Ginsenosides are the major bioactive natural compounds derived from Panax ginseng. Several studies report the pharmaceutical benefits of several ginsenosides, including antidementia, antitumor, and anti-inflammatory activity. Biotransformations by gut microbiome contribute to the biological function of these ginsenosides. After ingestion ginsenosides are hydrolyzed to Rg2, Rg3, compound K, and others by human gut flora. Compound K is considered the representative active metabolite after oral administration of ginseng or ginsenosides. Various studies report the diverse biological functions of compound K, such as antitumor, antidiabetic, antiallergic, and anti-inflammatory activity. Recent clinical trial and in vitro studies demonstrate the antiaging activities of ginsenosides in human skin. Ginsenosides have been considered as an important natural dermatological agent. In this review, we will cover the modern tools and techniques to understand biotransformation and delivery of compound K. Also the biological function of compound K on skin disorder and its potential dermatological application will be discussed.