Doxorubicin-loaded nanocarriers were produced employing folate-modified polyethylene glycol (PEG)-functionalized gold nanoparticles for targeted delivery to positive folate-receptor cancer cells. Doxorubicin and folate were, respectively, conjugated to activated-folate and activated-PEG. The conjugates formed doxorubicin nanocarrier with an average size of 12 nm in diameter. The drug release response of functionalized gold nanoparticles was characterized by an initial rapid drug release followed by a controlled release. The doxorubicin nanocarriers showed higher cytotoxic effect on folate-receptor-positive cells (KB cells) than folate-receptor-negative cells (A549 cells). Cell viability in healthy cells (HFF cells) in drug-loaded nanoparticles was higher compared to free doxorubicin. These nanocarriers might offer a cancer therapy with high targeting efficiency and lower side effects.