Objective:To explore the fabrication of poly（vinyl alcohol）（PVA）-lipoic acid（LA） polymers and to study the basic physicochemical properties

as well as the anti-breast cancer cell activity;to preliminarily evaluate the biodistribution of PVA27 K-4%LA in breast cancer-bearing mice. Methods:"One-step"method was used to fabricate the PVA27 K-4%LA polymer. The mean particle size

poly dispersity and ζ potential were detected using dynamic light scattering;the morphology was observed under transmission electron microscope（TEM）;the cytotoxicity of the polymer was studied. Dialysis method was employed to incorporate Doxorubicin（DOX）into PVA27 K-4% LA. The drug content

drug release rate

cell uptake and cytotoxicity were further investigated. The breast cancer-bearing mouse model was established

and study the biodistribution of the nanoparticles in vivo. Results:PVA27 K-4%LA can be self-assembled into nanoparticles in water solution

which was irregular in shape when observed under TEM. The mean particle size

poly dispersity and ζ potential were（8.30 ±3.02） nm

（0.129 ±0.063） and（-26.68 ±0.98） m V respectively. The encapsulation efficiency was 86.12%;dialysis method was used to incorporate DOX into PVA27 K-4%LA. The morphology of PVA27 K-4%LA-DOX was similar with that of PVA27 K-4%LA. The mean particle size

poly dispersity and ζ potential were（9.35 ±3.30） nm

（0.114±0.056） and（-28.57 ±1.63） m V respectively（P value were0.023

0.0512 and 0.332 respectively）. The DOX released from PVA27 K-4%LA-DOX was much faster in the first 4 hours. On the24 th hours

about 60% of the DOX was released. The breast cancer cells MDA-MB-231 could uptake PVA27 K-4%LA-DOX quickly. The cancer cells could be killed efficiently

with the IC50 of537.3 ng/m L（P =0.005）. PVA27 K-4% LA accumulated in tumor site

and reached highest dose at the 24 th hour. Liver

lung and spleen also had PVA27 K-4%LA distribution. Conclusion:PVA27 K-4%LA could be self-assembled into irregular nanoparticles in water solution. DOX could be incorporated into PVA27 K-4%LA efficiently. PVA27 K-4%LA-DOX could be uptaken by breast cancer cells MDA-MB-231

and could kill the cancer cells via releasing DOX gradually. PVA27 K-4%LA nanoparticles could targeted accumulate in the tumor site of breast cancer-bearing mice.