Senyei A E, Reich S D, Gonczy C, Widder K J
J Pharm Sci. 1981 Apr;70(4):389-91. doi: 10.1002/jps.2600700412.
The in vivo kinetics of low-dose doxorubicin (0.05 mg/kg), entrapped in a carrier and magnetically targeted, were characterized in a rat tail model. Tissue concentrations of doxorubicin at a preselected target site and in various organs were followed over time. As late as 60 min postinjection, 3.7 microgram/g of drug was found at the target site with no detectable drug levels found in any organ. In comparison, a 100-fold higher dose (5.0 mg/kg iv) of free doxorubicin yielded drug concentrations of 1.8 microgram/g at the target site and 15.0 microgram/kg in the pooled organs. Therefore, 1% of the free intravenous dose targeted magnetically yielded approximately twice the local doxorubicin concentration at a preselected target site with no detectable systemic distribution. Magnetic targeting of particulate drug carriers to localized disease sites is suggested as an efficient method of obtaining high local drug concentrations and may reduce many unwanted side effects from unrestricted systemic circulation.
在大鼠尾部模型中对包裹于载体并经磁靶向的低剂量阿霉素（0.05mg/kg）的体内动力学进行了表征。随着时间推移，监测了预选靶位点及各个器官中阿霉素的组织浓度。注射后60分钟时，靶位点发现有3.7微克/克的药物，而在任何器官中均未检测到药物水平。相比之下，游离阿霉素100倍高剂量（5.0mg/kg静脉注射）在靶位点产生的药物浓度为1.8微克/克，在合并器官中的浓度为15.0微克/千克。因此，经磁靶向的1%游离静脉剂量在预选靶位点产生的局部阿霉素浓度约为其两倍，且未检测到全身分布。将微粒药物载体磁靶向至局部疾病位点被认为是获得高局部药物浓度的有效方法，并且可能减少不受限制的全身循环带来的许多不良副作用。
