RESUMEN
Wound-healing activity of the crystalline form of dihydroquercetin and its microtubular pseudopolymorphic modification obtained by crystal engineering was compared using the rat model of IIIA degree burn. The rate of wound healing in the group treated with microtubular pseudopolymorphic modification of dihydroquercetin was 4.8±0.1%, which was higher by 11.6% than in the group treated with crystalline form (4.3±0.1%). Bioavailability analysis on MDCK cell culture showed that the apparent permeability coefficient of microtubular pseudopolymorphic modification was higher than that of crystalline form by 31.1% (19.4±0.2×10-4 and 14.8±0.3×10-4 cm/sec, respectively). It was proven that the use of crystal engineering improved the biopharmaceutical parameters of dihydroquercetin and increased its pharmacological efficiency.
Asunto(s)
Quercetina/análogos & derivados , Cicatrización de Heridas/fisiología , Animales , Masculino , Polimorfismo Genético/genética , Quercetina/farmacología , Ratas , Ratas Sprague-Dawley , Medicina Regenerativa/métodos , Cicatrización de Heridas/genéticaRESUMEN
Flavonoid-mediated materials are promising substances for the design of new functional materials because of their bioactivity, eco-friendliness, and cost-effectiveness. Dihydroquercetin (DHQ) is the major flavonoid in the wood of Larix dahurica Turcz. Previously some new modifications were created on the basis of DHQ, they were characterized by different morphological, physico-chemical and biopharmaceutical properties. This study was performed to research the influence of the solvent on the formation of the solid phase in DHQ microtubes and crystal form as commercially available active pharmaceutical ingredient (API). The choice of the models for the computational simulation was based on the data of differential scanning calorimetry. All calculations were performed using Materials Science Suite. In silico analysis demonstrated that the molecules of solvent are a key player in the formation of the solid phase of the flavonoid-mediated material. Also the comparative analysis of physical characteristics between DHQ microtubes and crystal form was performed. These data give an opportunity to suggest, that DHQ microtubes may have a grate application as the dressing material and in the drug delivering. The results of this study could be helpful for the design of the new flavonoid-mediated materials by crystal engineering.
Asunto(s)
Larix/química , Quercetina/análogos & derivados , Simulación por Computador , Modelos Químicos , Quercetina/químicaRESUMEN
The antioxidant effect of dihydroquercetin (DHQ) was studied in Wistar rats with experimental hepatitis, caused by tetrachloromethane (CCl(4)). Animals were divided into three groups: intact (n = 9); control (n = 9) which received CCl(4) subcutaneously for 4 days (4 mL/kg); and experimental (n = 9) which received DHQ (100 mg/kg) for 4 days prior to the first administration of CCl(4) and during the course of the subsequent 14 days. DHQ was intubated per os, using a water crystalline suspension. The content of products of lipid peroxidation, reacting with thiobarbituric acid in the serum and liver of the control animals, was increased by more than 1.5 fold compared with the intact and experimental animals (p < 0.01). The blood plasma antioxidant activity of the control animals was 1.8 to 2 times lower than that of experimental and intact animals (p < 0.01) It is suggested that the data obtained are dependent on the anti-oxidant properties of DHQ.