In vitro evaluation of anti-methylglyoxal/glyoxal activity of three phytosterols using glycated bovine serum albumin models.

Reactive intermediate dicarbonyls, such as methylglyoxal (MGO) and glyoxal (GO), have received extensive attention recently due to their high reactivity and capability to form advanced glycation end products (AGEs) in foods, which have been implicated in the progression of age-related complaints. We aimed to investigate the effects of three structurally different phytosterols (PS), including stigmasterol (SS), ß-sitosterol (ßS), and γ-oryzanol (γO), on AGEs-formation by measuring their anti-GO/MGO activity. The glycoxidation-based products, SDS-PAGE intensity, free lysine, protein thiols, fluorescence microscopy clicks, scavenging of dicarbonyl activity, and protein aggregation in bovine serum albumin (BSA) models were therefore measured. The results showed that PS could strongly inhibit fluorescent-AGEs, lysine residues, intermediate di-carbonyls, beside their disaggregation effects in a dose and structure dependent manner. Additionally, γ-oryzanol strongly inhibited AGEs more than the other PS, mostly due to its distinctive structure. Our results will provide a new foundation for development of different structure of PS as natural AGEs-inhibitors.

Ketoprofen mesoporous silica nanoparticles SBA-15 hard gelatin capsules: preparation and in vitro/in vivo characterization.

SBA-15 is used to enhance the bioavailability of poorly soluble ketoprofen (KP) through stabilization of its amorphous state. Additionally, the current work provides a complete in vitro and in vivo study on preformulated KP-SBA-15 sample and formulated KP-SBA-15 in hard gelatin capsule. Loading of KP was done by a novel method called immersion-rotavapor method. KP was quantified by extraction and thermal gravimetric analysis (TGA). Characterization of the loaded SBA-15 sample was done by high resolution transmission electron microscopy (HRTEM), small angle X-ray diffraction (SAXRD), nitrogen adsorption/desorption isotherms, differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy and dissolution profiles. The loaded sample was formulated in hard gelatin capsule. The anti-inflammatory and analgesic studies were carried out on 24 adult male albino rats. TGA and extraction results showed 54.4 wt% of drug incorporated. Characterization of KP-SBA-15 sample confirmed the successful encapsulation of KP into the carrier pores in a molecular amorphous state. Additionally, loading of KP did not affect the mesoporous internal structure. During the first 5 min, the dissolution study showed very high release rates; nearly 50% of KP was released. These results were reflected on the in vivo study resulting in 82% inhibition in edema after 1 h and maximum analgesia after 30 min from the administration of the formulated sample. SBA-15 mesoporous silica nanoparticle proved to be a very promising drug delivery carrier that can be used as a facile way to enhance the bioavailability of poorly soluble drugs.