Enhanced solubility of quercetin by forming composite particles with transglycosylated materials

Fujimori, Miki; Kadota, Kazunori; Shimono, Keisuke; Shirakawa, Yoshiyuki; Sato, Hideyuki; Tozuka, Yuichi

doi:10.1016/j.jfoodeng.2014.10.010

Cited by 50 publications

(22 citation statements)

References 37 publications

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“…This average C MAX value is 12.7-fold higher than the average C MAX value attained by crystalline Q (6.16 µg/mL). The degrees of enhancement of Q solution concentrations achieved are comparable to those achieved from different amorphous matrices by others (Fujimori et al, 2015) and in our previous work (Li et al, 2013). Blending with the miscible and hydrophilic PVP enhanced Q release from both CCAB and CASub as anticipated.…”

Section: Simulated Small Intestinal Conditions (Ph = 68)supporting

confidence: 88%

Novel cellulose-based amorphous solid dispersions enhance quercetin solution concentrations in vitro

Gilley

Arca

Nichols

et al. 2017

Carbohydrate Polymers

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Quercetin (Q) is a bioactive flavonol with potential to benefit human health. However, Q bioavailability is relatively low, due to its poor aqueous solubility and extensive phase-II metabolism. Strategies to increase solution concentrations in the small intestinal lumen have the potential to substantially increase Q bioavailability, and by extension, efficacy. We aimed to achieve this by incorporating Q into amorphous solid dispersions (ASDs) with cellulose derivatives. Q was dispersed in matrices of cellulose esters including 6-carboxycellulose acetate butyrate (CCAB), hydroxypropylmethylcellulose acetate succinate (HPMCAS) and cellulose acetate suberate (CASub) to afford ASDs that provided stability against crystallization, and pH-triggered release. Blends of CASub and CCAB with the hydrophilic polyvinylpyrrolidone (PVP) further enhanced dissolution. The ASD 10% Q:20% PVP:70% CASub most significantly enhanced Q solution concentration under intestinal pH conditions, increasing area under the concentration/time curve (AUC) 18-fold compared to Q alone. This novel ASD method promises to enhance Q bioavailability in vivo.

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Section: Simulated Small Intestinal Conditions (Ph = 68)supporting

confidence: 88%

Novel cellulose-based amorphous solid dispersions enhance quercetin solution concentrations in vitro

Gilley

Arca

Nichols

et al. 2017

Carbohydrate Polymers

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“…It was revealed that different affinities among the drug and the aggregated nanostructures led to increased solubility, which may explain the enhanced dissolution of MC-SDP. 46…”

Section: X-ray Diffraction Analysismentioning

confidence: 99%

<p>Characterization and Dissolution Study of Micellar Curcumin-Spray Dried Powder for Oral Delivery</p>

Wijiani¹,

Isadiartuti²,

Rijal³

et al. 2020

IJN

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Introduction: Curcumin faces a major challenge in clinical use due to its poor aqueous solubility, which affects its bioavailability over oral use. The present study was carried out to overcome this problem. Methods: An amorphous micellar curcumin-spray dried powder (MC-SDP) with selfassembled casein was prepared by the addition of sucrose as a protectant. The dry powder of curcumin-loaded micelles was obtained by a spray-drying technique in the presence of sucrose as a protectant. The MC-SDP in the form of dry powder was further developed into tablets to investigate the dissolution profile. The physical properties of preformed powder were characterized by differential thermal analysis (DTA), X-ray diffraction (XRD), and scanning electron microscopy (SEM). Quantitative analysis in the form of solutions was analyzed by high-performance liquid chromatography (HPLC). Results: The physical properties demonstrated that MC-SDP varies from dented to smoother surfaces as a function of sucrose. Furthermore, melting transitions of curcumin in the form of MC-SDP were broadened in all sample mixtures, as observed in the DTA thermogram. The XRD spectra showed that the sharp and very intense peaks of single curcumin crystalline structure no longer existed in all MC-SDP forms, indicating that the mixtures were amorphous. Moreover, a further dissolution study of MC-SDP showed a significant increase of drug dissolved with the presence of sucrose, where >80% of curcumin from MC-SDP was dissolved within 30 min. Conclusion: The study demonstrated the manufacture of micellar spray-dried powder that would contribute to the development of oral delivery of curcumin.

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“…Our recent studies revealed that the specific properties of transglycosylated compounds, including transglycosylated hesperidin (hesperidin-G), transglycosylated stevia (stevia-G), and transglycosylated rutin (rutin-G), can be employed as effective excipients to prepare solubilized formulations of poorly water-soluble materials Tozuka et al, 2010;Uchiyama et al, 2010). Indeed, we have successfully enhanced the nutraceutical functions of food materials with low water solubility such as quercetin, ipriflavone, and sesamin (Fujimori et al, 2015(Fujimori et al, , 2016Sato et al, 2017). To implement the practical use of this technology in the food industry, a further reduction in the amount of the excipient is desired.…”

Section: Introductionmentioning

confidence: 99%

Preparation of a Highly Water-dispersible Powder Containing Hydrophobic Polyphenols Derived from Chrysanthemum Flower with Xanthine Oxidase-inhibitory Activity

Kadota

Hashimoto

Yamaguchi

et al. 2018

FSTR

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We aimed to develop a highly water-dispersible dry powder of hydrophobic polyphenols derived from chrysanthemum flower. A dry powder resulting from the mixture of an ethanolic extract of chrysanthemum flower (CF) with transglycosylated rutin (rutin-G) and sucrose fatty acid esters (SEs) was successfully formulated. This powder dispersed easily in water, and the mean particle size in water remained at ~150 nm without apparent changes even after one-week storage. Furthermore, the particle size of the dispersed powder prepared by heat-and-acid treatment shifted below 100 nm after one-week storage. The xanthine oxidase-inhibitory activity of the resulting CF-rutin-G-SEs powder was almost equivalent to that of chrysanthemum flower oil according to in vitro analysis. This technique for preparing a highly water-dispersible dry powder from natural products containing hydrophobic polyphenols should be applicable to the development of functional food products.

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Enhanced solubility of quercetin by forming composite particles with transglycosylated materials

Cited by 50 publications

References 37 publications

Novel cellulose-based amorphous solid dispersions enhance quercetin solution concentrations in vitro

Novel cellulose-based amorphous solid dispersions enhance quercetin solution concentrations in vitro

<p>Characterization and Dissolution Study of Micellar Curcumin-Spray Dried Powder for Oral Delivery</p>

Preparation of a Highly Water-dispersible Powder Containing Hydrophobic Polyphenols Derived from Chrysanthemum Flower with Xanthine Oxidase-inhibitory Activity

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