Arriagada Francisco, Günther Germán, Morales Javier
Instituto de Farmacia, Facultad de Ciencias, Universidad Austral de Chile, Valdivia 5110033, Chile.
Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380494, Chile.
Pharmaceutics. 2020 Mar 26;12(4):302. doi: 10.3390/pharmaceutics12040302.
Nanosystems used in pharmaceutical formulations have shown promising results in enhancing the administration of drugs of difficult formulations. In particular, porous silica nanoparticles have demonstrated excellent properties for application in biological systems; however, there are still several challenges related to the development of more effective and biocompatible materials. An interesting approach to enhance these nanomaterials has been the development of nanoantioxidant carriers. In this work, a hybrid nanoantioxidant carrier based on porous silica nanoplatform with rosmarinic acid antioxidant immobilized on its surface were developed and characterized. Techniques such as dynamic light scattering (DLS), zeta potential, transmission electron microscopy (TEM), N adsorption-desorption measurements, differential scanning calorimetry (DSC), Fourier transform-infrared spectroscopy (FT-IR), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay were used to characterize and evaluate the antioxidant activity of nanocarriers. In addition, drug release profile was evaluated using two biorelevant media. The antioxidant activity of rosmarinic acid was maintained, suggesting the correct disposition of the moiety. Kinetic studies reveal that more morin is released in the simulated intestinal fluid than in the gastric one, while an anomalous non-Fickian release mechanism was observed. These results suggest a promising antioxidant nanocarrier suitable for future application in drug delivery.
用于药物制剂的纳米系统在改善难制剂药物的给药方面已显示出有前景的结果。特别是,多孔二氧化硅纳米颗粒已证明在生物系统中的应用具有优异的性能;然而,在开发更有效和生物相容的材料方面仍存在若干挑战。一种增强这些纳米材料的有趣方法是开发纳米抗氧化剂载体。在这项工作中,开发并表征了一种基于多孔二氧化硅纳米平台的杂化纳米抗氧化剂载体,其表面固定有迷迭香酸抗氧化剂。使用动态光散射(DLS)、zeta电位、透射电子显微镜(TEM)、N吸附-脱附测量、差示扫描量热法(DSC)、傅里叶变换红外光谱(FT-IR)和2,2-二苯基-1-苦基肼(DPPH)测定等技术来表征和评估纳米载体的抗氧化活性。此外,使用两种生物相关介质评估药物释放曲线。迷迭香酸的抗氧化活性得以保持,表明该部分的正确配置。动力学研究表明,在模拟肠液中释放的桑色素比在胃液中更多,同时观察到一种异常的非菲克释放机制。这些结果表明一种有前景的抗氧化纳米载体,适用于未来的药物递送应用。