2018 Volume 33 Issue 4 Pages 259-267
The skin consists of at least three compartments, epidermis, dermis, and hypodermis. Stratum corneum outside of epidermis generally acts as a physical barrier for transdermal absorption of most of therapeutic agents after topical application, whereas biological barrier may also exist at epidermis and dermis. Recent studies have clarified functional expression of a variety of transporters in the latter barrier. Transporters involved in dermal homeostasis could be a target of novel therapeutic agents. On the other hand, a certain type of anticancer agents exhibit severe dermal toxicity after systemic administration, and transporters may play fundamental role in their dermal distribution and toxicity. In this chapter, we summarized the latest information on which transporters are expressed in the skin. Their possible involvement in dermal homeostasis, transdermal absorption after topical application, and dermal distribution after systemic administration of therapeutic agents will also be discussed.