Background and Objectives: Nanotechnology is becoming a new yet practical means in drug delivery with better therapeutic outcomes and less systemic toxicity. PSNPs have been the focus of extensive research due to their large surface area, adjustable pore size, good biocompatibility, and ability to provide controlled drug release, which makes them excellent agents for delivering anticancer drugs. Objective: To synthesize and characterize the chemotherapeutic agent 5-fluorouracil (5-FU) loaded PSNPs and to investigate the possibility of these drug carriers as effective tools in targeted anticancer therapy. Material and Methods: The sol-gel technique was employed to synthesize PSNPs using tetraethyl orthosilicate as precursor. The nanoparticles were loaded with 5-FU and analyzed by SEM, EDX and UV–vis spectroscopy to determine morphology, elemental composition and drug encapsulation respectively. In vitro studies were done to assess cytotoxicity against cancer cell lines and antioxidant activity of drug loaded nanoparticles. Result: SEM revealed consistent, spherical, and porous nanoparticles which facilitate in drug loading process. The purity of the silica and hence successful drug loadingeventually was confirmed by EDX. UV–Vis spectra indicated the 5-FU retained its structural characteristic after encapsulation. The results of cell viability assays showed a pronounced decrease in the survival of cancer cells treated with 5-FU loaded PSNPs as compared to the free drug, suggesting improved efficacy. Antioxidant test indicated significant additional therapeutic advantage by reducing oxidative stress. Conclusion: PSNPs could efficiently encapsulate 5-FU and release the drug in a controlled manner, with enhanced anticancer effect. Together, these results poise PSNPs as potential candidates for the development of targeted and less toxic cancer therapy. Additional in vivo studies are warranted to prove clinical relevance.