To improve the skin permeation of theophylline and cianidanol ((+)-catechin), the essential oil of Magnolia fargesii was evaluated using in-vitro and in-vivo permeation techniques. Oxygenated monoterpenes and sesquiterpenes are the major components of M. fargesii essential oil. The in-vitro permeation of theophylline and cianidanol was significantly enhanced after treatment with M. fargesii essential oil. The essential oil increased the in-vivo skin deposition of cianidanol but not theophylline. On the other hand, in-vivo microdialysis showed a higher subcutaneous theophylline amount after essential oil treatment. In-vitro cell viability and prostaglandin E(2) release by skin keratinocytes indicated that there was low or negligible cytotoxicity by M. fargesii essential oil. The in-vivo skin tolerance study determined by transepidermal water loss and colorimetry confirmed that no irritation of the skin was detected when using M. fargesii essential oil.