In order to achieve the benefits of targeted drug delivery, this study intended to encapsulate doxorubicin in a linear polyamidoamine and its PEGylated co-polymer. The drug was loaded by using the emulsion solvent evaporation method. By adjusting the doxorubicin to polymer ratios to 1:10, 1:20 and 1:30, three formulations of each polymer/copolymer were prepared. The drug release profile was investigated using phosphate buffered saline. In vitro cytotoxicity investigation was executed on liver cancer cell line (Hep G2 cell lines) by 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay. The outcome demonstrated that doxorubicin had been successfully loaded on polyamidoamine and its PEGylated co-polymer with a drug loading efficiency of about 90%. Nanocarrier sizes were between 245±1.10 nm -579±1.00 nm and the zeta potential range was +22.4±0.5 mV-+37.9±0.3 mV. In-vitro drug release investigations revealed a characteristic pH-dependent drug release. The cytotoxicity testing of optimal formulation revealed that the doxorubicin was successfully released from the formulations and exerted therapeutic effect. According to our research, doxorubicin could be loaded onto linear polyamidoamines for potent antitumor effects on the target liver cancer cell lines (Hep G2).