OBJECTIVE：To study distribution and targeting of Gardenia jasminoides extract niosomes in rats. METHODS：G. jasminoides extract niosomes were prepared by modified thin film dispersion method. 30 rats were randomly divided into G. jasminoides extract group（57 mg/kg）and G. jasminoides extract liposome group（131 mg/kg）according to their weight. They were given relevant medicine intragastrically，once a day，for consecutive 7 days. 1 h after last administration，heart，liver，spleen，lung and kidney tissue were isolated，and HPLC method was adopted to the contents of active ingredients gardenoside in them. The targeting of G. jasminoides extract niosomes was evaluated by DTI quantitatively. RESULTS：Compared with G. jasminoides extract group， the contents of gardenoside in heart，spleen and brain tissue of rats increased significantly in G. jasminoides extract niosomes group （P＜0.01），and DTI were 1.718，1.972 and 13.071；the contents of gardenoside in liver and kidney decreased significantly（P＜ 0.01），and DTI were 0.431 and 0.467，respectively. CONCLUSIONS：G. jasminoides extract niosomes change the distribution of gardenoside in rats，showing brain targeting effect and decreasing first pass effect for liver.