Diethylenetriaminepentaacetic acid neolactosyl human serum albumin (DTPA-LSA) was prepared and labeled with technetium-99m. The labeling conditions of Tc-99m-DTPA-LSA were optimized, and lyophilized kit was developed for instant preparing of Tc-99m-DTPA-LSA. Tc-99m-DTPA-LSA showed high liver uptake in normal mice (> 96% ID/g at 5 min after injection), and it could be blocked significantly by pre-injecting free neogalactosylalbumin (NGA). Single photon emission computed tomography (SPECT) study was performed in normal Japanese White rabbits and SPECT images with high quality were obtained at 15, 30, 60, and 120 min after injection of the radiotracer. The promising biological properties of Tc-99m-DTPA-LSA combined with the development of reliable and instant lyophilized DTPA-LSA kit afford the opportunity of hepatic receptor imaging for routine clinical assessment of hepatic function. (c) 2012 Elsevier Ltd. All rights reserved.