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Cocrystal of phloretin with isoniazid: preparation, characterization, and evaluation.

ABSTRACT: Phloretin (Phl) is a natural flavonoid compound with wide range of biological activities but demonstrates poor water solubility and limited pharmacological effects. In this study, one cocrystal of phloretin-isoniazid (Phl-Inz) was prepared successfully using the solvent evaporation method. The physical properties of cocrystal were characterized by differential scanning calorimetry (DSC), thermogravimetric analysis (TG), powder X-ray diffraction (PXRD), Fourier-transform infrared (FT-IR) and single crystal X-ray diffraction (SCXRD). The Hirshfeld surface analysis explained further interactions in the cocrystal. The solubility test showed that the solubility of the cocrystal was increased at pH 1.2 and pH 6.8 compared to that of the pure drug. The test in vitro simulated gastrointestinal digestion showed that the release of phloretin in the cocrystal was better than that in the pure phloretin. The results of the DPPH and ABTS scavenging activity showed that the in vitro antioxidant activity of the cocrystal was improved. The anticancer assay exhibited improved cytotoxicity in the Phl-Inz cocrystal as compared with the pure Phl.

SUBMITTER: Lu Z

PROVIDER: S-EPMC10077513 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature

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Cocrystal of phloretin with isoniazid: preparation, characterization, and evaluation.

Lu Zhongyu Z Chen Hankun H Mo Jiaxin J Yuan Xiaohong X Wang Dawei D Zheng Xianhui X Zhu Wei W

RSC advances 20230406 16

Phloretin (Phl) is a natural flavonoid compound with wide range of biological activities but demonstrates poor water solubility and limited pharmacological effects. In this study, one cocrystal of phloretin-isoniazid (Phl-Inz) was prepared successfully using the solvent evaporation method. The physical properties of cocrystal were characterized by differential scanning calorimetry (DSC), thermogravimetric analysis (TG), powder X-ray diffraction (PXRD), Fourier-transform infrared (FT-IR) and sing ...[more]

PMID: 37033443

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Project description:BackgroundPhloretin (Phl) is a flavonoid compound that contains multiple phenolic hydroxyl groups. It is found in many plants, such as apple leaves, lychee pericarp, and begonia, and has various biological activities, such as antioxidant and anticancer effects. The strong hydrogen bonding between Phl molecules results in poor water solubility and low bioavailability, and thus the scope of the clinical application of Phl is limited. Therefore, it is particularly important to improve the water solubility of Phl for its use to further combat or alleviate skin aging and oxidative damage and develop antioxidant products for the skin. The purpose of this study was to develop and evaluate a phloretin transfersome gel (PTG) preparation for transdermal drug delivery to improve the bioavailability of the drug and delay aging.MethodsPhloretin transfersomes (Phl-TFs) were prepared and optimized by the thin-film dispersion-ultrasonication method. Phl-TFs were characterized by transmission electron microscopy (TEM), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD). The Log P method was used to determine the solubility of the Phl-TFs. The skin penetration ability of the prepared PTG was evaluated using the Franz diffusion cell method. In addition, the in vivo pharmacokinetics of PTG were studied in rats, and an antioxidant activity investigation was conducted using a D-gal rat model.ResultsPhl-TFs were successfully prepared with a Soybean Phosphatidylcholine (SPC)/CHOL ratio of 2.7:1 w/v, a phloretin concentration of 1.3 mg/mL, a hydration time of 46 min, an ultrasound time of 5 min, and an ultrasound power of 180 W. The Log P was 2.26, which was significantly higher than that of phloretin (p < 0.05, paired t test). The results of the in vitro penetration test demonstrated that the cumulative skin penetration of the Phl-TFs after 24 h was 842.73 ± 20.86 μg/cm2. The data from an in vivo pharmacokinetic study showed that the Cmax and AUC of PTG were 1.39- and 1.97-fold higher than those of the phloretin solution gel (PSG), respectively (p < 0.05, paired t test). The experimental results in aging rats showed that PTG had a better antioxidant effect.ConclusionsPhl-TFs and PTG preparations with a good shape, safety, and stability were successfully prepared. In vivo pharmacokinetics and preliminary antioxidant experiments further verified the transdermal penetration and antioxidant activity of the phloretin transdermal drug delivery preparation, providing an experimental basis for its further development.

Dataset Information

Cocrystal of phloretin with isoniazid: preparation, characterization, and evaluation.

Publications

Cocrystal of phloretin with isoniazid: preparation, characterization, and evaluation.

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