摘要
目的研究甘草次酸衍生物(甘草次酸硬脂醇酯-3-O-半乳糖苷,Gal-GAOSt)修饰去甲斑蝥素脂质体(Gal-GAOStNC-LP)在小鼠体内的分布及肝靶向性。方法利用薄膜分散法制备甘草次酸衍生物修饰去甲斑蝥素脂质体后,经小鼠尾静脉给药,采用HPLC法检测去甲斑蝥素在小鼠肝肾中的浓度随时间的变化,与去甲斑蝥素水溶液组进行比较,并以靶向指数TI=(AUC)NC-SOL/(AUC)Gal-GAOStNC-LP来判断Gal-GAOStNC-LP对主要器官的靶向性。结果Gal-GAOStNC-LP组在肝脏中组织浓度明显高于NC-SOL组,肝的靶向指数大于1,而肾的靶向指数小于1。结论甘草次酸衍生物修饰去甲斑蝥素脂质体具有肝靶向性,能提高药物疗效,降低毒副作用。
Objective To study the distribution and liver targeting of glycyrrhetinic acid derivatives （ stearin glycyrrhetinic acid ester - 3 - O - galactosidase, Gal - GAOSt） modifying norcantharidin liposomes （ Gal - GAOStNC - LP） in rats. Methods Making use of film decentralization to prepare glycyrrhetinic acid derivatives modifying norcantharidin liposomes, and then injecting it to the tail vein of rats. Making use of HPLC to detect the Change of norcantharidin concentration in the rats＇ liver and kidney over time and com- pared it with norcantharidin solution group and targeting index TI = （AUC） NC - SOL / （AUC） Gal - GAOStNC - LP to determine the targeting of Gal - GAOStNC - LP to the main organs. Results Organization concentration of Gal - GAOStNC - LP group in the liver was significantly higher than NC - SOL group, the liver targeting index was greater than 1, and the targeting index of the kidney was less than 1. Conclusions Glycyrrhetinic acid derivatives modifying norcantharidin liposomes possess liver targeting that can improve the efficacy of drugs, reduce toxicity and side effect.
出处
《辽宁医学院学报》
CAS
2008年第6期490-491,495,I0001,共4页
Journal of Liaoning Medical University (LNMU) Bimonthly
