Protocatechuic acid (PCA) has antioxidant, anticancer, and antidiabetic properties. However, its poor water solubility affects its absorption and bioavailability. Bovine serum albumin nanoparticles (BSA-NPs) can encapsulate significant amounts of hydrophobic substances by attracting charged molecules through electrostatic adsorption. This study aimed to prepare PCA-loaded BSA nanoparticles, producing PCA-BSA-NPs, and subsequently characterize the resulting nanocomposite using zeta potential, dynamic light scattering, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). In vitro, PCA-BSA-NPs were evaluated for their anticancer, antioxidant, and free radical scavenging properties. Our data indicated that the average particle size of PCA-BSA-NPs was 202 nm. The in vitro study demonstrated that PCA-BSA-NPs exhibited potent anticancer activity comparable to doxorubicin. Additionally, PCA-BSA-NPs displayed highly antioxidant activity (2,2-diphenyl-1-picrylhydrazyl (DPPH), superoxide dismutase (SOD) like activity, and catalytic activity) and a strong antidiabetic effect (alpha-amylase inhibition). The drug release study indicated the effective release of PCA from PCA-BSA-NPs at pH = 6.5, which is suitable for targeting cancer cells. In conclusion, PCA-BSA-NPs could provide a more effective and safer alternative to traditional chemotherapeutic agents like doxorubicin. Moreover, their higher antioxidant and antidiabetic activities could expand their therapeutic applications, making them valuable in treating oxidative stress-related diseases and diabetes.