The effect of vehicle on the tissue distribution profiles of radioiodinated cholesterol esters in the rat

Several groups have examined the possible use of radioiodinated cholesterol esters to achieve selective uptake of radioactivity in the adrenal cortex and have obtained variable results. This study indicates that the tissue distribution profile varies not only with the type of ester, but also with the vehicle employed for administration. Radioiodinated 19-iodocholesteryl (125-IC), iodocholesteryl palmitate (125-ICP)and iodocholesteryl oleate (125-ICO) were dissolved in either tween vehicle (saline containing 1.6% tween 80 and 10% ethanol) or myristate vehicle (isopropyl myristate-ethanol, 1:5 v/v) and administered i.v. to rats. Irrespective of the agent, considerably more radioactivity appeared in the target organs when the tween vehicle was employed. When the myristate vehicle was used, higher levels of radioactivity appeared in the lung. This finding suggests precipitation of the agents from the myristate vehicle occurred upon administration. In the tween vehicle, 125-ICO showed almost three times greater predilection for adrenal cortex than 125-ICP with levels of activity approaching those seen for 125-IC. Adrenal activity and adrenal to non-target ratios were sufficient for visualization of the adrenals at 5 days after injection of 125-ICO in the tween vehicle. Lipid extraction and TLC analysis of tissue radioactivity revealed that radioactivity in the adrenal and ovary was predominantly in an esterified form. Further analysis of the esters present after injection of 125-ICP showed these to be a mixture of mono and polyunsaturated esters. The site of hydrolysis and subsequent reesterification is an interesting biochemical aspect that remains to be elucidated.Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/24488/1/0000764.pd