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Curcumin is a natural molecule with proved anticancer efficacy on several human cancer cell lines. However, its clinical application has been limited due to its poor bioavailability. Nanocarrier-based drug delivery approaches could make curcumin dispersible in aqueous media, thus overtaking the limits of its low solubility. The aim of this study was to increase the bioavailability and the antitumoral activity of curcumin, by entrapping it into nanostructured lipid carriers (NLCs). For this purpose here we describe the preparation and characterization of three kinds of curcumin-loaded NLCs. The nanosystems allowed the achievement of a controlled release of curcumin, the amounts of curcumin released after 24 h from Compritol-Captex, Compritol-Miglyol, and Compritol NLCs being, respectively, equal to 33, 28, and 18% w/w on the total entrapped curcumin. Considering the slower curcumin release profile, Compritol NLCs were chosen to perform successive in vitro studies on ovarian cancer cell lines. The results show that curcumin-loaded NLCs maintain anticancer activity, and reduce cell colony survival more effectively than free curcumin. As an example, the ability of A2780S cells to form colonies was decreased after treatment with 5 μM free curcumin by 50% ± 6, whereas, at the same concentration, the delivery of curcumin with NLC significantly (p < 0.05) inhibited colony formation to approximately 88% ± 1, therefore potentiating the activity of curcumin to inhibit A2780S cell growth. The obtained results clearly suggest that the entrapment of curcumin into NLCs increases curcumin efficacy in vitro, indicating the potential use of NLCs as curcumin delivery systems.

Sicilian cultivars of prickly pear (Opuntia ficus indica) produce yellow, red, and white fruits, due to the combination of two betalain pigments, the purple-red betanin and the yellow-orange indicaxanthin. The betalain distribution in the three cultivars and the antioxidant activities of methanolic extracts from edible pulp were investigated. In addition, the reducing capacity of purified betanin and indicaxanthin was measured. According to a spectrophotometric analysis, the yellow cultivar exhibited the highest amount of betalains, followed by the red and white ones. Indicaxanthin accounted for about 99% of betalains in the white fruit, while the ratio of betanin to indicaxanthin varied from 1:8 (w:w) in the yellow fruit to 2:1 (w:w) in the red one. Polyphenol pigments were negligible components only in the red fruit. When measured as 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (Trolox) equivalents per gram of pulp, the methanolic fruit extracts showed a marked antioxidant activity. Vitamin C did not account for more than 40% of the measured activity. In addition, the extracts dose-dependently inhibited the organic hydroperoxide-stimulated red cell membrane lipid oxidation, as well as the metal-dependent and -independent low-density lipoprotein oxidation. The extract from the white fruit showed the highest protection in all models of lipid oxidation. Purified betanin and indicaxanthin were more effective than Trolox at scavenging the [2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)] diammonium salt cation radical. Cyclic voltammetric measurements show two anodic waves for betanin and indicaxanthin, and differential pulse voltammetry shows three anodic waves for betanin, with calculated peak potentials of 404, 616, and 998 mV, and two anodic waves for indicaxanthin, with peak potentials of 611 and 895 mV. Betanin underwent complex formation through chelation with Cu(2+), whereas indicaxanthin was not modified. These findings suggest that the above betalains contribute to the antioxidant activity of prickly pear fruits.