肝细胞靶载体分子体内分布和代谢动力学

目的：为证明本研究制备的靶细胞特异性受体的配体分子无唾液酸糖蛋白（ASOR）是否能成为肝细胞靶向带药载体。方法：用同位素^125I标记ASOR分子，注入Strague-Dawley(SD)大鼠后从整体器官及细胞水平检测大鼠内ASOR的分布。结果ASOR仅分布在肝脏且与肝细胞结合，不与体内其他重要脏器如心、脑、肺、脾、肾、骨及生殖腺等组织细胞结合。代谢动力学为：注药10min后90％ASOR分子位于肝内，表明其有很高的亲肝性，代谢动力学方程为Ct＝662216e^-3.362t 8896e^-0.2343t，前半减期T1／2α=0.206h，后半减期T1／2β=5.575h。ASOR在肝内分解后的肽与胃组织细胞有亲和力。结论：ASOR具备肝细胞靶向带药载体的条件，具有研究价值。

Distribution and metabodynamics of hepatocyte targeting vector molecules in vivo]

OBJECTIVE: To testify whether asiaorosomucoid (ASOR), the ligamental molecule of specific hepatocyte receptor prepared in our laboratory, can be used as a delivery drug vector for targeting hepatocyte. METHODS: ASOR molecules marked with isotope 125I were injected into Strague-Dawley rats, and the distribution of ASOR on both organ and cellular levels was detected. RESULTS: ASOR could only combine with hepatocyte and distribute in the liver. It did not combine with other important organ cells, such as the heart, brain, lung, spleen, kidney, bone and germen. The metabodynamics included: 10 mins after the injection, 90% ASOR was located in the liver, indicating that ASOR had a high hepatotropic; the metabodynamic equation was Ct = 66221e-3.362t + 8869e-0.2343t; the former half-life (T1/2 alpha was 0.206 h, and the latter half-life (T1/2 beta) was 5.575 h. The catabolite peptide of ASOR in the liver had affinity with the stomach. CONCLUSION: ASOR could have the qualification of being a drug targeting vector for the liver and is worth further research.