Seltzer S E, Davis M A, Adams D F, Shulkin P M, Landis W J, Havron A
Invest Radiol. 1984 Mar-Apr;19(2):142-51. doi: 10.1097/00004424-198403000-00012.
We have prepared and characterized a suspension of liposomes carrying diatrizoate. Vesicles were made with egg lecithin, cholesterol, and stearylamine in a 4:1:1 molar ratio, and contained meglumine sodium diatrizoate in their aqueous phase. They ranged up to 2.0 microns in size and had a multilamellar structure. These vesicles were then injected into normal and tumor-bearing rats, as well as normal dogs and a baboon. The iodine component proved to have a prolonged blood pool residence time, was cleared through reticuloendothelial and urinary tissues, and was completely excreted within seven days. The LD50 in mice was 2.3 g I/kg (38.5 g of liposome suspension/kg). Imaging studies with diatrizoate-carrying liposomes demonstrated marked and prolonged contrast enhancement of blood pool, liver, spleen, kidneys, urine, and tumor rims. Furthermore, the blood, liver, and spleen opacification was greater and longer sustained than when an equivalent amount of iodine in free diatrizoate was used. These diatrizoate-carrying liposomes are particularly well suited for computed tomographic imaging of blood pool and reticuloendothelial structures.
我们制备并表征了携带泛影酸盐的脂质体悬浮液。脂质体由卵磷脂、胆固醇和硬脂胺按4:1:1的摩尔比制成,水相中含有葡甲胺泛影酸钠。其大小可达2.0微米,具有多层结构。然后将这些脂质体注射到正常大鼠、荷瘤大鼠、正常犬和一只狒狒体内。结果表明,碘成分在血池中的滞留时间延长,通过网状内皮组织和泌尿组织清除,并在7天内完全排出。小鼠的半数致死量为2.3 g I/kg(38.5 g脂质体悬浮液/kg)。用携带泛影酸盐的脂质体进行的成像研究表明,血池、肝脏、脾脏、肾脏、尿液和肿瘤边缘有明显且持久的对比增强。此外,与使用等量游离泛影酸盐中的碘相比,血液、肝脏和脾脏的显影更明显且持续时间更长。这些携带泛影酸盐的脂质体特别适合用于血池和网状内皮结构的计算机断层扫描成像。