ABSTRACT
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.
Subject(s)
Animals , Dogs , Female , Humans , Rats , Administration, Oral , Antioxidants/chemistry , Biological Availability , Calorimetry, Differential Scanning , Dose-Response Relationship, Drug , Drug Carriers , Hep G2 Cells , Hesperidin/chemistry , Light , Madin Darby Canine Kidney Cells , Micelles , Phosphatidylcholines/chemistry , Polyethylene Glycols/chemistry , Rats, Sprague-Dawley , Scattering, Radiation , Solubility , Solvents , Vitamin E/chemistry , Water/chemistry , alpha-Tocopherol/chemistryABSTRACT
<p><b>OBJECTIVE</b>Dermabrasion has been of great value in plastic surgery. Dermabrasion was developed for a specific indication; however, within a very short time, the concept of dermabrasion found wide applicability. This study was to investigate the application of dermabrasion in the treatment of acne scars.</p><p><b>METHODS</b>From Feb. 1996 to May 2004, a total of 110 patients with acne scar were treated with dermabrasion.</p><p><b>RESULTS</b>Postoperatively, the curative results were achieved in 45 cases; good results in 40 cases and effective results in 25 cases. The study revealed that the patients at 18-46 years of age have good results.</p><p><b>CONCLUSIONS</b>Dermabrasion is a good and safe technique to treat the scar of acne.</p>