Scientific Reports ( IF 3.8 ) Pub Date : 2022-11-30 , DOI: 10.1038/s41598-022-25095-4
Ozi Adi Saputra, Windy Ayu Lestari, Viardi Kurniansyah, Witri Wahyu Lestari, Takashi Sugiura, Rino R. Mukti, Ronny Martien, Fajar Rakhman Wibowo
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Controlling the premature release of hydrophobic drugs like quercetin over physiological conditions remains a challenge motivating the development of smart and responsive drug carriers in recent years. This present work reported a surface modification of mesoporous silica nanoparticles (MSN) by a functional compound having both amines (as a positively charged group) and carboxylic (negatively charged group), namely 4-((2-aminoethyl)amino)-4-oxobut-2-enoic acid (AmEA) prepared via simple mechanochemistry approach. The impact of MSN surface modification on physical, textural, and morphological features was evaluated by TGA, N2 adsorption–desorption, PSA-zeta, SEM, and TEM. The BET surface area of AmEA-modified MSN (MSN-AmEA) was found to be 858.41 m2 g−1 with a pore size of 2.69 nm which could accommodate a high concentration of quercetin 118% higher than MSN. In addition, the colloidal stability of MSN-AmEA was greatly improved as indicated by high zeta potential especially at pH 4 compared to MSN. In contrast to MSN, MSN-AmEA has better in controlling quercetin release triggered by pH, thanks to the presence of the functional groups that have a pose-sensitive interaction hence it may fully control the quercetin release, as elaborated by the DFT study. Therefore, the controlled release of quercetin over MSN-AmEA verified its capability of acting as a smart drug delivery system.
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有机表面工程介孔二氧化硅纳米颗粒通过 pH 刺激控制槲皮素的释放
控制疏水性药物如槲皮素在生理条件下的过早释放仍然是近年来推动智能和反应性药物载体发展的挑战。目前的工作报道了通过具有胺(作为带正电荷的基团)和羧基(带负电荷的基团)即 4-((2-氨基乙基)氨基)-4- 的功能化合物对介孔二氧化硅纳米粒子 (MSN) 进行表面改性oxobut-2-enoic acid (AmEA) 通过简单的机械化学方法制备。通过 TGA、N 2吸附-解吸、PSA-zeta、SEM 和 TEM评估了 MSN 表面改性对物理、结构和形态特征的影响。发现 AmEA 修饰的 MSN (MSN-AmEA) 的 BET 表面积为 858.41 m 2 g −1孔径为 2.69 nm,可容纳比 MSN 高 118% 的高浓度槲皮素。此外,与 MSN 相比,MSN-AmEA 的胶体稳定性得到了极大改善,这由高 zeta 电位表明,尤其是在 pH 4 时。与 MSN 相比,MSN-AmEA 在控制由 pH 触发的槲皮素释放方面具有更好的效果,这要归功于存在具有姿势敏感相互作用的官能团,因此它可以完全控制槲皮素的释放,正如 DFT 研究所阐述的那样。因此,槲皮素在 MSN-AmEA 上的控释验证了其作为智能药物递送系统的能力。