Long-acting bioactive composition based on chitosan and taxifolin

Baranov, I. A.; Dzhons, Daria Yu.; Будруев, А. В.; Мочалова, А. Е.; Смирнова, Л. А.; Koryagin, Andrey V.

doi:10.1134/s2075113315050020

Cited by 8 publications

(5 citation statements)

References 12 publications

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“…The use of Tax polymorphs, characterized by a better solubilization rate than Pristine-Tax, would consent to improve its efficacy and eventually extend its application field without the necessity of using excipients. In fact, reviewing the literature, several papers disclose the use of excipients as a strategy to increase Tax bioavailability [ 56 , 57 , 58 , 59 , 60 ].…”

Section: Resultsmentioning

confidence: 99%

Exploring Taxifolin Polymorphs: Insights on Hydrate and Anhydrous Forms

et al. 2021

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Taxifolin, also known as dihydroquercetin, possesses several interesting biological properties. The purpose of the study was to identify polymorphs of taxifolin prepared using crystallization in different solvents. Data from X-ray powder diffraction, differential scanning calorimetry, and thermogravimetry enabled us to detect six different crystalline phases for taxifolin. Besides the already known fully hydrated phase, one partially hydrated phase, one monohydrated phase, two anhydrous polymorphs, and one probably solvated phase were obtained. The unit cell parameters were defined for three of them, while one anhydrous polymorph was fully structurally characterized by X-ray powder diffraction data. Scanning electron microscopy and hot stage microscopy were also employed to characterize the crystallized taxifolin powders. The hydrate and anhydrous forms showed remarkable stability in drastic storage conditions, and their solubility was deeply evaluated. The anhydrous form converted into the hydrate form during the equilibrium solubility study and taxifolin equilibrium solubility was about 1.2 mg/mL. The hydrate taxifolin intrinsic dissolution rate was 56.4 μg cm−2 min−1. Using Wood’s apparatus, it was not possible to determine the intrinsic dissolution rate of anhydrous taxifolin that is expected to solubilize more rapidly than the hydrate form. In view of its high stability, its use can be hypothesized.

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Section: Resultsmentioning

confidence: 99%

Exploring Taxifolin Polymorphs: Insights on Hydrate and Anhydrous Forms

et al. 2021

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“…These flavonoids are well-known natural antioxidants whose potential health benefits have attracted a great deal of interest in their studies as prospective drugs [ 7 , 32 , 33 , 34 , 35 , 36 , 37 , 38 , 39 ]. Thus, a large and growing body of literature has been devoted to the modification of their biopharmaceutical and physicochemical properties, such as antioxidant activity and bioavailability, by crystal engineering [ 40 , 41 , 42 , 43 , 44 ], obtaining solid dispersions [ 45 , 46 , 47 , 48 , 49 ], and the development of new polymorphic forms [ 50 , 51 , 52 , 53 , 54 ]. This report is in line with the abovementioned works and aims to study the possible alteration of the antioxidant activity of flavonoids by combining them with other natural antioxidants.…”

Section: Introductionmentioning

confidence: 99%

Flavonoids with Glutathione Antioxidant Synergy: Influence of Free Radicals Inflow

et al. 2020

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This report explores the antioxidant interaction of combinations of flavonoid–glutathione with different ratios. Two different 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid radical (ABTS•+)-based approaches were applied for the elucidation of the antioxidant capacity of the combinations. Despite using the same radical, the two approaches employ different free radical inflow systems: An instant, great excess of radicals in the end-point decolorization assay, and a steady inflow of radicals in the lag-time assay. As expected, the flavonoid–glutathione pairs showed contrasting results in these two approaches. All the examined combinations showed additive or light subadditive antioxidant capacity effects in the decolorization assay. This effect showed slight dilution dependence and did not change when the initial ABTS•+ concentration was two times as high or low. However, in the lag-time assay, different types of interaction were detected, from subadditivity to considerable synergy. Taxifolin–glutathione combinations demonstrated the greatest synergy, at up to 112%; quercetin and rutin, in combination with glutathione, revealed moderate synergy in the 30–70% range; while morin–glutathione appeared to be additive or subadditive. In general, this study demonstrated that, on the one hand, the effect of flavonoid–glutathione combinations depends both on the flavonoid structure and molar ratio; on the other hand, the manifestation of the synergy of the combination strongly depends on the mode of inflow of the free radicals.

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“…Interestingly, the adaptogenic effect of taxifolin (dihydroquercetin) has been the subject of two studies, in which the authors confirmed that the formulation of taxifolin with chitosan as a vehicle produced a strong antihypoxic effect under conditions of experimental hypobaric hypoxia, with the lactate/pyruvate ratio much lower in the group of rats that received the taxifolin than in hypoxic animals ( Baranov et al, 2015;Murach et al, 2014). However, it is believed that the sum effect of a crude extract is most probably a synergy of different pharmacologically active compounds present in the extract, which might be responsible for the adaptogenic effect of HEHt (Wagner, 2011).…”

Section: Discussionmentioning

confidence: 97%