The study described the development of lipid vesicles as colloidal carriers for uricase, an enzyme with low activity at physicological conditions and low stability in vitro and in vivo. The lipid vesicles containing uricase (UOXLVs) were prepared and the process parameters were optimized with the indexes of entrapment efficiency, polydispersion, particle size, and zeta potential. The storage stability of uricase in lipid vesicles was significantly increased compared to that of free uricase at 4°C. The stability to proteolytic digestion was also increased obviously by entrapping the uricase in the lipid vesicles. In vitro and in vivo pharmacodynamic studies on the hyperuricemia rat model explicitly suggested that the uricase entrapped by UOXLVs possessed high uricolytic activity and distinctively decreased the uric acid level.