In Vitro Dissolution, Cellular Membrane Permeability, and Anti-Inflammatory Response of Resveratrol-Encapsulated Mesoporous Silica Nanoparticles

Estelle Juère, Justyna Florek, Meryem Bouchoucha, Siddharth Jambhrunkar, Kuan Yau Wong, Amirali Popat, Freddy Kleitz

Sizing drugs down to the sub-micron 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.