Centro de Ciências Biológicas, Universidade Federal de Pernambuco, Recife, Brazil.
Eur J Pharm Biopharm. 2011 Sep;79(1):162-70. doi: 10.1016/j.ejpb.2011.02.013. Epub 2011 Feb 22.
The aim was to synthesize and characterize fucoidan-coated poly(isobutylcyanoacrylate) nanoparticles. The nanoparticles were prepared by anionic emulsion polymerization (AEP) and by redox radical emulsion polymerization (RREP) of isobutylcyanoacrylate using fucoidan as a new coating material. The nanoparticles were characterized, and their cytotoxicity was evaluated in vitro on J774 macrophage and NIH-3T3 fibroblast cell lines. Cellular uptake of labeled nanoparticles was investigated by confocal fluorescence microscopy. Results showed that both methods were suitable to prepare stable formulations of fucoidan-coated PIBCA nanoparticles. Stable dispersions of nanoparticles were obtained by AEP with up to 100% fucoidan as coating material. By the RREP method, stable suspensions of nanoparticles were obtained with only up to 25% fucoidan in a blend of polysaccharide composed of dextran and fucoidan. The zeta potential of fucoidan-coated nanoparticles was decreased depending on the percentage of fucoidan. It reached the value of -44 mV for nanoparticles prepared by AEP with 100% of fucoidan. Nanoparticles made by AEP appeared more than four times more cytotoxic (IC(50) below 2 μg/mL) on macrophages J774 than nanoparticles made by RREP (IC(50) above 9 μg/mL). In contrast, no significant difference in cytotoxicity was highlighted by incubation of the nanoparticles with a fibroblast cell line. On fibroblasts, both types of nanoparticles showed similar cytotoxicity. Confocal fluorescence microscopy observations revealed that all types of nanoparticles were taken up by both cell lines. The distribution of the fluorescence in the cells varied greatly with the type of nanoparticles.
目的是合成和表征褐藻糖胶包覆的聚异丁基氰基丙烯酸酯纳米粒子。纳米粒子通过阴离子乳液聚合（AEP）和氧化还原自由基乳液聚合（RREP）制备，使用褐藻糖胶作为新的包覆材料。对纳米粒子进行了表征，并在体外对 J774 巨噬细胞和 NIH-3T3 成纤维细胞系评估了其细胞毒性。通过共焦荧光显微镜研究了标记的纳米粒子的细胞摄取。结果表明，这两种方法都适合制备稳定的褐藻糖胶包覆的 PIBCA 纳米粒子制剂。通过 AEP 可以获得高达 100％褐藻糖胶作为包覆材料的稳定分散体。通过 RREP 方法，仅在由葡聚糖和褐藻糖胶组成的多糖混合物中加入 25％的褐藻糖胶，就可以获得稳定的纳米粒子悬浮液。褐藻糖胶包覆纳米粒子的zeta 电位取决于褐藻糖胶的百分比。当用 AEP 制备 100％褐藻糖胶时，zeta 电位达到-44 mV。通过 AEP 制备的纳米粒子在巨噬细胞 J774 上的细胞毒性（IC（50）低于 2 μg/mL）比通过 RREP 制备的纳米粒子高四倍以上（IC（50）高于 9 μg/mL）。相反，在用成纤维细胞系孵育纳米粒子时，未突出显示出细胞毒性的显著差异。在成纤维细胞上，两种类型的纳米粒子均表现出相似的细胞毒性。共焦荧光显微镜观察表明，两种类型的纳米粒子都被两种细胞系摄取。细胞内荧光的分布随纳米粒子的类型而有很大差异。
