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In Vitro Dissolution, Cellular Membrane Permeability, and Anti-Inflammatory Response of Resveratrol-Encapsulated Mesoporous Silica Nanoparticles
Molecular Pharmaceutics ( IF 4.9 ) Pub Date : 2017-11-27 00:00:00 , DOI: 10.1021/acs.molpharmaceut.7b00529
Estelle Juère 1, 2 , Justyna Florek 1 , Meryem Bouchoucha 2 , Siddharth Jambhrunkar 3, 4 , Kuan Yau Wong 3, 4 , Amirali Popat 3, 4 , Freddy Kleitz 1, 2
Affiliation  

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–1, 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.

中文翻译:

白藜芦醇包裹的介孔二氧化硅纳米粒子的体外溶解,细胞膜通透性和抗炎反应。

使用纳米颗粒将药物定型至亚微米和纳米尺寸已被广泛用于制药工业中,以克服潜在治疗剂的不良水溶性。在这里,我们报道了白藜芦醇的封装和释放,白藜芦醇,一种有希望的消炎和抗癌保健食品,从各种粒径(即90、150和300 nm)的MCM-48型二氧化硅纳米球的中孔中释放出来。此外,还评估了载体孔径对药物溶解度的影响(3.5对7 nm)。从我们的结果可以看出,饱和溶解度不仅取决于孔径,而且取决于纳米载体的粒径。而且,借助我们的白藜芦醇-介孔二氧化硅纳米颗粒配方,我们已经观察到,当通过人结肠癌细胞单层(Caco-2)测试时,与白藜芦醇悬浮液相比,封装在MCM-48纳米颗粒(90 nm)中的白藜芦醇的渗透性可以提高。使用在体外NF-κB检测中,我们显示白藜芦醇胶囊包封不会改变其生物活性,并且在较低浓度(即5μgmL –1)下,与白藜芦醇悬浮液和溶液相比,白藜芦醇胶囊包埋提供更高的抗炎活性。综合起来,已报道的结果清楚地表明了小尺寸介孔二氧化硅纳米颗粒作为疏水性药物和营养保健品的下一代纳米载体的潜力。
更新日期:2017-11-28
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