Tanshinone IIA nanoparticles were constructed and perfused in rabbit's right carotid after intimal denudation with ballon. Localization and retention at different time points of the coumarin-labeled drug nanoparticles were evaluated under laser confocal microscope. Nanoparticles were seen in the three layers of the cross-section artery. At 7 days, they were mainly deposited in the medial layer, while the deposition was generally observed in the adventitia and media at 14 days and 28 days. In the Tanshinone IIA nanoparticle study, a significant reduction of the neo-intimal hyperplasia was noted by comparing the intimal area and the intima-media ratio in the three groups. And the PLGA nanoparticles appeared to be fully biocompatible. As a result, the local administration of the nanoparticles with incorporated Tanshinone IIA showed not only the preventive effects, but aslo the high absorption and good biocompatability in the whole arterial wall.