Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion

Ishimoto, Kenji; Shimada, Yukiko; Ohno, Akane; Otani, Shuichi; Ago, Yukio; Maeda, Soya; Lin, Bangzhong; Nunomura, Kazuto; Hino, Nobumasa; Suzuki, Masayuki; Nakagawa, Shinsaku

doi:10.3389/fnut.2022.850103

Cited by 12 publications

(6 citation statements)

References 46 publications

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“…The amorphous state of polyphenols is most often stabilized by hydrogen bonds. Recent work shows the amorphous solid dispersion of such polyphenols as quercetin [11,16,17], resveratrol [18], curcumin [18][19][20], naringenin [21], daidzein [22], and genistein [23]. The amorphous form of pterostilbene was obtained, for example, by Tzeng et al via nanoprecipitation with Eudragit ® e100 and polyvinyl alcohol (PVA) [24].…”

Section: Introductionmentioning

confidence: 99%

Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

2023

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The aim of our research was to improve the solubility and antioxidant activity of pterostilbene (PTR) by developing a novel amorphous solid dispersion (ASD) with Soluplus® (SOL). DSC analysis and mathematical models were used to select the three appropriate PTR and SOL weight ratios. The amorphization process was carried out by a low-cost and green approach involving dry milling. An XRPD analysis confirmed the full amorphization of systems in 1:2 and 1:5 weight ratios. One glass transition (Tg) observed in DSC thermograms confirmed the complete miscibility of the systems. The mathematical models indicated strong heteronuclear interactions. SEM micrographs suggest dispersed PTR within the SOL matrix and a lack of PTR crystallinity, and showed that after the amorphization process, PTR-SOL systems had a smaller particle size and larger surface area compared with PTR and SOL. An FT-IR analysis confirmed that hydrogen bonds were responsible for stabilizing the amorphous dispersion. HPLC studies showed no decomposition of PTR after the milling process. PTR’s apparent solubility and antioxidant activity after introduction into ASD increased compared to the pure compound. The amorphization process improved the apparent solubility by ~37-fold and ~28-fold for PTR-SOL, 1:2 and 1:5 w/w, respectively. The PTR-SOL 1:2 w/w system was preferred due to it having the best solubility and antioxidant activity (ABTS: IC50 of 56.389 ± 0.151 µg·mL−1 and CUPRAC: IC0.5 of 82.52 ± 0.88 µg·mL−1).

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Section: Introductionmentioning

confidence: 99%

Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

2023

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“…These methods allow for achieving a molecularlevel dispersion of polyphenols within the matrix, creating a highly homogeneous and amorphous system. In recent years, it has been demonstrated that compounds such as sinapic acid [18], resveratrol [17], pterostilbene [10], curcumin [17,20,21], hesperidin [9,22], daidzein [16], genistein [19,23], hesperetin [12,22], naringenin [24], and quercetin [25][26][27] can be can be formulated using ASD. To date, no ASDs of KMP have been reported.…”

Section: Introductionmentioning

confidence: 99%

The Study of Amorphous Kaempferol Dispersions Involving FT-IR Spectroscopy

Rosiak,

Tykarska,

Cielecka-Piontek

2023

IJMS

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Attenuated total reflection-Mid-Fourier transform-infrared (ATR-Mid-FT-IR) spectroscopy combined with principal component analysis (PCA) has been applied for the discrimination of amorphous solid dispersion (ASD) of kaempferol with different types of Eudragit (L100, L100-55, EPO). The ASD samples were prepared by ball milling. Training and test sets for PCA consisted of a pure compound, physical mixture, and incomplete/complete amorphous solid dispersion. The obtained results confirmed that the range 400–1700 cm−1 was the major contributor to the variance described by PC1 and PC2, which are the fingerprint region. The obtained PCA model selected fully amorphous samples as follows: five for KMP-EL100, two for KMP-EL100-55, and six for KMP-EPO (which was confirmed by the XRPD analysis). DSC analysis confirmed full miscibility of all ASDs (one glass transition temperature). FT-IR analysis confirmed the formation of hydrogen bonds between the –OH and/or –CH groups of KMP and the C=O group of Eudragits. Amorphization improved the solubility of kaempferol in pH 6.8, pH 5.5, and HCl 0.1 N.

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“…Female BALB/c mice were obtained from Japan SLC Inc. (Shizuoka, Japan) and acclimatized under controlled environmental conditions (22 ± 1°C; 50% ± 10% relative humidity; 12-h light-dark cycle; lights on at 08:00 AM) for some days before the start of the experiment. All animals were fed with normal powdered food (MF, Oriental Yeast Co. Ltd., Tokyo, Japan) and had ad libitum access to water [18]. TFM, TFM-lc, and TF1 were each prepared by mixing with powdered food at a concentration of 0.02-0.20% and administration was started 2 weeks prior to OVA sensitization.…”

Section: Animalsmentioning

confidence: 99%

Suppressive effect of black tea polyphenol theaflavins in a mouse model of ovalbumin-induced food allergy

et al. 2023

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Food allergy is recognized as a global medical problem with increasing prevalence in recent years. Currently, the treatment of food allergy mainly involves avoidance of allergens and allergen-specific immunotherapy. Barring the spontaneous resolution of food allergy during the growth process, this disease is difficult to treat fundamentally. In recent years, the use of functional food ingredients derived from natural products has been attracting attention for their prophylactic use in food allergy. Theaflavins, i.e. black tea polyphenols, are potent antioxidants that have inhibitory effects on a variety of diseases. However, little is known about the preventive effect of theaflavins on food allergy. In this study, we designed a mouse model of food allergy and examined the effect of theaflavins using the severity of diarrhea, a symptom of food allergy, as an indicator. The administration of a black tea extract rich in theaflavins or theaflavin 1 (subgroup of theaflavins) to mice reduced the severity of diarrhea when compared with a normal diet. A reduction in malondialdehyde levels, a key marker of lipid peroxidation, was also observed. Overall, these data suggest that theaflavins may potentially inhibit food allergy by alleviating oxidative stress in the colon and can be a potential food material for prevention of food allergy.

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Physicochemical and Biochemical Evaluation of Amorphous Solid Dispersion of Naringenin Prepared Using Hot-Melt Extrusion

Cited by 12 publications

References 46 publications

Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

Amorphous Pterostilbene Delivery Systems Preparation—Innovative Approach to Preparation Optimization

The Study of Amorphous Kaempferol Dispersions Involving FT-IR Spectroscopy

Suppressive effect of black tea polyphenol theaflavins in a mouse model of ovalbumin-induced food allergy

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