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The aim of the present work was to assess the merits of an actively targetable nanoparticles (ATN), PEG-coated biodegradable polycyanoacrylate nanoparticles (PEG-nanoparticles) conjugated to transferrin, for paclitaxel delivery. PEG-nanoparticles loading paclitaxel were prepared by solvent evaporation technique in advance. ATN were prepared by coupling of transferrin to PEG-nanoparticles. The results showed that the average encapsulation efficiency of ATN was 93.4 ± 3.6% with particle size (101.4 ± 7.2 nm) and zeta-potential (−13.6 ± 1.1 mV). The paclitaxel loaded ATN exhibited a low burst effect with about only 16.2% drug release within the first phase. Subsequently, paclitaxel release profiles displayed a sustained release phase. The amount of cumulated paclitaxel release over 30 days was 81.6%. ATN exhibited a markedly delayed blood clearance in mice, and the paclitaxel level from ATN remained much higher at 24 h compared with that of free drug from paclitaxel injection. The distribution profiles of ATN in S-180 solid tumor-bearing mice after intravenous administration showed the tumor accumulation of paclitaxel increase with time, and the paclitaxel concentration in tumor was about 4.8 and 2.1 times higher than those from paclitaxel injection and PEG-nanoparticles at 6 h after intravenous injection. For mice treated with 20 mg/kg × 5 of ATN, the decrease in body weight was limited within 4% of the initial weight at 5 days after the final administration, and tumor regression was significantly observed with complete tumor regression for five out of nine mice. The tumor burden with ATN-treated mice was much smaller compared with free paclitaxel or NTN-treated mice. In addition, the life span of tumor-bearing mice was significantly increased when they were treated with ATN, in particular, three mice survived over 60 days. Thus, PEG-coated biodegradable polycyanoacrylate nanoparticles conjugated to transferrin could be an effective carrier for paclitaxel delivery.