The study was to develop paclitaxel-loaded formulations using a novel type of self-assembled nanoparticles thatwas composed of block copolymers synthesized from poly(
![](/images/gifchars/gamma.gif)
-glutamic acid) and poly(lactide) via a simple couplingreaction. The nanoparticles (the NPs) were prepared with various feed weight ratios of paclitaxel to block copolymer(the P/BC ratio). The morphology of all prepared nanoparticles was spherical and the surfaces were smooth.Increasing the P/BC ratio significantly increased the drug loading content of the prepared nanoparticles, butremarkably reduced the drug loading efficiency. The release rate of paclitaxel from the NPs decreased significantlyas the P/BC ratio increased. For the potential of targeting liver cancer cells, galactosamine was further conjugatedon the prepared nanoparticles (the Gal-NPs) as a targeting moiety. It was found that the activity in inhibiting thegrowth of HepG2 cells (a liver cancer cell line) by the Gal-NPs was comparable to that of a clinically availablepaclitaxel formulation, while the NPs displayed a significantly less activity. This may be attributed to the factthat the Gal-NPs had a specific interaction with HepG2 cells via ligand-receptor recognition. Cells treated withdistinct paclitaxel formulations resulted in arrest in the G2/M phase. The arrest of cells in the G2/M phase washighly suggestive of interference by paclitaxel with spindle formation and was consistent with the morphologicalfindings presented herein. In conclusion, the active targeting nature of the Gal-NPs prepared in the study may beused as a potential drug delivery system for the targeted delivery to liver cancers.