Bin Jardan Yousef A, Ahad Abdul, Raish Mohammad, Al-Mohizea Abdullah M, Al-Jenoobi Fahad I
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Pharmaceuticals (Basel). 2023 Nov 22;16(12):1641. doi: 10.3390/ph16121641.
Pterostilbene (PTS) is a naturally occurring phytoalexin. PTS displays limited water solubility, which consequently results in its diminished oral bioavailability. Therefore, a ternary inclusion complex (TIC) of PTS with β-cyclodextrin (βCD) in the presence of ternary substance Pluronic F-127 (PLF) was prepared using microwave technology. The PTS-TIC was characterized by dissolution performance. Further, the prepared TIC was characterized by DSC, FTIR, NMR, XRD, and SEM analysis. Additionally, the antioxidant activity of PTS and PTS-TIC was also evaluated. Phase-solubility studies revealed that PTS's solubility in water was increased by 6.72 times when βCD/PLF was present. In comparison with PTS, prepared PTS-TIC produced a considerable improvement in PTS release. After 1 h, 74.03 ± 4.47% of PTS was released from PTS-TIC. Outcomes of DSC, FTIR, NMR, XRD, and SEM analysis revealed that the PTS was enclosed in the βCD cavity. In terms of antioxidant properties, the PTS-TIC formulation demonstrated superior activity compared to PTS, possibly attributed to the improved solubility of PTS resulting from the formation of TIC using microwave technology. It was concluded that microwave technology proved to be an extremely beneficial means of interacting PTS with βCD. In addition to increasing the solubility of PTS, the findings are also expected to improve its bioavailability by increasing its solubility. As a result, this study could provide insight into potential methods for enhancing the solubility of polyphenolic substances like PTS.
紫檀芪（PTS）是一种天然存在的植物抗毒素。PTS的水溶性有限，因此导致其口服生物利用度降低。因此，采用微波技术制备了PTS与β-环糊精（βCD）在三元物质普朗尼克F-127（PLF）存在下的三元包合物（TIC）。通过溶出性能对PTS-TIC进行了表征。此外，还通过差示扫描量热法（DSC）、傅里叶变换红外光谱法（FTIR）、核磁共振法（NMR）、X射线衍射法（XRD）和扫描电子显微镜法（SEM）对制备的TIC进行了表征。此外，还评估了PTS和PTS-TIC的抗氧化活性。相溶解度研究表明，当存在βCD/PLF时，PTS在水中的溶解度提高了6.72倍。与PTS相比，制备的PTS-TIC在PTS释放方面有显著改善。1小时后，74.03±4.47%的PTS从PTS-TIC中释放出来。DSC、FTIR、NMR、XRD和SEM分析结果表明，PTS被包封在βCD腔内。在抗氧化性能方面，PTS-TIC制剂表现出优于PTS的活性，这可能归因于使用微波技术形成TIC后PTS溶解度的提高。得出的结论是，微波技术被证明是使PTS与βCD相互作用的极其有益的手段。除了提高PTS的溶解度外，这些发现还有望通过提高其溶解度来提高其生物利用度。因此，本研究可以为提高PTS等多酚类物质溶解度的潜在方法提供见解。
