Cocrystals of quercetin: synthesis, characterization, and screening of biological activity

Veverka, Miroslav; Dubaj, Tibor; Gallovič, Ján; Jorı́k, Vladimı́r; Veverková, Eva; Danihelová, Martina; Šimon, Peter

doi:10.1007/s00706-014-1314-6

Cited by 32 publications

(31 citation statements)

References 37 publications

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“…This result suggests that there is no interaction between Qu and Ma in the physical mixture. On the other hand, the diffractogram of Co Qu-Ma showed new diffraction peaks at 9.81, 12.99, and 19.80° which are not identified in the diffractogram of pure components or physical mixture, this result indicates the successful formation of Co Qu-Ma [2,7,9,[14][15].…”

Section: Powder X-ray Diffractionmentioning

confidence: 78%

“…Furthermore, the formation of new crystal lattice in cocrystallization product was clarified using powder Xray diffraction analysis. The formation of cocrystal is confirmed by the appearance of new peak in the diffractogram [2,7,9,11,14]. The large number of sharp and specific peaks shown by Qu and Ma indicates the unique crystalline form of these compounds [9,15].…”

Section: Powder X-ray Diffractionmentioning

confidence: 84%

“…The formation of cocrystal is confirmed by the appearance of new peak in the diffractogram [2,7,9,11,14]. The large number of sharp and specific peaks shown by Qu and Ma indicates the unique crystalline form of these compounds [9,15]. The diffractogram of the physical mixture showed a superposition of diffraction peaks of the components compared to the original Qu as well as Ma.…”

Section: Powder X-ray Diffractionmentioning

confidence: 87%

“…The thermogram of Co Qu-Ma showed an endothermic peak at 277.9 °C which is higher when compared to that of Ma and is lower when compared to that of Qu. The shifting of the melting point indicates the possible interaction between components to form cocrystals [2,9,11,14]. One of the parameter used to The appearance of new melting point positioned between the melting points of cocrystals components may clarify the cocrystals formation.…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

“…It has been reported that quercetin cocrystals were successfully produced using several coformers such as caffeine, isonicotinamide and theobromine. Previous finding showed that cocrystallization with caffeine increased water solubility of quercetin up to 8 times compared to the pure quercetin [8][9][10][11][12][13]. Nevertheless, none has been reported for the cocrystallization of quercetin with malonic acid as coformer.…”

Section: Introductionmentioning

confidence: 99%

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Improvement <i>in vitro</i> Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

et al. 2018

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The aim of the study was to improve the in-vitro dissolution rate of quercetin (Qu) using cocrystallization of quercetin. Cocrystals of quercetin (Co Qu) were produced with malonic acid (Ma) as coformer at ratio 1:2 using solvent evaporation method. Cocrystals quercetin-malonic acid (Co Qu-Ma) was characterized using Differential Thermal Analysis (DTA), Powder X-Ray Diffraction (PXRD), Scanning Electron Microscope (SEM), and Fourier Transforms Infrared Spectrophotometer (FTIR) and in-vitro dissolution study. A new endothermic peak at 277.9 °C was shown from the thermogram. Diffractogram of Co Qu-Ma showed a new diffraction peak at 2θ 9.81, 12.99, and 19.80°. Microphotograph showed that Qu and Ma exhibited a columnar-shaped and a pebble-shaped crystal, respectively, and FTIR wavenumber of O-H functional group of quercetin was shifted from its original position at 3411 to 3428 cm-1 in the physical mixture (pm) of Qu-Ma and 3418 cm-1 in Co Qu-Ma, respectively. The physicochemical characterizations using DTA, PXRD, SEM and FTIR indicated that Co Qu-Ma were successfully obtained through solvent evaporation method. The in-vitro dissolution rate of Co Qu-Ma was 95.30% at 60 min. Cocrystals effectively increased dissolution rate and dissolution efficiency in comparison to the pure quercetin and physical mixture of quercetin-malonic acid.

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Section: Powder X-ray Diffractionmentioning

confidence: 78%

Section: Powder X-ray Diffractionmentioning

confidence: 84%

Section: Powder X-ray Diffractionmentioning

confidence: 87%

Section: In Vitro Dissolution Studymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Improvement <i>in vitro</i> Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

et al. 2018

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Cocrystallization for Improving Anticancer Activity of Drugs

Alvani,

Shayanfar

2024

Cryst. Res. Technol.

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Cocrystallization can change the physicochemical and pharmacokinetic properties of active pharmaceutical ingredients (API) and improve biological activities. This study focuses on the documented biological activities of APIs in cocrystal form, specifically those with anticancer properties. Additionally, the mechanisms by which these APIs exhibit modified anticancer effects are discussed. Generally, this technique can change anticancer activity through solubilization, enhancing dissolution rate, permeability improvement, stabilization, producing a slow‐release form, and retaining transient in solution and interaction with receptors.

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Crystal engineering as a scientific basis for modification of physicochemical properties of bioflavonoids

Селиванова

Terekhov

2019

Russ Chem Bull

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Cocrystals of quercetin: synthesis, characterization, and screening of biological activity

Cited by 32 publications

References 37 publications

Improvement <i>in vitro</i> Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

Improvement <i>in vitro</i> Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

Cocrystallization for Improving Anticancer Activity of Drugs

Crystal engineering as a scientific basis for modification of physicochemical properties of bioflavonoids

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