The preparation of 99mTc-DTPA–LSA and its instant lyophilized kit for hepatic receptor imaging

Diethylenetriaminepentaacetic acid neolactosyl human serum albumin (DTPA–LSA) was prepared and labeled with technetium-99m. The labeling conditions of 99mTc-DTPA–LSA were optimized, and lyophilized kit was developed for instant preparing of 99mTc-DTPA–LSA. 99mTc-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 99mTc-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.

► DPTA-LSA conjugate was prepared for 99mTc labeling and ASGP receptor targeting. ► A lyophilized DTPA–LSA kit was developed for instant preparation of 99mTc-compound. ► 99mTc-DTPA–LSA accumulated mainly in the liver (>96 % ID/g at 5 min p.i.). ► High quality SPECT images were obtained in normal Japanese White rabbits. ► A potential alternative agent for assessment of hepatocyte function in the future.