Shikonin is a naphthoquinone isolated from Arnebia species such as Arnebia euchroma. The dried root of A.euchroma is a traditional Chinese medicine with anti-inflammatory and antiviral activities. Though there are about 500 publications on shikonin, no clinical trials for shikonin and its derivatives have been reported yet because of inherent properties such as poor solubility in water and low bioavailability. Therefore, it is of great importance to conquer these problems to exploit the clinical potential of shikonin and its derivatives.