Gupta P K, Hung C T
Department of Pharmacy, University of Otago, Dunedin, New Zealand.
J Microencapsul. 1990 Jan-Mar;7(1):85-94. doi: 10.3109/02652049009028426.
The efficacy of magnetic albumin microspheres in the targeted delivery of an anti-cancer agent, doxorubicin hydrochloride, has been investigated in rats. Using the tail as a target organ, the animals were intra-arterially administered with either 0.12 mg/kg of free drug, or 0.04 mg/kg of microsphere entrapped drug in the presence of a 8000 Gauss magnet applied for 30 min at the target-site. In each group, the animals were sacrificed over a 48 h period and their various tissues analysed for drug concentration using HPLC. It was found that compared to the free drug, a one-third dose of microsphere entrapped drug resulted in almost eight times higher drug exposure (AUC0-infinity) at the target site. In addition, the drug delivery to all the non-target tissues, including liver and heart, was substantially reduced. The study confirms the efficacy of magnetic albumin microspheres in the targeted delivery of chemotherapeutic agents.
已在大鼠中研究了磁性白蛋白微球在抗癌药物盐酸多柔比星靶向递送中的功效。以尾巴作为靶器官,给动物动脉内注射0.12mg/kg游离药物,或在靶部位施加8000高斯磁场30分钟的情况下,注射0.04mg/kg微球包封药物。在每组中,在48小时内处死动物,并使用高效液相色谱法分析其各种组织中的药物浓度。结果发现,与游离药物相比,三分之一剂量的微球包封药物在靶部位的药物暴露量(AUC0-无穷大)几乎高出八倍。此外,向包括肝脏和心脏在内的所有非靶组织的药物递送量大幅减少。该研究证实了磁性白蛋白微球在化疗药物靶向递送中的功效。