Preparation and characterization of biodegradable polymeric nanoparticles containing curcuminoids

Abstract

In recent years, nanotechnology has provided significant advances of sciences and technology, including drug delivery technology, in which most of research has been attracted by an innovation of nanoparticulate carriers. Biodegradable polymeric nanoparticles prepared from poly (lactide-co-glycolide) (PLGA) copolymer have been widely investigated. Regarding curcuminoids, which have been used as an alternative therapeutic agent due to their various biological activities, especially antioxidant activity, they also have some limitations of use, e.g. low bioavailability, short circulation half-life, etc. Thus, an effective carrier is required to overcome this problem. In this study, curcuminoids-PLGA nanoparticles were prepared following the modified spontaneous emulsification solvent diffusion (modified-SESD) method, using vitamin E TPGS, poloxamer 407, or polyvinyl alcohol (PVA) as stabilizers. A three-factor, three-level Box-Behnken design was used to determine the effect of formulation ingredients, which were PLA-PGA ratio of PLGA (50:50, 75:25, or 85:15), curcuminoids amount (2, 6, or 10%) and concentration of each stabilizer on five responses of the nanoparticles; %recovery, particle size, size distribution, %curcuminoids content, and entrapment efficiency. From the simultaneous optimization technique, three optimal formulations were established. Each formulation was composed of (1) PLGA 50:50, curcuminoids 10%, and vitamin E TPGS 3%; (2) PLGA 50:50, curcuminoids 4.56%, and poloxamer 407 15% and (3) PLGA 50:50, curcuminoids 10%, and PVA 3%. The optimized formulations were prepared and evaluated on the five responses, which provided the actual values similar to the predicted values. In addition, the morphology study showed that the particles were spherical in shape with smooth surface and no unentrapped curcuminoids were observed. The in vitro release study of entrapped curcuminoids indicated that the release of curcuminoids was in a sustained manner.