Perez-Soler R, Lopez-Berestein G, Jahns M, Wright K, Kasi L P
Int J Nucl Med Biol. 1985;12(4):261-6. doi: 10.1016/0047-0740(85)90177-9.
The distribution of negatively charged multilamellar vesicles (MLV) composed of dimyristoyl phosphatidylcholine and dimyristoyl phosphatidylglycerol administered subcutaneously (s.c.) and intralymphatically (i.l.) was studied in rats and dogs. In rats, the drainage of 99mTc-MLV from the s.c. space was slow, with 35% of the activity still remaining at the site of injection after 48 h and minimal systemic distribution (less than 5% at any time point). In the dog, 99mTc-MLV and 111In-MLV injected s.c. on the dorsal surface of a hindpaw were drained both by the lymphatic system and the systemic circulation; at 24 and 72 h, significant activity still remained at the site of injection. Lymphatic uptake was almost limited to the popliteal nodes and was enhanced by dividing the dose in several s.c. injections. Liver and kidney uptake was also observed, most likely as a result of direct liposome absorption into the systemic circulation. The i.l. administration (via left hindpaw) of 99mTc-MLV to a dog resulted in an immediate uptake in the abdominal and mediastinal lymph nodes, and in the liver and spleen. Compared with small unilamellar vesicles, MLV injected s.c. can provide a slower and more prolonged delivery of drugs to the regional lymph nodes.
在大鼠和犬体内研究了由二肉豆蔻酰磷脂酰胆碱和二肉豆蔻酰磷脂酰甘油组成的带负电荷多层囊泡（MLV）皮下（s.c.）和淋巴管内（i.l.）给药后的分布情况。在大鼠中，99mTc - MLV从皮下间隙的引流缓慢，48小时后仍有35%的活性保留在注射部位，全身分布极少（在任何时间点均小于5%）。在犬中，注射在后爪背侧皮下的99mTc - MLV和111In - MLV通过淋巴系统和体循环引流；在24小时和72小时时，注射部位仍有显著活性。淋巴摄取几乎仅限于腘淋巴结，通过分几次皮下注射给药可增强摄取。还观察到肝脏和肾脏摄取，这很可能是脂质体直接吸收进入体循环的结果。给犬经淋巴管内（通过左后爪）注射99mTc - MLV会导致腹部和纵隔淋巴结以及肝脏和脾脏立即摄取。与小单层囊泡相比，皮下注射MLV可向局部淋巴结提供更缓慢、更持久的药物递送。
