定量评价去氢骆驼蓬碱注射用乳剂的组织靶向性

QUANTITATIVE EVALUATION OF HARMINE INTRAVENOUS EMULSION AS TARGETED DRUG DELIVERY SYSTEM

目的:定量评价静脉注射用乳剂作为药物载体给药后对主要脏器的靶向性并对给药系统靶向性的定量评价参数进行讨论和评价。方法:用3H标记的去氢骆驼蓬碱(harmine,HAR)分别制成静脉注射乳剂、水溶液和脂质体,经小鼠静脉注射后测定主要脏器组织中的总放射性强度,计算重量-平均总靶向性系数Te和靶向性系数Te,并对乳剂的靶向性意义作出定量评价。结果:静脉乳剂可显著提高放射性在肝、脾、淋巴器官的分布,降低放射性向脑组织的转运。结论:静脉注射乳剂是一很有意义的靶向给药系统,重量-平均总靶向性系数Te是较全面的靶向性评价参数。

AIM: The experiment was carried out in mice to study the tissue distribution characteristics of harmine (HAR) intravenous emulsion and quantitatively evaluate it as targeting drug delivery system. METHODS: Harmine was labelled with 3H as a tracer isotope. The distribution of 3H to the various organs and blood of mice, following its iv administration(1 85×10 7 Bq·kg -1 ) as an emulsion, a solution and liposome, was determined by liquid scintillation counting technique. The total radioactivity time curves in important tissues were obtained. The weighted average overall drug targeting efficiency ( T e *) was calculated as well. RESULTS: The intravenous emulsion, as a drug delivery system, may enhance the 3H quantity in liver, spleen and lymph system. The results also demonstrate that it can prevent the 3H from transporting to brain. The emulsion plays an important role of effectively reducing the side effects of harmine in nervous system. CONCLUSION: The weight average overall drug targeting efficiency( T e *) is a more reasonable evaluation parameter. The emulsion is an obviously targeted drug delivery system.