High-quality water-soluble quantum dots had been synthesized following the one-step method. Furtherly, the impact factors on the optical properties of quantum dots, which were the feed ratio of S/In and the reflux time, had been concerned emphatically. By changing the reaction parameters, we made the fluorescence emission of ZnInAgS quantum dot tunable from green to orange, and the maximum fluorescence quantum efficiency was up to 30%. Then we modified bovine serum albumin (BSA) on the surface of ZnInAgS quantum dot, which was conjugated with BSA-QDs through the linker of 3'3-dimercapto-diacetate DOX. Finally, the reduction-sensitive drug delivery system based on ZnInAgS quantum dots (QBSSD) was successfully constructed. The resultant QBSSD complex were observed to be significantly stable in aqueous solution. In addition, owing to their cellular reduction responsiveness at the cleavable disulfide linker, the QBSSD complex were able to release DOX rapidly. In vitro drug release and cell level release experiments proved that our QBSSD complexes could make a quick drug release in the environment with GSH. The efficacy experiments showed that our QBSSD complexes exhibited a strong killing effect to cancer cells, and low toxic to normal cells. All the results indicated that the reduction-sensitive drug delivery system was a promising model of administration.