Optimization of rhein-loaded polymeric nanoparticles using a factorial design and evaluation of the cytotoxic and anti-inflammatory effects
Abstract
The aim of the work was to develop rhein loaded polymeric nanoparticles (R-PNPs). Nanoparticles were prepared by three methods, solvent emulsion-evaporation, double emulsion, and nanoprecipitation, by means of experimental design. Additionally, the effects of the best formulation on in vitro cytotoxicity and inflammation were evaluated. The solvent emulsion-evaporation method presented the highest encapsulation efficiency of the three techniques (38.41%), as well as had a mean diameter of 189.33 nm and a polydispersity index of less than 0.1. Despite efforts to optimize the encapsulation of rhein, the drug release from nanoparticles was close to 50% during the first 5 min, followed by a continuous release within 60 min. It was observed that macrophages exposed to the highest concentration of R-PNPs showed cell viability about 80% and at the lowest nanoparticle concentrations was closed to 100%. IL-1β in cell culture supernatants was decreased in the presence of R-PNPs and TNFα concentrations were lower than the sensitivity of the assay. ROS production was only inhibited with R-PNPs at concentrations of 2.5 and 5 μM. In conclusion, the solvent emulsion-evaporation was the best method evaluated to obtain nanoparticles with the de...Continue Reading
References
Pharmacological studies of diacerein in animal models of inflammation, arthritis and bone resorption
Protein adsorption and cellular uptake of cerium oxide nanoparticles as a function of zeta potential
Estimates of the prevalence of arthritis and other rheumatic conditions in the United States. Part I
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