Hartig Sean M, Greene Rachel R, Carlesso Gianluca, Higginbotham James N, Khan Wasif N, Prokop Ales, Davidson Jeffrey M
Department of Chemical Engineering, Vanderbilt University, Nashville, TN 37235-1604, USA.
Biomaterials. 2007 Sep;28(26):3843-55. doi: 10.1016/j.biomaterials.2007.04.027. Epub 2007 May 3.
A non-toxic, nanoparticulate polyelectrolyte complex (PEC) drug delivery system was formulated to maintain suitable physicochemical properties at physiological pH. Toxicity, binding, and internalization were evaluated in relevant microvascular endothelial cells. PEC were non-toxic, as indicated by cell proliferation studies and propidium iodide staining. Inhibitor studies revealed that PEC were bound, in part, via heparan sulfate proteoglycans and internalized through macropinocytosis. A novel, flow cytometric, Scatchard protocol was established and showed that PEC, in the absence of surface modification, bind cells non-specifically with positive cooperativity, as seen by graphical transformations.
制备了一种无毒的纳米颗粒聚电解质复合物(PEC)药物递送系统,以在生理pH值下保持合适的物理化学性质。在相关微血管内皮细胞中评估了其毒性、结合和内化情况。细胞增殖研究和碘化丙啶染色表明,PEC无毒。抑制剂研究表明,PEC部分通过硫酸乙酰肝素蛋白聚糖结合,并通过巨胞饮作用内化。建立了一种新颖的流式细胞术Scatchard方案,结果显示,在没有表面修饰的情况下,PEC以正协同性非特异性结合细胞,这从图形转换中可以看出。