increase drug transfer through the skin. Niosomal carriers are suitable for the transdermal delivery of numerous pharmacological agents, including antioxidant, anticancer, anti-inflammatory, antimicrobial, and antibacterial molecules, and this review attempts to provide an exhaustive collection of recent investigations in this interesting field, with special emphasis on the strategies used to enhance the potential of niosomes.