Abstract: Recent advances in nanotechnology have greatly facilitated the development of nanoparticle drug delivery system. The present work reviews recent literature on nanotechnology-based applications and developments of silymarin preparation. A variety of nanoparticle formulations have been extensively investigated to improve the absorption and bioavalability of silymarin, including: improving the drug dissolution signficantly(such as nanosuspensions, inclusion complex with β-cyclodextrins, self-emulsifying drug delivery systems, solid dispersions, micronization), promoting the permeability across cell membrane(such as complexation with phospholipids, nanostructured lipid carriers)and other methods(such as micelles, mesoporous silica nanoparticles, polyamidoamine dendrimers). The applications of nanoscience and nanotechnology can help to promote the further pharmaceutical development of silymarin.