OBJECTIVE： To prepare Pteris semipinnata extract 5F-liposome modified by pentapeptide YIGSR （YIGSR-5F-LP） and study its physicochemical property. METHODS： 5F-LP were prepared by film-dispersion and ultrasonic method. Using encapsulation efficiency as index， orthogonal test was adopted to investigate the effects of phospholipid-cholesterol mass ratio， drug-lipid mass ratio， ultrasonic reaction time and temperature on the preparation of liposome. The appearance of drug-loaded liposome was modified by post-insertion method， and 5F-LP modified with pentapeptide YIGSR was prepared. The morphology and particle size of the liposome were also observed by TEM， and encapsulation efficiency of liposome was determined by protamine precipitation method. The content of 5F in liposome was determined by HPLC， and in vitro drug release of liposome was evaluated by dialysis method. RESULTS： The optimal preparation technology was as follows as phospholipid-cholesterol mass ratio of 6 ∶ 1， mass ratio of drug-lipid 1 ∶ 10， ultrasonic time 10 min， temperature 45 ℃. The prepared YIGSR-5F-LP was sphere or sphere type in shape with average particle size of 174. 8 nm， encapsulation efficiency of 88.9％ and drug-loading amount of  8.2％. The release of liposome in vitro was slower than that of 5F solution and relased completely at 48 h. CONCLUSIONS： YIGSR-5F-LP is prepared successfully； and the YIGSR-5F-LP has sustained release property.