Polyiodinated Triglyceride Analogs as Potential Computed Tomography Imaging Agents for the Liver

Abstract

A series of glyceryl 2-oleoyl 1,3-bis[omega-(3-amino-2,4,6-triiodophenyl)] alkanoates was synthesized, radioiodinated with iodine-125, emulsified, and evaluated for their ability to selectively localize in the liver for potential use as hepatographic agents in computed tomography. All seven analogs displayed rapid liver uptake wherein between 65 and 78% of the injected dose accumulated in the liver by 30 min. Liver values ranged from 46 to 93% 3 h after injection which corresponded to liver to blood ratios ranging from 21 to 450. Moreover, subsequent elimination of radioactivity from the liver was nearly linear with respect to alkyl chain length. Analogs with longer alkyl chain length were eliminated from the liver more rapidly than their shorter chain counterparts. Because of their biochemical similarities to naturally occurring triglycerides, these novel analogs may prove useful not only for high-resolution anatomic imaging of focal liver lesions, but also for evaluating a variety of diffuse diseases known to affect hepatic function and biochemistry.

In‐vivo high‐resolution X‐ray microtomography for liver and spleen tumor assessment in mice

“…Such uptake, on the other hand, was found only in healthy spleen and liver parenchyma: in the present animal model, with a formula where oil particles were around 200 nm in size, uptake was probably mediated by the reticulo-endothelial system, which is present in both liver (Kupffer cells) and spleen (macrophages) (10,18,22).…”

“…Image acquisition was timed on the basis of previous studies defining the agent's pharmacokinetic and dose-response profiles (4,8,10,(18)(19)(20).…”

Structural imaging of the pancreas in rat using micro-CT: application to a non-invasive longitudinal evaluation of pancreatic ductal carcinoma monitoring

“…According to the manufacturer recommends, the ITG contrast enhancers for CT, trade-named Fenestra liver contrast (LC) and vascular contrast (VC) both from Advanced Research Technologies (Inc., Montreal, Canada), [9][10][11] should be injected together intravenously (vol/vol) at the dose of 1 ml/100 g of body weight for each of them, with a iodine concentration of 50 mg/ml. Such a fluid volume highly exceeds the maximal intravenous amount allowed by the European current best practice guideline, which is 0.5 ml/100 g body weight at the maximum corresponding to 10% of the rat volemia.…”

“…tool remains still relatively rare in small animal studies [5][6][7][8][9][10][11][12][13][14][15]. Furthermore until now, very few data concerning its use for pancreatic imaging in animal models have been reported in the literature [16].…”

In vivo small animal imaging: Current status and future prospects

“…Novel compounds mainly include lipid-emulsion formulations of conventional iodinated contrast media ͑under the commercial names Fenestra VC and Fenestra LC͒. [178][179][180] The Fenestra product line is based on iodinated triglycerides contained in the lipophilic cores of oil-in-water lipid emulsions similar to the naturally occurring chylomicron remnants. Use of such lipid-conjugated contrasts with iodine concentration greater than 100 mg I/ml is particularly useful in micro-CT imaging of small animals with extremely short contrast circulation lifetime.…”