¹Faculty of Pharmacy, University of Indonesia, Depok, Indonesia DOI : 10.35333/jrp.2019.39 The potential benefits of resveratrol (Trans-3, 5, 4’-trihidroxy stilbene) as an anti-cancer are lowered because of it’s low aquous solubility, instability and low bioavailability. Recent progresses in nanoparticle technology offer a promising loophole to solve many problems in developing theurapetic agents. The ability of a nanocarrier to selectively bring drug substances to the site of a tumor solely based on passive targeting can be enhanced by coupling a ligand to the surface of the nanocarrier knowingly as active targeting. This research aimed to test the cytotoxic activity of resveratrol conjugated to gold nanoparticles-folate as a carrier. Gold nanoparticles (AuNp) was chosen as a suitable carriers to increase the potency of resveratrol (Rsv) as an anti cancer agent with the help of folic acid (FA). The expression of folate receptors are hightened due to the excessive need of folic acid by certain types of cancer cells. Thus folic acid can act as a targeting agent to help introduce gold nanoparticles to the target cells. Furthermore, the cytotoxic activity of the final conjugate (FA-AuNp-Rsv) will be tested against human breast cancer MCF-7 cell line using MTT cholorimetric test. Gold nanoparticles were fabricated using optimized amount of polyvinyl alcohol (PVA) as a stabilizers. FA were attached to the surface of gold nanoparticles using 4-Aminothiophenol (4-Atp) as a linker. The carboxilic group of FA was first activated using common EDC-NHS reaction and reacted with amine group of 4-Atp to form amide bond. The physical and chemical characterization has been conducted and it was found that the final 86.9 nm nanoconjugate (FA-AuNp-Rsv) were successfuly synthesized with good stability and possesed an elevated activity (IC50=21.28 ± 1.04 μM) compared to resveratrol alone (49.94 ± 1.06 μM). Thus this results were hoped to be an adequate addition to the development of nanotechnology in cancer therapy. Keywords : Cytotoxic activity; gold nanoparticles; resveratrol; MTT method; MCF-7 cells