Kao Y J, Loo T L
J Pharm Sci. 1980 Nov;69(11):1338-40. doi: 10.1002/jps.2600691126.
The pharmacological disposition of four negatively charged phospholipid vesicles with radioactive cholesteryl oleate as a tracer was investigated in rats. The acidic phospholipids included phosphatidylserine, phosphatidylglycerol, phosphatidylinositol, and diphosphatidylglycerol (cardiolipin). The blood half-life of phosphatidylserine vesicles was the shortest (< 2 min), while that of phosphatidylinositol was the longest (90 min). Cardiolipin and phosphatidylglycerol vesicles had intermediate blood half-lives (7 and 18 min, respectively). The distribution of these vesicles in six major organs (liver, spleen, heart, kidneys, lungs, and brain) varied greatly. Contrary to the long-held belief, it was possible to prepare negatively charged phospholipid vesicles with long blood half-lives. Furthermore, tissue disposition of these negatively charged vesicles could be manipulated partially by judicious selection of their components.
以放射性胆固醇油酸酯作为示踪剂，对四种带负电荷的磷脂囊泡在大鼠体内的药物处置情况进行了研究。酸性磷脂包括磷脂酰丝氨酸、磷脂酰甘油、磷脂酰肌醇和二磷脂酰甘油（心磷脂）。磷脂酰丝氨酸囊泡的血液半衰期最短（<2分钟），而磷脂酰肌醇的半衰期最长（90分钟）。心磷脂和磷脂酰甘油囊泡的血液半衰期处于中间水平（分别为7分钟和18分钟）。这些囊泡在六个主要器官（肝脏、脾脏、心脏、肾脏、肺和脑）中的分布差异很大。与长期以来的观点相反，有可能制备出血液半衰期长的带负电荷的磷脂囊泡。此外，通过明智地选择其成分，可以部分地控制这些带负电荷囊泡的组织处置情况。
