The protective effects of synthetic lung
surfactant Exosurf® (containing
cetyl alcohol) against
endotoxin-induced
inflammation have been demonstrated in the literature. Thus, it is envisioned that nanoparticles loaded with
quercetin (Q-NPs) prepared with binary mixtures of
cetyl alcohol (CA) and Gelucire 44/14® (gelucire) as matrix materials will be capable of overcoming some of the protracted challenges confronting clinical application of
quercetin and possess innate protective activity against inflammatory responses, which could be synergistic with
quercetin. The NPs were stable in simulated
biological media while retaining their particle size and spherical morphology. Further analysis by gel permeation chromatography, spectroscopic analysis (ultraviolet-visible, fluorescence, and Fourier transform infrared spectroscopy) indicated entrapment of
quercetin in NPs. Q-NPs effectively enhanced
xanthine oxidase inhibitory and
free radical scavenging effect of
quercetin. Furthermore, Q-NPs showed marked reduction (compared to
quercetin alone) in production of
nitric oxide and
cytokine (
interleukin-6 and
tumor necrosis factor alpha) from
lipopolysaccharide-activated macrophages. Superiority of Q-NPs over
quercetin alone was confirmed from in vivo anti-inflammatory efficacy studies in BALB/c mice. Data from additional studies with blank NPs (without
quercetin) showed that the NPs reported herein most likely possessed intrinsic protective properties against LPS-induced
inflammation. Although further mechanistic studies are warranted, the overall work depicted a novel approach of possible exploiting innate protective properties of NPs in
quercetin delivery for treating oxidative stress and
inflammation.