Department of Inorganic Chemistry - Functional Materials, Faculty of Chemistry, University of Vienna , Währinger Straße 42, 1090 Vienna, Austria.
Department of Chemistry, Université Laval , Quebec City G1V 0A6, Canada.
Mol Pharm. 2017 Dec 4;14(12):4431-4441. doi: 10.1021/acs.molpharmaceut.7b00529. Epub 2017 Nov 27.
Sizing drugs down to the submicron and nanometer scale using nanoparticles has been extensively used in pharmaceutical industries to overcome the poor aqueous solubility of potential therapeutic agents. Here, we report the encapsulation and release of resveratrol, a promising anti-inflammatory and anticancer nutraceutical, from the mesopores of MCM-48-type silica nanospheres of various particle sizes, i.e., 90, 150, and 300 nm. Furthermore, the influence of the carrier pore size on drug solubility was also evaluated (3.5 vs 7 nm). From our results, it is observed that the saturated solubility could depend not only on the pore size but also on the particle size of the nanocarriers. Moreover, with our resveratrol-mesoporous silica nanoparticles formulation, we have observed that the permeability of resveratrol encapsulated in MCM-48 nanoparticles (90 nm) can be enhanced compared to a resveratrol suspension when tested through the human colon carcinoma cell monolayer (Caco-2). Using an in vitro NF-κB assay, we showed that resveratrol encapsulation did not alter its bioactivity and, at lower concentration, i.e., 5 μg mL, resveratrol encapsulation provided higher anti-inflammatory activity compared to both resveratrol suspension and solution. All combined, the reported results clearly highlight the potential of small size mesoporous silica nanoparticles as next generation nanocarriers for hydrophobic drugs and nutraceuticals.
使用纳米颗粒将药物缩小到亚微米和纳米级规模已广泛应用于制药行业，以克服潜在治疗剂的不良水溶性。在这里，我们报告了白藜芦醇的包封和释放，白藜芦醇是一种有前途的抗炎和抗癌营养保健品，来自各种粒径的 MCM-48 型硅纳米球的介孔中，即 90、150 和 300nm。此外，还评估了载体孔尺寸对药物溶解度的影响（3.5 与 7nm）。从我们的结果可以看出，饱和溶解度不仅取决于孔径，还取决于纳米载体的粒径。此外，使用我们的白藜芦醇介孔硅纳米粒子制剂，我们观察到当通过人结肠癌细胞单层（Caco-2）进行测试时，包封在 MCM-48 纳米粒子（90nm）中的白藜芦醇的渗透性可以比白藜芦醇悬浮液增强。通过体外 NF-κB 测定，我们表明白藜芦醇的包封不会改变其生物活性，并且在较低浓度下，即 5μgmL，与白藜芦醇悬浮液和溶液相比，白藜芦醇包封提供了更高的抗炎活性。综上所述，报告的结果清楚地突出了小尺寸介孔硅纳米粒子作为下一代用于疏水性药物和营养保健品的纳米载体的潜力。
