Enhanced water solubility, antioxidant activity, and oral absorption of hesperetin by D-α-tocopheryl polyethylene glycol 1000 succinate and phosphatidylcholine / 浙江大学学报（英文版）（B辑：生物医学和生物技术）

Hesperetin, an abundant bioactive component of citrus fruits, is poorly water-soluble, resulting in low oral bioavailability. We developed new formulations to improve the water solubility, antioxidant activity, and oral absorption of hesperetin. Two nano-based formulations were developed, namely hesperetin-TPGS (D-α-tocopheryl polyethylene glycol 1000 succinate) micelles and hesperetin-phosphatidylcholine (PC) complexes. These two formulations were prepared by a simple technique called solvent dispersion, using US Food and Drug Administration (FDA)-approved excipients for drugs. Differential scanning calorimetry (DSC) and dynamic light scattering (DLS) were used to characterize the formulations' physical properties. Cytotoxicity analysis, cellular antioxidant activity assay, and a pharmacokinetic study were performed to evaluate the biological properties of these two formulations. The final weight ratios of both hesperetin to TPGS and hesperetin to PC were 1:12 based on their water solubility, which increased to 21.5- and 20.7-fold, respectively. The hesperetin-TPGS micelles had a small particle size of 26.19 nm, whereas the hesperetin-PC complexes exhibited a larger particle size of 219.15 nm. In addition, the cellular antioxidant activity assay indicated that both hesperetin-TPGS micelles and hesperetin-PC complexes increased the antioxidant activity of hesperetin to 4.2- and 3.9-fold, respectively. Importantly, the in vivo oral absorption study on rats indicated that the micelles and complexes significantly increased the peak plasma concentration (Cmax) from 2.64 μg/mL to 20.67 and 33.09 μg/mL and also increased the area under the concentration-time curve of hesperetin after oral administration to 16.2- and 18.0-fold, respectively. The micelles and complexes increased the solubility and remarkably improved the in vitro antioxidant activity and in vivo oral absorption of hesperetin, indicating these formulations' potential applications in drugs and healthcare products.

Effects of alpha-tocopherol on fracture resistance after endodontic treatment, bleaching and restoration

Abstract This study evaluated the effects of 10% alphatocopherol on the fracture resistance of endodontically treated teeth subjected to tooth bleaching with hydrogen peroxide and immediately restored with composite resin. Fifty bovine incisors were selected, including 10 sound teeth that constituted the control group (G1 (C)). The remaining 40 teeth, which were endodontically treated, were divided into four groups (n = 10): G2 (CR), consisting of teeth immediately restored with composite resin; G3 (HP + CR), consisting of teeth subjected to tooth bleaching with 38% hydrogen peroxide and immediately restored with composite resin; G4 (HP + SA + CR), which received treatment similar to that used for G3, but with 10% sodium ascorbate gel applied after the bleaching protocol; and G5 (HP + AT + CR), which was similar to G4 but included 10% alphatocopherol gel as an antioxidant. After 24 h, composite restorations were performed, and teeth were subjected to a fracture resistance test at a speed of 0.5 mm/min in an electromechanical testing machine. The axial force was applied with an angle of incidence of 135° relative to the long axis of the root. Data were subjected to ANOVA and Tukey tests (p = 0.05). G1 exhibited the highest fracture resistance (p < 0.05). No significant differences among the other experimental groups were observed. The 10% sodium ascorbate and 10% alphatocopherol gels did not improve the fracture resistance of endodontically treated teeth subjected to bleaching with 38% hydrogen peroxide.