Objective: To study inhibitory effect of folate receptor active targeting docetaxel-loaded liposomes (FA-PDCT-L) on S180 cell transplanted tumor and its in vivo toxicity in mice. Method: A self synthesized amphiphilic copolymer

folate-poly (PEG-cyanoacrylate-co-cholesteryl cyanoacrylate) (FA-PEG-PCHL) was used as liposomal modifying material to form FA-PDCT-L.Confocal laser scanning microscopy was adopted to detect affinity between liposomes and MCF-7 cells.Subcutaneous transplanted model of S180 sarcoma was made.Tumor mice were randomized into 4 groups

such as docetaxel (DCT) injection (DCT-I)

unmodified DCT-loaded liposomes (DCT-L)

FA-PDCT-L and model group (saline)

dosages were 10 mg·kg-1·d-1 through tail vein.Tumor weight and inhibition rate of tumor were detected at the end of experiments

tumor cell apoptosis was analyzed by TUNEL.Hepatic function and hematology assay for myelosuppression were evaluated. Result: FA-PDCT-L had better affinity to cells than the other two reference preparation.Compared with model group

weight of tumor in DCT-I

DCT-L and FA-PDCT-L were decreased

especially for FA-PDCT-L

its inhibitory rates was 79.03% with apoptosis index at (45.7±3.4)%.There was no significant difference of hepatic function and hematology assay between the FA-PDCT-L group and the blank group. Conclusion: FA-PDCT-L is internalized into cells by mediation of FA-PEG-PCHL with better anti-tumor activity and lower in vivo toxicity by compared with DCT-I.