Cisplatin is one of the most effective cytotoxic agents against cancers. Its usage, however, is limited because of severe resistance and systemic toxicity. A formulation of cisplatin-loaded Au-Au(2)S nanoparticles (NPs) with near-IR (NIR) sensitivity is reported to partly overcome this limitation in this paper. NIR sensitive Au-Au(2)S NPs were successfully synthesized by the reduction of tetrachloroauric acid (HAuCl(4)) using sodium sulfide (Na(2)S), and cisplatin was loaded onto Au-Au(2)S NPs via a MUA (11-mercaptoundecanoic acid) layer. To further investigate the biological safety of cisplatin-loaded Au-Au(2)S NPs, three different cell lines were used to investigate the acute cytotoxicity and the long-term potential carcinogenicity in vitro. Cisplatin-loaded Au-Au(2)S NPs were also tested for limited hemocompatibility in vitro. Our in vitro short and long-term data provided preliminary evidence suggesting that cisplatin-loaded Au-Au(2)S NPs with NIR sensitivity are nontoxic below the maximum recommended dosage. Copyright 2007 Wiley Periodicals, Inc.