Borchardt G, Brandriss S, Kreuter J, Margel S
Institut für Pharmazeutische Technologie, J.W. Goethe-Universität Frankfurt, Germany.
J Drug Target. 1994;2(1):61-77. doi: 10.3109/10611869409015894.
Silica nanoparticles, radiolabeled with 75Selenium were coated with 14 types of omega-functionalized surfactants covalently bound to the particle surface. The particles were suspended in phosphate buffered saline (PBS) and injected intravenously via the tail vein of Wistar rats. The animals were sacrificed after 5 different time points (30 min, 2 h, 6 h, 24 h, and 7 d), and two samples of each organ and two blood samples were weighed into vials. The radioactivity of each sample was measured in a LKB-Wallac CliniGamma counter. Coated silica nanoparticles accumulated in the liver at much lower levels than other colloidal drug carriers after short time periods (30 min). The liver accumulation increased after longer time periods due to a natural redistribution process. Surface modification by increasing the hydrophilicity and thickness of coating yielded higher and longer persisting concentrations in the intestine, blood, and the muscles. Initially increased lung concentrations were decreasing with time, probably due to migration of the alveolar phagocytes.
用75硒进行放射性标记的二氧化硅纳米颗粒,表面共价结合了14种ω-官能化表面活性剂。将这些颗粒悬浮于磷酸盐缓冲盐水(PBS)中,经尾静脉注射到Wistar大鼠体内。在5个不同时间点(30分钟、2小时、6小时、24小时和7天)后处死动物,将每个器官的两个样本和两份血液样本称重后放入小瓶中。每个样本的放射性在LKB - Wallac CliniGamma计数器中进行测量。在短时间(30分钟)后,包覆的二氧化硅纳米颗粒在肝脏中的蓄积水平远低于其他胶体药物载体。由于自然再分布过程,较长时间后肝脏蓄积增加。通过增加包衣的亲水性和厚度进行表面修饰,在肠道、血液和肌肉中产生了更高且持续时间更长的浓度。最初肺部浓度升高,但随时间下降,这可能是由于肺泡吞噬细胞的迁移所致。