Li Yan, Song Fangxiang, Cheng Liang, Qian Jin, Chen Qianlin
Institute of Advanced Technology, Guizhou University, Guiyang 550025, China.
School of Chemistry and Chemical Engineering, Guizhou University, Guiyang 550025, China.
Materials (Basel). 2019 Mar 6;12(5):766. doi: 10.3390/ma12050766.
Large-pore coralline mesoporous silica microparticles (CMS) were synthesized using the triblock polymer PEG--PEO--PEG and a hydrothermal method. Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) revealed the coralline morphology of the fabricated materials. The Brunauer⁻Emmett⁻Teller (BET) method and the Barrett⁻Joyner⁻Halenda (BJH) model confirmed the existence of large pores (20 nm) and of a tremendous specific surface area (663.865 m²·g) and pore volume (0.365 cm³·g). A novel pH-sensitive multiamine-chain carboxyl-functionalized coralline mesoporous silica material (CMS⁻(NH)₃⁻COOH) was obtained via a facile "grafting-to" approach. X-ray photoelectron spectroscopy (XPS) and Fourier-transform infrared spectroscopy (FT-IR) validated the effective interfacial functionalization of CMS with carboxyl and multiamine chains. The encapsulation and release behavior of the dual drug (gefitinib (GB) and doxorubicin (DOX)) was also investigated. It was found that CMS⁻(NH)₃⁻COOH allows rapid encapsulation with a high loading capacity of 47.36% for GB and 26.74% for DOX. Furthermore, the release profiles reveal that CMS⁻(NH)₃⁻COOH can preferably control the release of DOX and GB. The accumulative release rates of DOX and GB were 32.03% and 13.66%, respectively, at a low pH (pH 5.0), while they reduced to 8.45% and 4.83% at pH 7.4. Moreover, all of the modified silica nanoparticles exhibited a high biocompatibility with a low cytotoxicity. In particular, the cytotoxicity of both of these two drugs was remarkably reduced after being encapsulated. CMS⁻(NH)₃⁻COOH@GB@DOX showed tremendously synergistic effects of the dual drug in the antiproliferation and apoptosis of A549 human cancer cells in vitro.
采用三嵌段聚合物聚乙二醇-聚环氧乙烷-聚乙二醇（PEG-PEO-PEG）和水热法合成了大孔珊瑚状介孔二氧化硅微粒（CMS）。扫描电子显微镜（SEM）和透射电子显微镜（TEM）揭示了所制备材料的珊瑚状形态。布鲁诺尔-埃米特-泰勒（BET）法和巴雷特-乔伊纳-哈伦达（BJH）模型证实了大孔（20 nm）的存在以及巨大的比表面积（663.865 m²·g）和孔体积（0.365 cm³·g）。通过简便的“接枝到”方法获得了一种新型的pH敏感型多胺链羧基功能化珊瑚状介孔二氧化硅材料（CMS-(NH)₃-COOH）。X射线光电子能谱（XPS）和傅里叶变换红外光谱（FT-IR）验证了CMS与羧基和多胺链的有效界面功能化。还研究了双药（吉非替尼（GB）和阿霉素（DOX））的包封和释放行为。发现CMS-(NH)₃-COOH能够快速包封，对GB的高负载量为47.36%，对DOX的高负载量为26.74%。此外，释放曲线表明CMS-(NH)₃-COOH能够较好地控制DOX和GB的释放。在低pH（pH 5.0）下，DOX和GB的累积释放率分别为32.03%和13.66%，而在pH 7.4时分别降至8.45%和4.83%。此外，所有改性二氧化硅纳米颗粒均表现出高生物相容性和低细胞毒性。特别是，这两种药物在包封后细胞毒性均显著降低。CMS-(NH)₃-COOH@GB@DOX在体外对A549人癌细胞的增殖抑制和凋亡方面显示出双药的巨大协同效应。
