Lenaerts V, Nagelkerke J F, Van Berkel T J, Couvreur P, Grislain L, Roland M, Speiser P
J Pharm Sci. 1984 Jul;73(7):980-2. doi: 10.1002/jps.2600730730.
Polyalkyl cyanoacrylate nanoparticles were previously developed as a biodegradable, ultrafine, solid drug carrier. Distribution studies in the rat showed an intense and rapid hepatic uptake. This liver accumulation appears to represent, to a certain extent, extracellularly bound nanoparticles. During liver perfusion, 15-20% of the liver-associated nanoparticles were washed out. The cellular distribution of strongly cell-associated nanoparticles was determined. At different intervals after injection of radioactive nanoparticles to rats, the cells were isolated according to a recently developed, low-temperature procedure during which processing of the carrier was inhibited. At all tested times, a relatively intense capture by Kupffer cells in comparison with endothelial and especially parenchymal cells was observed. This distribution pattern was not influenced by the size of the nanoparticles (0.08-0.215-micron diameter). This specific interaction of nanoparticles with Kupffer cells opens possibilities for the treatment of some parasitic diseases involving this cell type.
聚烷基氰基丙烯酸酯纳米颗粒先前被开发为一种可生物降解的超细固体药物载体。在大鼠体内的分布研究表明,肝脏对其摄取强烈且迅速。这种肝脏蓄积在一定程度上似乎代表细胞外结合的纳米颗粒。在肝脏灌注过程中,15%至20%与肝脏相关的纳米颗粒被洗脱。测定了与细胞紧密结合的纳米颗粒的细胞分布。在给大鼠注射放射性纳米颗粒后的不同时间间隔,根据最近开发的低温程序分离细胞,在此过程中载体的处理受到抑制。在所有测试时间,与内皮细胞尤其是实质细胞相比,观察到库普弗细胞有相对强烈的摄取。这种分布模式不受纳米颗粒大小(直径0.08 - 0.215微米)的影响。纳米颗粒与库普弗细胞的这种特异性相互作用为治疗一些涉及这种细胞类型的寄生虫病开辟了可能性。