Indium-111-labeled liposomes: quality and biodistribution in mice bearing human tumor xenografts

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Abstract
Phospholipid vesicles containing the ionophore A23187 in the bilayer (VesCan) are the only liposomes produced for clinical imaging purposes. We undertook preliminary experiments with In-loaded VesCan (indium-111-V-liposome) using normal rabbits and nude mice bearing human gastric (MKN45) and colon (COL0205) tumor xenografts before clinical application of the product. Two V-liposome vials with different expiration dates were labeled with 111In and then injected into rabbits immediately or 24 h after loading. The blood clearances of 111In were not significantly different from rabbit to rabbit, indicating that 111In-V-liposomes did not vary among vial lots. Both MKN45 and COL0205 tumor xenografts in nude mice were successfully imaged with 111In-V-liposome; V-liposome delivered sufficient radioactivity to allow tumor visualization as early as 8 h after iv injection. It was also found that MKN45 tumors exhibited uptake of 6.5% ID/g. The present results indicated that the quality and shelf life of 111In-V-liposomes are good and that scintigraphy of 111In-V-liposomes is a feasible technique for detecting tumor lesion in patients with cancer.