Zhang Xu, Wang Yamin, Zhao Yanbao, Sun Lei
Engineering Research Center for Nanomaterials, Henan University, Kaifeng 475004, China.
Henan Sports School, Zhengzhou 450045, China.
Mater Sci Eng C Mater Biol Appl. 2017 Aug 1;77:19-26. doi: 10.1016/j.msec.2017.03.224. Epub 2017 Mar 27.
In this work, pH-sensitive "dual-switch" porous silica (pSiO) nanoparticles (NPs) were constructed for drug delivery. Poly(acrylic acid) (PAA) was grafting onto the internal and external surfaces of amino groups functionalized porous silica (pSiO-NH) NPs by the amidation between the amino groups and the carboxyl groups of PAA for pH triggered drug release. The resultant pSiO/PAA NPs have an average diameter of 50-60nm and high specific surface area (914m·g). To improve the loading capacity, ZnO quantum dots (QDs) were used to block the partial pores of pSiO/PAA and the loading capacity reached to 28% for methotrexate (MTX) model drug. The in vitro cellular cytotoxicity test and a hemolysis assay demonstrated that the pSiO/PAA/ZnO NPs were highly biocompatible and suitable to utilize as drug carriers. The MTX-loaded pSiO/PAA/ZnO NPs displayed more efficient cytotoxic to HepG2 cells than free MTX. The pSiO/PAA/ZnO NPs displayed low premature, pH-responsive release and pH-dependent fluorescence. Moreover, pH-dependent fluorescence enables to trace MTX release behavior.
在本研究中，构建了用于药物递送的pH敏感“双开关”多孔二氧化硅（pSiO）纳米颗粒（NPs）。通过聚丙烯酸（PAA）的羧基与氨基官能化多孔二氧化硅（pSiO-NH）NPs内外表面的氨基之间的酰胺化反应，将PAA接枝到pSiO-NH NPs上，以实现pH触发的药物释放。所得的pSiO/PAA NPs平均直径为50-60nm，比表面积高（914m·g）。为了提高负载能力，使用氧化锌量子点（QDs）堵塞pSiO/PAA的部分孔隙，甲氨蝶呤（MTX）模型药物的负载能力达到28%。体外细胞毒性试验和溶血试验表明，pSiO/PAA/ZnO NPs具有高度的生物相容性，适合用作药物载体。负载MTX的pSiO/PAA/ZnO NPs对HepG2细胞显示出比游离MTX更有效的细胞毒性。pSiO/PAA/ZnO NPs表现出低的过早释放、pH响应释放和pH依赖性荧光。此外，pH依赖性荧光能够追踪MTX的释放行为。
