111In–L–LDL and 153Gd–L–LDL as radiotracers for detection of AR4‐2J rat pancreatic tumors

Abstract

AbstractPancreatic cancer has an extremely poor prognosis, due, in part, to lack of methods for early diagnosis. The present study was designed to evaluate the potential of labeling low‐density lipoprotein (LDL) with a radionuclide using a lipid chelating agent, bis(stearylamide) of diethylenetriaminepentaacetic acid (L), to detect pancreatic tumors by gamma‐scintigraphy. Previous studies indicated that the difficulty of visualization of pancreatic tumors was due to their poor vascularization. This study compares the ability of two radiotracers, 111In–L–LDL and 153Gd–L–LDL to target highly vascularized rat pancreatic tumors (AR4‐2J) implanted in nude mice. Biodistribution studies showed that the tumor uptake of 111In–L–LDL and 153Gd–L–LDL tracers was twofold and fivefold higher respectively than with the controls (111In citrate and 153Gd citrate respectively). These tracers would thus be suitable for scintigraphic imaging.We show here that LDL could be employed as a delivery system for tracers such as 111In or 153Gd when these two radionuclides are complexed by a lipid‐chelating anchor, and that 111In–L–LDL and 153Gd–L–LDL enabled better visualization of the pancreatic tumor tissues, with a better result with 153Gd–L–LDL. Copyright © 2004 John Wiley & Sons, Ltd.