Abstract：Genistein doped mannoseconjugated PEGmodified liposomes (manPEG@LP/Ge) were prepared via filmsonic method by using targeted lipid DSPEPEGman and helper lipid DOTAP. Concanavalin A (ConA) agglutination assay had proved that mannose has been modified to nanoliposomes successfully. The asprepared manPEG@LP/Ge were spherical in shape with a homogeneous size distribution around (270±15) nm in diameter as characterized by SEM. The Zeta potential was +7.5 mV in pure water. Furthermore, manPEG@LP/Ge appeared to be very homogeneous and stable in water. It is considered that the sterichinerance effects of surface PEG long chain and the strong electrostatic repulsion of the positive charge play an important role in the good dispersion of manPEG@LP/Ge. Flow cytometry examination confirmed the targeting specificity of manPEG@LP/Ge against human hepatoma Huh7 cells which are of overexpression of mannose receptors. The cell toxicity viability demonstrated that unloaded manPEG@LP are practically nontoxic, indicating that the drug delivery vehicles possess excellent biocompatibility. Systematic in vitro and in vivo studies showed that the manPEG@LP/Ge kill tumor cells with high specificity and excellent efficiency, owing to the mannosemediated active tumortargeted drug delivery.
