To eliminate the toxic effect of chemotherapy drug of lobaplatin (LBP) on body tissue in liver cancer therapy, this work prepared a nanodrug carrier based on polyethylene glycol-modified carbon nanotubes (PEG–CNTs) and then constructed a targeted drug delivery system (LBP–PEG–CNTs) by loading LBP on PEG–CNTs. Fluorescein isothiocyanate (FITC) was used to label PEG–CNTs to observe the cellular uptake of PEG–CNTs. In addition, the inhibitions of LBP–PEG–CNTs on HepG2 cells were investigated. The results show that the FITC-labeled PEG–CNTs have good cell penetrability; meanwhile, LBP–PEG–CNTs have good stability, pH-controlled release property, and high inhibition rate on HepG2 cells. To be specific, 80% of LBP is released under physiological conditions of liver cancer cells at pH 5.0, and LBP–PEG–CNTs show a high inhibition rate of 77.86% on HepG2 cells, demonstrating that they have targeted, pH-controlled release and inhibition properties on HepG2 cells.