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Curcumin diglutaric acid-loaded polyethylene glycol-chitosan oligosaccharide-coated superparamagnetic iron oxide nanoparticles (CG-PEG-CSO-SPIONs) were fabricated by co-precipitation and optimized using a Box–Behnken statistical design in order to achieve the minimum size, optimal zeta potential (≥ ±20 mV), and maximum loading efficiency and capacity. The results demonstrated that CG-PEG-CSO-SPIONs prepared under the optimal condition were almost spherical in shape with a smooth surface, a diameter of 130 nm, zeta potential of 30.6 mV, loading efficiency of 83.3%, and loading capacity of 8.3%. The vibrating sample magnetometer results of the optimized CG-PEG-CSO-SPIONs showed a superparamagnetic behavior. Fourier transform infrared spectroscopy and X-ray diffraction analyses indicated that the CG physically interacted with PEG-CSO-SPIONs. In addition, the CG-PEG-CSO-SPIONs could be stored dry for up to 12 weeks or in aqueous solution for up to 4 days at either 4 °C or 25 °C with no loss of stability. The CG-PEG-CSO-SPIONs exhibited a sustained release profile up to 72 h under simulated physiological (pH 7.4) and tumor extracellular (pH 5.5) environments. Furthermore, the CG-PEG-CSO-SPIONs showed little non-specific protein binding in the simulated physiological environment. The CG-PEG-CSO-SPIONs enhanced the cellular uptake and cytotoxicity of CG against human colorectal adenocarcinoma HT-29 cells compared to free CG, and more CG was delivered to the cells after applying an external magnetic field. The overall results suggest that PEG-CSO-SPIONs have potential to be used as a novel drug delivery system for CG.

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Capsaicin (CAP) is a pungent alkaloid of chili peppers that is obtained from chili peppers that has a variety of pharmacological activities and can be used in various areas, such as functional foods, nutritional supplements and medical nutrition. Capsaicin has important anticancer, antioxidant and anti-inflammatory properties that allow to be applied as treatment for several diseases. However, its lack of water solubility, as well as its poor oral bioavailability in biological systems, show limiting factors for its successful application. Recently, the formulation of capsaicin for food and pharmaceutical use is limited. Therefore, the present study emphasized on preparation of capsaicin-loaded chitosan nanoparticles (CAP-CSNPs) and design and optimization of the formulation using Box-Behnken experimental design (BBD) and response surface methodology (RSM). The capsaicin-loaded chitosan nanoparticles were prepared by o/w emulsification and ionotropic gelification. The optimized formulation of capsaicin-loaded chitosan nanoparticles had a chitosan concentration of 0.11 (%w/v), a Tween 80® concentration of 1.55 (%w/v) and a CAP concentration of 1 mg/mL and that it should be stored at 4°C. Box-Behnken experimental design and response surface methodology was found to be a powerful technique for design and optimization of the preparation of capsaicin-loaded chitosan nanoparticles using limited number of experimental runs. Our study demonstrated that capsaicin-loaded chitosan nanoparticles can be potentially utilized as dietary supplements, nutraceuticals and functional foods.