Nanodispersions of taxifolin: Impact of solid-state properties on dissolution behavior

Shikov, Alexander N.; Pozharitskaya, Olga N.; Miroshnyk, Inna; Mirza, Sabiruddin; Уракова, И. Н.; Hirsjärvi, Samuli; Makarov, Valery G.; Heinämäki, Jyrki; Yliruusi, Jouko; Hiltunen, R.

doi:10.1016/j.ijpharm.2009.04.044

Cited by 53 publications

(31 citation statements)

References 22 publications

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“…Taxifolin is a natural compound with poor solubility, which leads to a low bioavailability [8]. This drawback limits the medical development as well as the use of food, health products and cosmetics.…”

Section: Introductionmentioning

confidence: 99%

Micronization of Taxifolin by Supercritical Antisolvent Process and Evaluation of Radical Scavenging Activity

Yang

Huang

et al. 2012

IJMS

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The aim of this study was to prepare micronized taxifolin powder using the supercritical antisolvent precipitation process to improve the dissolution rate of taxifolin. Ethanol was used as solvent and carbon dioxide was used as an antisolvent. The effects of process parameters, such as temperature (35–65 °C), pressure (10–25 MPa), solution flow rate (3–6 mL/min) and concentration of the liquid solution (5–20 mg/mL) on the precipitate crystals were investigated. With a lower temperature, a stronger pressure and a lower concentration of the liquid solution, the size of crystals decreased. The precipitation temperature, pressure and concentration of taxifolin solution had a significant effect. However, the solution flow rate had a negligible effect. It was concluded that the physicochemical properties and dissolution rate of crystalline taxifolin could be improved by physical modification such as particle size reduction using the supercritical antisolvent (SAS) process. Further, the SAS process was a powerful methodology for improving the physicochemical properties and radical scavenging activity of taxifolin.

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Section: Introductionmentioning

confidence: 99%

Micronization of Taxifolin by Supercritical Antisolvent Process and Evaluation of Radical Scavenging Activity

Yang

Huang

et al. 2012

IJMS

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“…Taxifolin solubility was assessed by preparing its saturated solution [2,5,12,19,20,23,24]. The excess amount of taxifolin was placed in 2 ml of water (about 5 g) and then exposed to 1-hour blending in a magnetic stirrer at a tempe-rature of no more than 50 °С.…”

Section: Conditions Of the Experiments Performed With Expert -6011 Coumentioning

confidence: 99%

Sonochemical Micronization of Taxifolin Aimed at Improving Its Bioavailability in Drinks for Athletes

Potoroko¹,

Калинина²,

Науменко³

et al. 2018

HSM

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Aim. The aim of this study is to overcome the problem of nutrient bioavailability in drinks for athletes, which is the result of their low permeability in metabolic processes of the body. For this purpose, we used sonochemical micronization of taxifolin -the most effective antioxidant. Materials and methods. To improve taxifolin solubility and bioavailability we used ultrasound treatment, which allowed us to provide taxifolin micronization on the following conditions: 5-, 15-and 25-minute treatment of 20 ± 2 kHz with radiation intensity of at least 10 W/cm 2 , power of 170, 400 and 630 W and temperature within 50 °С. The study was conducted using the following methods: microstructural analysis of native taxifolin and its solutions, including those obtained with sonochemical micronization; analysis of the disperse composition of taxifolin solutions; assessment of the total antioxidant activity of these solutions; assessment of taxifolin solubility and colloidal stability of its solutions. Results. We established that sonochemical micronization allows us to obtain solutions with the predominance of particles of no more than 100 nm. The morphological structure of taxifolin particles has significantly changed, particles are characterized by more homogenous and amorphous structure. We noticed some decrease in antioxidant activity under increased ultrasound exposure. Optimization of ultrasound exposure with the controlling parameter "average particle size" allowed us to establish the most effective mode (600 W, 18 minutes), which helped us to improve the colloidal stability of taxifolin solution and taxifolin solubility 6 times in comparison with the control sample. Conclusion. Sonochemical micronization should be regarded as convenient for the development of a new form of taxifolin with increased solubility and bioavailability, which can be used for the production of drinks for athletes.

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“…It has also been shown to possess anticancer properties, antimicrobial activities, antitumor effects, improved immune functions, and the prevention of cardiovascular diseases. Due to the above characteristics, taxifolin can be added to a wide range of applications such as food additives, healthy foods, medicine and other related products …”

Section: Introductionmentioning

confidence: 99%

“…Despite a wide range of biological effects, the use of taxifolin in food formulation is largely restricted because of its low water solubility (0.87–1.00 mg mL −1 at 25 °C) . Taxifolin hydrophobicity and its depressed rate of dissolution in the aqueous gastro‐intestinal liquids often result in inadequate bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Characterization of Taxifolin‐Loaded Lipid Nanovesicles (Liposomes, Niosomes, and Transfersomes) for Beverage Fortification

Hasibi

Nasirpour

Varshosaz

et al. 2019

Euro J Lipid Sci & Tech

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In this study, nanovesicles such as transfersomes, niosomes, and liposomes prepared by an ethanol injection method (EIM) (EIM) and formulated with soybean lecithin, Tween 80, Span 60, and cholesterol, are used to improve the bioavailability of taxifolin, a natural antioxidant with beneficial properties for health and food preservation. Morphology, stability, and the in-vitro release of the optimal formulations are fully examined. The obtained results indicate that taxifolin-loaded nanovesicles present sizes ranging between 98 and 215 nm along with a narrow size distribution (polydispersity index less than 0.250). The zeta potential of nanovesicles is negative and in the range of −20.40 to −32.20 mV. The optimal formulations with the maximum encapsulation efficiency (72-75%) are the transfersomes formulated with lecithin and Tween 80 in the presence and absence of cholesterol. Additionally, in vitro release behavior of nanovesicles shows low taxifolin released (3.68-10.13%) at intestinal conditions, whereas more than 90% of taxifolin is released in gastrointestinal conditions. The compatibility between taxifolin and nanovesicles components is confirmed by FTIR. Transmission electron microscopy demonstrates spherical shaped particles around 200 nm. Backscattering profiles variations show the potential application of taxifolin nanovesicles for producing fortified apple juice with excellent physical stability. Practical Applications: Taxifolin is a flavanonol, which fulfills a particular task in preserving stable functions of the circulatory system owing to its special antioxidant ability and biological activity. Nevertheless, its low bioavailability is a salient drawback for biomedical and food applications. Thus, the current study is conducted to encapsulate taxifolin in nanovesicles (such as liposome, niosome, transfersome) by EIM to improve its bioavailability. Nanocarriers with relatively decent physical stability and high encapsulation efficiency can be brought about through Tween 80, soybean lecithin, and in the presence and absence of cholesterol as stabilizer which ensures the successful delivery of taxifolin to food formats such as beverages.

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Nanodispersions of taxifolin: Impact of solid-state properties on dissolution behavior

Cited by 53 publications

References 22 publications

Micronization of Taxifolin by Supercritical Antisolvent Process and Evaluation of Radical Scavenging Activity

Micronization of Taxifolin by Supercritical Antisolvent Process and Evaluation of Radical Scavenging Activity

Sonochemical Micronization of Taxifolin Aimed at Improving Its Bioavailability in Drinks for Athletes

Formulation and Characterization of Taxifolin‐Loaded Lipid Nanovesicles (Liposomes, Niosomes, and Transfersomes) for Beverage Fortification

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