TPGS/Solutol polymeric micelles was prepared to load together insoluble paclitaxel (PTX) and soluble S-HM-3(PHTSm), expecting to together deliver them to the tumor site with long-circulating, targeting function and combating multi-drug resistance (MDR). As the result,micelles exhibited smooth spherical morphology and  low critical micelle concentration (CMC) value. The results of in vitro cell assay proved that PTX were slowly released  and S-HM-3 could be easier to get into MDA-MB-231 cell, and its angiogenesis inhibition ability was also enhanced after integrating into micelles.  The results of in vivo studies showed that the half-life of S-HM-3 and PTX was significantly prolonged 25.27 and 5.54 folds, and their AUC0–∞ was enhanced 129.78 and 15.65 times, respectively. Meanwhile 83.05% tumor inhibition rate of PHTSm was achieved compared with 59.99% of PTX.