Dunn S E, Brindley A, Davis S S, Davies M C, Illum L
Department of Pharmaceutical Sciences, University of Nottingham, University Park, U.K.
Pharm Res. 1994 Jul;11(7):1016-22. doi: 10.1023/a:1018939521589.
The effect of differing densities of poly (ethylene glycol-2000) (PEG2000) at the particle surface of polystyrene-poly (ethylene glycol-2000) (PS-PEG2000) particles was assessed in terms of hydrophobic interaction chromatography (HIC) and the in vitro and in vivo behaviour of the particles. The particles, with different surface densities of PEG, were prepared by varying the copolymerizing reaction of styrene with a PEG macromonomer. There is a clear relationship between the surface density of PEG as determined by X-ray photoelectron spectroscopy and surface hydrophobicity as assessed by hydrophobic interaction chromatography (HIC). Similarly, the interaction of the particles with non-parenchymal liver cells in in vitro studies was shown to decrease as the surface density of PEG increases. The in vivo study investigating the biodistribution of the PS-PEG particles after intravenous injection into rats reveals that a relationship exists between the surface density of PEG and the extent to which the particles remain in the circulation, avoiding recognition by the reticuloendothelial system. Particles with the higher surface densities show increased circulatory times which compared well with data for particles prepared with the surface adsorbed PEO-PPO block copolymer, Poloxamine 908.
在疏水相互作用色谱法(HIC)以及聚苯乙烯 - 聚(乙二醇 - 2000)(PS - PEG2000)颗粒的体外和体内行为方面,评估了聚苯乙烯 - 聚(乙二醇 - 2000)(PS - PEG2000)颗粒表面不同密度的聚(乙二醇 - 2000)(PEG2000)的影响。通过改变苯乙烯与PEG大分子单体的共聚反应,制备了具有不同PEG表面密度的颗粒。通过X射线光电子能谱测定的PEG表面密度与通过疏水相互作用色谱法(HIC)评估的表面疏水性之间存在明显的关系。同样,在体外研究中,随着PEG表面密度的增加,颗粒与非实质肝细胞的相互作用显示出减少。在对大鼠静脉注射后PS - PEG颗粒的生物分布进行的体内研究表明,PEG的表面密度与颗粒在循环中保留的程度之间存在关系,从而避免被网状内皮系统识别。具有较高表面密度的颗粒显示出循环时间增加,这与用表面吸附的PEO - PPO嵌段共聚物泊洛沙明908制备的颗粒的数据相比良好。