Umbrain V, Alafandy M, Bourgeois P, D'Haese J, Boogaerts J G, Goffinet G, Camu F, Legros F J
Department of Anaesthesiology, Flemish Free University of Brussels Clinical Centre, Belgium.
Br J Anaesth. 1995 Sep;75(3):311-8. doi: 10.1093/bja/75.3.311.
We have mapped over 24 h the biodistribution of 99mTc-labelled multilamellar and small unilamellar liposomes in rabbits and rats by scintigraphic imaging after extradural injection. Multilamellar vesicles formed a depot at the site of injection; small unilamellar vesicles spread immediately along the extradural space and entered the systemic compartment 30 min after injection. Well-delineated liver and kidney labellings were seen after 24 h. The use of 3H-cholesterol-labelled small unilamellar vesicles suggested hepatic capture of intact liposomes with sizes averaging 0.05 microns drained unmodified into the systemic circulation through the extradural lymphatics. These results have led to the selection of multilamellar vesicles (0.1-15 microns size range) for clinical trials using liposome-associated local anaesthetics.
我们通过硬膜外注射后的闪烁成像，在兔和大鼠体内对99mTc标记的多层脂质体和小单层脂质体的生物分布进行了超过24小时的测绘。多层囊泡在注射部位形成一个贮库；小单层囊泡在注射后立即沿硬膜外腔扩散，并在30分钟后进入体循环。24小时后可见清晰的肝脏和肾脏标记。使用3H-胆固醇标记的小单层囊泡表明，平均大小为0.05微米的完整脂质体被肝脏捕获，并通过硬膜外淋巴管未经修饰地排入体循环。这些结果促使我们选择多层囊泡（大小范围为0.1-15微米）用于脂质体相关局部麻醉剂的临床试验。
