Abstract: OBJECTIVE To introduce the progress on the research in oridonin targeted delivery. METHODS The researches of both domestic and abroad were reviewed in recent years. The targeting principal, efficiency, pharmacokinetics as well as pharmacodynamics were summarized. Its feasibility and prospect in drug delivery system was analyzed. RESULTS Oridonin targeted drug delivery system not only improves the solubility of oridonin, but also accumulates the drug at targeted sites, increases the anti-tumor activity and decreases toxicity. CONCLUSION The future research will focus on the development of kinds of oridonin targeted drug delivery system with high targeting efficiency, safety and economic.