There is great interest in developing colloidal delivery systems to enhance the water solubility and oral bioavailability of curcumin, which is a hydrophobic nutraceutical claimed to have several health benefits. In this study, a natural emulsifier was used to form sophorolipid-coated curcumin nanoparticles. The curcumin was loaded into sophorolipid micelles using a pH-driven mechanism based on the decrease in curcumin solubility at lower pH values. The sophorolipid-coated curcumin nanoparticles formed using this mechanism were relatively small (61 nm) and negatively charged (-41 mV). The nanoparticles also had a relatively high encapsulation efficiency (82%) and loading capacity (14%) for curcumin, which was present in an amorphous state. Both in vitro and in vivo studies showed that the curcumin nanoparticles had an appreciably higher bioavailability than that of free curcumin crystals (2.7-3.6-fold), which was mainly attributed to their higher bioaccessibility. These results may facilitate the development of natural colloidal systems that enhance the oral bioavailability and bioactivity of curcumin in food, dietary supplements, and pharmaceutical products.
Curcumin is a bioactive phytochemical that can be utilized as a nutraceutical or pharmaceutical in functional foods, supplements, and medicines. However, the application of curcumin as a nutraceutical in commercial food and beverage products is currently limited by its low water-solubility, chemical instability, and poor oral bioavailability. In this study, all-natural colloidal delivery systems were developed to overcome these challenges, which consisted of saponin-coated curcumin nanoparticles formed using a pH-driven loading method. The physicochemical and structural properties of the curcumin nanoparticles formed using this process were characterized, including particle size distribution, surface potential, morphology, encapsulation efficiency, and loading capacity. Fourier transform infrared spectroscopy and X-ray diffraction indicated that curcumin was present in the nanoparticles in an amorphous form. The curcumin nanoparticles were unstable to aggregation at low pH values (<3) and high NaCl concentrations (>200 mM), which was attributed to a reduction in electrostatic repulsion between them. However, they were stable at higher pH values (3 to 8) and lower NaCl levels (0 to 200 mM), due to a stronger electrostatic repulsion between them. They also exhibited good stability during refrigerated storage (4 °C) or after conversion into a powdered form (lyophilized). A simulated gastrointestinal tract study demonstrated that the in vitro bioaccessibility was around 3.3-fold higher for curcumin nanoparticles than for free curcumin. Furthermore, oral administration to Sprague Dawley rats indicated that the in vivo bioavailability was around 8.9-fold higher for curcumin nanoparticles than for free curcumin. These results have important implications for the development of curcumin-enriched functional foods, supplements, and drugs.
Fluid and gelled nutraceutical emulsions were formulated from quercetin-loaded caseinate-stabilized emulsions by the addition of gellan gum with or without acidification with glucono-δ-lactone. Gellan gum addition increased the viscosity or gel strength of the fluid and gelled emulsions, respectively. The behavior of the nutraceutical emulsions in a simulated gastrointestinal tract depended upon their initial composition. Fluid emulsions containing different gellan gum levels (0-0.2%) had similar protein and lipid hydrolysis rates as well as similar quercetin bioaccessibility (∼51%). Conversely, proteolysis, lipolysis, and quercetin bioaccessibility decreased with an increasing gellan gum level in the gelled emulsions. In comparison to gelled emulsions, fluid emulsions were digested more rapidly and led to higher quercetin bioaccessibility. There was a good correlation between quercetin bioaccessibility and the lipolysis rate. These findings are useful for designing nutraceutical-loaded emulsions that can be used in a wide range of food products with different rheological properties.
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