To study the preparation, activity and targeting ability evaluation in vitro on epigallocatechin-3- gallate (EGCG) bovine serum albumin nanoparticles targeting to PC-3 cells, the folate mediated EGCG bovine serum albumin nanoparticles (FA-EGCG-BSANP) were prepared by desolvation process.  The morphology and particle size of the nanoparticles were determined by atomic force microscope (AFM).  HPLC was used to analyse the entrapment efficiency and drug loading rate of EGCG.  The amount of folate conjugation on the BSANP  was determined by quantitative ultraviolet (UV) spectrophotometer analysis.  The targeting ability to PC-3 was observed using laser scanning confocal microscope (LSCM) and fluorophotometer microscope.  And the activity of FA-EGCG-BSANP was mensurated by MTT method.  The morphology and particle size distribution of FA-EGCG-BSANP were uniform and even with the mean particle size of 200 nm.  The entrapment efficiency and loading rate of EGCG were (81.5 ± 1.8) % and (29.3 ± 0.6) %, respectively, and the amount of folate conjugation was 18.363 μg·mg⁻¹ BSA.  The FA-EGCG-BSANP uptakes by cultured PC-3 cells were 23.65 times the amount of EGCG-BSANP in a concentration dependant manner.  The lethality of PC-3 cells treated with FA-EGCG-BSA was 82.8%, while those treated with EGCG and EGCG-BSANP were 58.6% and 55.1%, respectively.  And   lethality of PC-3 cells was positively correlated with the nanoparticles uptake amount.  FA-EGCG-BSANP  can significantly promote EGCG to PC-3 cells sites and improve their efficacy, which is considered to an experimental foundation for further research on its activity, targeting ability and metabolism in vivo.