Sustained-Release Solid Dispersion of High-Melting-Point and Insoluble Resveratrol Prepared through Hot Melt Extrusion to Improve Its Solubility and Bioavailability
| العنوان: | Sustained-Release Solid Dispersion of High-Melting-Point and Insoluble Resveratrol Prepared through Hot Melt Extrusion to Improve Its Solubility and Bioavailability |
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| المؤلفون: | Wenling Fan, Xiaotong Zhang, Meiqi Gao, Wenjing Zhu |
| المصدر: | Molecules Volume 26 Issue 16 Molecules, Vol 26, Iss 4982, p 4982 (2021) |
| بيانات النشر: | MDPI AG, 2021. |
| سنة النشر: | 2021 |
| مصطلحات موضوعية: | Hot Temperature, Materials science, Scanning electron microscope, dissolution, Biological Availability, Pharmaceutical Science, resveratrol, Article, hot melt extrusion, Polyethylene Glycols, Analytical Chemistry, QD241-441, Differential scanning calorimetry, Drug Discovery, sustained-release, Physical and Theoretical Chemistry, Solubility, Dissolution, solid dispersion, Drug Carriers, Organic Chemistry, Hot Melt Extrusion Technology, Amorphous solid, Chemical engineering, Chemistry (miscellaneous), Delayed-Action Preparations, Melting point, Molecular Medicine, Extrusion, Dispersion (chemistry), Hydrophobic and Hydrophilic Interactions |
| الوصف: | This study aimed to prepare a sustained-release solid dispersion of poorly water-soluble resveratrol (RES) with high melting point in a single hot melt extrusion step. A hydrophobic–hydrophilic polymeric blend (Eudragit RS and PEG6000) was used to control the release of RES. With the dispersive mixing and high shear forces of hot melt extrusion, the thermodynamic properties and dispersion of RES were changed to improve its solubility. The effects of the formulation were investigated through univariate analysis to optimize the preparation of the sustained-release solid dispersion. In vitro and in vivo studies were performed to evaluate the prepared RES/RS/PEG6000 sustained-release solid dispersion. The physical state of the solid dispersion was characterized using differential scanning calorimetry and X-ray diffraction. Surface properties of the dispersion were visualized using scanning electron microscopy, and the chemical interaction between RES and excipients was detected through Fourier-transform infrared spectroscopy. Results suggested that the optimized sustained-release solid dispersion was obtained when the mass ratio of RES-polymeric blend was 1:5, the ratio of PEG6000 was 35%, the barrel temperature was 170 °C, and the screw speed was 80 rpm. In vitro studies demonstrated that the solid dispersion showed a good sustained release effect. The cumulative release of RES reached 82.42% until 12 h and was fit by the Weibull model. In addition, the saturated solubility was 2.28 times higher than that of the bulk RES. In vitro studies demonstrated that the half-life increased from 3.78 to 7.09 h, and the bioavailability improved to 140.38%. The crystalline RES was transformed into the amorphous one, and RES was highly dispersed in the polymeric blend matrix. |
| وصف الملف: | application/pdf |
| تدمد: | 1420-3049 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fd1c78e4b5325126708fb3cb4285135Test https://doi.org/10.3390/molecules26164982Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....1fd1c78e4b5325126708fb3cb4285135 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 14203049 |
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