Nanosphere Coated with Lactosyl-Polystyrene Polymer as a Targeting Carrier to Hepatocytes

Polystyrene-latex nanosphere (PSL-NS, mean diameter: 85 nm) was coated with lactosyl-polystyrene polymer (PVLA, high affinity to hepatocytes) to evaluate its targeting characteristics to hepatocytes and PSL-NS surface hydrophilicity. Hepatocytes were adhered specifically with PVLA-coated dishes made of the same material as PSL-NS. Flow-cytometry investigation showed that PVLA-coated fluorescein-isothiocyanate (FITC)-PSL-NS was taken up by hepatocytes compared with noncoated FITC-PSL-NS as a control. These findings indicated PVLA-PSL-NS could target to hepatocytes. The surface of PVLA on PSL-NS had a higher hydrophilicity than polyethyleneglycol 6,000, Tween 80, poloxamer 407, and poloxamer 908, which indicated that PVLA-PSL-NS may avoid the reticuloendothelial system capture and have a long plasma duration after intravenous administration in vivo. Plasma coagulation can be prevented by the addition of polyvinylalcohol (0.1%) in PVLAPSL-NS solution when PVLA-PSL-NS was injected. We concluded that PVLA-PSL-NS is one of the most potential hepatocyte targeting carriers for injectable formulations.