Department of Pharmaceutics, School of Pharmacy, Shandong University, 44 Wenhuaxi Road, Jinan, Shandong Province 250012, China.
Colloids Surf B Biointerfaces. 2011 Apr 1;83(2):237-44. doi: 10.1016/j.colsurfb.2010.11.027. Epub 2010 Nov 28.
Two types of novel nanogels were prepared using shell cross-linking of Pluronic F127 micelles with polyethylenimine (PEI) (F127/PEI nanogel), and penetrating network of poly(butylcyanoacrylate) (PBCA) in Pluronic F127 micelles (F127/PBCA nanogel). Poorly soluble anticancer drug, paclitaxel (PTX) and 10-hydroxycamptothecin (HCPT), were used as model drugs and incorporated into nanogels. The results obtained from FT-IR spectroscopy confirmed that the drugs were molecularly dispersed in the nanogels. DLS measurements demonstrated that the nanogel size distribution was narrow with average diameter less than 200 nm. TEM images indicated that the nanogels were spherical in shape and had smooth surfaces. The drug-loaded nanogels showed sustained release profiles compared with the free drugs as revealed by in vitro release experiments. Cytotoxicity tests showed that the cytotoxicity of drug-loaded nanogels against cancer cell in vitro was much higher than that of the free drug. The data demonstrate that these novel nanogels improved stability towards dilution, increased solubility and showed better cellular uptake by cells compared with free drug.
两种新型纳米凝胶通过聚氧乙烯-聚氧丙烯嵌段共聚物 F127 胶束与聚乙烯亚胺（PEI）的壳交联（F127/PEI 纳米凝胶），以及聚丁基氰基丙烯酸酯（PBCA）在 F127 胶束中的穿透网络（F127/PBCA 纳米凝胶）来制备。将疏水性抗癌药物紫杉醇（PTX）和 10-羟基喜树碱（HCPT）用作模型药物并包封于纳米凝胶中。傅里叶变换红外光谱（FT-IR）的结果证实药物以分子形式分散在纳米凝胶中。动态光散射（DLS）测量表明纳米凝胶的粒径分布较窄，平均直径小于 200nm。透射电子显微镜（TEM）图像表明纳米凝胶呈球形且表面光滑。与游离药物相比，载药纳米凝胶在体外释放实验中表现出持续释放的特征。细胞毒性试验表明，载药纳米凝胶对体外癌细胞的细胞毒性明显高于游离药物。这些数据表明，与游离药物相比，这些新型纳米凝胶提高了稀释稳定性、增加了溶解度并表现出更好的细胞摄取。
