The final FA-HSA-RES-NPs showed spherical shape, proper size (~102 nm), high encapsulation efficiency (EE; ~98%, with RES amorphously encapsulated and in low crystallinity) and drug loading (DL; ~15%), superior cell uptake rate and antiproliferative activity in vitro than RES (IC50 = 110.8 μM vs. IC50 = 152.7 μM in HepG2 cells), and optimal tumor-targeting ability (detected in vivo by near-infrared imaging in tumor-bearing mice). Here, ALB is linked to neoplasm.