OBJECTIVE: To study the absorption features of Silymarin enteric coated-polyllactic-co-glycolic acid (PLGA) nanoparticles in rat in situ intestine perfusion model and colonic adenoma Caco-2 cell model. METHODS: HPLC method was used to determine the content of silymarin. The absorption rate constant (Ka) and apparent absorption coefficient (Kapp) of Silymarin suspension, Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles were investigated in duodenum, jejunum, ileum and colon of rat in situ intestine perfusion model; the apparent permeability coefficient (Papp) of those drugs containing low-concentration, medium-concentration and high-concentration (20, 40, 60 μg/mL) of silymarin in Caco-2 cell model were also investigated. RESULTS: Compared with Silymarin suspension, Ka and Kapp of Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles were all increased in duodenum, jejunum, ileum and colon (P<0.05); compared with the corresponding concentration Silymarin suspension, two-way Papp of Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles containing low-concentration, medium-concentration and high-concentration of silymarin were all increased in Caco-2 cell model (P<0.05); there was no statistical significance between Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles (P>0.05). CONCLUSIONS: Silymarin enteric coated-PLGA nanoparticles can effectively increase the intestinal absorption, cellular uptake and transmembrane transport rate of silymarin.