Peracchia M T, Vauthier C, Passirani C, Couvreur P, Labarre D
Université Paris-Sud XI-URA CNRS 1218, Physico-chimie, Pharmacotechnie, Biopharmacie, Châtenay-Malabry, France.
Life Sci. 1997;61(7):749-61. doi: 10.1016/s0024-3205(97)00539-0.
There is an increasing interest to develop injectable drug polymeric carriers not recognizable by the body as foreign particles and eliminated very quickly from the bloodstream. A polyethylene glycol (PEG)-coating onto injectable particles showed to reduce either protein adsorption and complement consumption, as a function of the PEG density. In this work we compared the complement rejecting ability of PEG in different conformations coupled to polyisobutylcyanoacrylate (PIBCA) nanoparticles, through the analysis of the residual hemolytic capacity of the human serum after contact with the particles. Nanoparticles were formed by chemical coupling of PEG during emulsion/polymerization of isobutylcyanoacrylate (IBCA). Nanoparticles characterization included an investigation of their surface properties, such as hydrophilicity and conformational mobility of the PEG chains grafted on the nanoparticles surface, and PEG total content. The polymerization kinetics of IBCA in presence of PEG or MePEG were also studied. Complement consumption was observed to be very sensitive to the number of particles in contact with human serum, as well as to the PEG conformation, suggesting PEG configuration could affect the particle exposed surface.
开发可注射药物聚合物载体的兴趣日益浓厚,这种载体不会被身体识别为外来颗粒,并能很快从血液中清除。在可注射颗粒上涂覆聚乙二醇(PEG)可减少蛋白质吸附和补体消耗,这取决于PEG的密度。在这项工作中,我们通过分析人血清与颗粒接触后的残余溶血能力,比较了不同构象的PEG与聚异丁基氰基丙烯酸酯(PIBCA)纳米颗粒偶联时的补体排斥能力。纳米颗粒是在异丁基氰基丙烯酸酯(IBCA)乳液/聚合过程中通过PEG的化学偶联形成的。纳米颗粒表征包括对其表面性质的研究,如接枝在纳米颗粒表面的PEG链的亲水性和构象流动性,以及PEG总含量。还研究了在PEG或甲氧基聚乙二醇(MePEG)存在下IBCA的聚合动力学。观察到补体消耗对与人血清接触的颗粒数量以及PEG构象非常敏感,这表明PEG构型可能会影响颗粒的暴露表面。