We have created a mechanism for delivering drugs using nanoparticles. The system contained transferrin, paclitaxel (PTX), and PLGA (TF). Through intravenous delivery, this approach can target liver cancer cells with particularity. In vitro, the PLGA-PTX-TF nanoparticles exhibit outstanding anti-liver cancer activity (IC50 = 4.79 g/mL) and are dose-dependent. In vivo, the PLGA-PTX-TF nanoparticle has significantly more anti-tumor activity than PLGA-PTX (anti-cancer rate: 79.09% vs. 35.47%). As a result, PLGA-PTX-TF nanoparticles can be regarded as a successful anticancer drug delivery method for the treatment of liver cancer in clinical settings. We have created an in vitro and in vivo targeted nanoparticle medication delivery system for liver cancer cells. The liver cancer therapeutic effects of the PLGA-PTX-TF nanoparticles are outstanding. There is almost no cytotoxicity in the PLGA empty nanoparticles. The anti-tumor activity of the PLGA-PTX-TF nanoparticle is clearly visible in vivo. We can fairly infer from the aforementioned results that PLGA-PTX-TF nanoparticles are an efficient anticancer medication delivery technology for the treatment of liver cancer.