Optimization of rhein-loaded polymeric nanoparticles using a factorial design and evaluation of the cytotoxic and anti-inflammatory effects.

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.

Development, characterization and in vitro evaluation of biodegradable rhein-loaded microparticles for treatment of osteoarthritis.

Rhein is an active metabolite of the drug diacerein, whose anti-inflammatory properties have been demonstrated in both in vitro and in vivo models. However, the low oral bioavailability of rhein has limited its utility as a potential treatment of osteoarthritis (OA), a chronic inflammatory disease. In order to overcome this limitation, the aim of this work was the development of a drug delivery system intended for intra-articular administration of rhein, based on polymeric biodegradable PLGA microparticles (MPs) loaded with the drug.