Mesoporous silica as topical nanocarriers for quercetin: characterization and in vitro studies

Abstract

The flavonoid quercetin is extensively studied for its antioxidant and chemopreventive properties.However the poor water-solubility, low stability and short half-life could restrict its use in skin care products and therapy.The present study is aimed to evaluate the potential of aminopropyl functionalized mesoporous silica nanoparticles (NH 2 -MSN) as topical carrier system for quercetin delivery. Thermo gravimetric analysis, X-ray diffraction, high resolution transmission electron microscopy, nitrogen adsorption isotherms, FT-IR spectroscopy, zeta potential measurements and differential scanning calorimetry allowed analyzing with great detail the organic-inorganic molecular interaction.The protective effect of this vehicle on UV-induced degradation of the flavonoid was investigated revealing a certain positive influence of the inclusion on the photostability over time.Epidermal accumulation and transdermal permeation of this molecule were ex vivo evaluated using porcine skin mounted on Franz diffusion cells. The inclusion complexation with the inorganic nanoparticles increased the penetration of quercetin into the skin after 24 h post-application without transdermal delivery.The effect of quercetin alone or given as complex with NH 2 -MSN on proliferation of JR8 human melanoma cells was evaluated by sulforhodamine B colorimetric proliferation assay. At a concentration 60 M the complex with NH 2 -MSN was more effective than quercetin alone, causing about 50% inhibition of cell proliferation.

Chemical and pharmaceutical evaluation of the relationship between triazole linkers and pore size on cyclodextrin–calixarene nanosponges used as carriers for natural drugs

“…Indeed, many studies have shown that these compounds have anticancer activities against various cancer cells such as colon, prostate, skin, glioma and breast cancer cells. [13][14][15] However pharmaceutical applications of phenolic compounds in general are severely hampered by their unsatisfactory bioavailability, due to poor water solubility, low stability and short half-life. 15,16 In addition, the biological activity of these natural products can be affected by physicochemical factors such as light, oxygen/air, humidity or other reactive compounds from the environment.…”

“…[13][14][15] However pharmaceutical applications of phenolic compounds in general are severely hampered by their unsatisfactory bioavailability, due to poor water solubility, low stability and short half-life. 15,16 In addition, the biological activity of these natural products can be affected by physicochemical factors such as light, oxygen/air, humidity or other reactive compounds from the environment. In order to protect these bioactive compounds against degradation and to enhance their bioavailability, in recent years various encapsulation and complexation methods have been explored.…”

Experimental and theoretical study of quercetin complexes formed on pure silica and Zn-modified mesoporous MCM-41 and SBA-16 materials

“…Thus, loading of flavanols in nanoporous silica systems can stabilize and protect them from degradation, ensuring high loading capacity [22][23][24][25][26][27]. Preliminary studies show that immobilization of quercetin in the mesoporous silica, like MCM-41, successfully stabilized quercetin, improving its antioxidant efficacy [28,29,31]. In addition, the increased specific surface area of mesoporous silica particles could eventually improve the bioavailability of bioactive compounds.…”

Cellular Interactions and Formation of an Epithelial “Nanocoating-Like Barrier” with Mesoporous Silica Nanoparticles

“…Generally, silica nanoparticles with an average size less than 25 nm can penetrate but could not permeate the skin [24]. As the vehicles of quercetin, MSNs with an average size of 250 nm can facilitate drug penetration in the skin while without transdermal delivery [26]. This could be due to the barrier property of stratum corneum.…”