Bessarabov Volodymyr, Lisovyi Vadym, Lyzhniuk Viktoriia, Kostiuk Viktor, Smishko Roman, Yaremenko Volodymyr, Goy Andriy, Derkach Tetiana, Kuzmina Galina, Gureyeva Svitlana
Kyiv National University of Technologies and Design, 2 Mala Shyianovska Str., Kyiv, 01011, Ukraine.
L. M. Litvinenko Institute of Physical-Organic Chemistry and Coal Chemistry, National Academy of Sciences of Ukraine, 50 Kharkivske shose Str., Kyiv, 02155, Ukraine.
Heliyon. 2025 Feb 14;11(4):e42702. doi: 10.1016/j.heliyon.2025.e42702. eCollection 2025 Feb 28.
The flavonoid hesperidin is a crucial, biologically active substance of great interest because of its polypharmacological properties and high safety profile. However, its widespread use of this bioflavonoid in remedies for the treatment and prevention of various diseases is limited by its low water solubility. This study reports on solid dispersed systems (SDSs) of hesperidin, fabricated for the first time via the method of centrifugal fibre. For one of the compositions of these SDSs, the solubility of the flavonoid in water is observed to be 150-170 times higher than that of the pure compound. Polyvinylpyrrolidones, with different molecular weights, was used as a fibre-forming polymer carrier, alongside sucrose and mannitol as auxiliary substances to enhance the yield of the composites. The SDSs of hesperidin in the form of fibres were characterised via differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR) and powder X-ray diffraction (PXRD). DSC and PXRD results confirmed the amorphisation of hesperidin in the fibrous SDSs. FTIR results confirmed that the interaction of hesperidin with the components of the SDS composites occurs due to the formation of intermolecular hydrogen bonds. Studies of in vitro release kinetics in buffer media with pH = 1.2, 4.5 and 6.8 showed that the release rate of hesperidin from the centrifugally formed SDSs is considerably higher than the dissolution rate of pure hesperidin. Thus, the results of this study confirm that centrifugal fibre formation is a simple and effective method for fabricating highly soluble SDSs of hesperidin.
黄酮类化合物橙皮苷是一种至关重要的生物活性物质,因其具有多种药理特性和高安全性而备受关注。然而,这种生物黄酮在治疗和预防各种疾病的药物中的广泛应用受到其低水溶性的限制。本研究报道了首次通过离心纤维法制备的橙皮苷固体分散体(SDSs)。对于这些SDSs的一种组合物,观察到该黄酮类化合物在水中的溶解度比纯化合物高150 - 170倍。使用不同分子量的聚乙烯吡咯烷酮作为成纤聚合物载体,同时使用蔗糖和甘露醇作为辅助物质以提高复合材料的产率。通过差示扫描量热法(DSC)、傅里叶变换红外光谱法(FTIR)和粉末X射线衍射法(PXRD)对纤维形式的橙皮苷SDSs进行了表征。DSC和PXRD结果证实了纤维状SDSs中橙皮苷的非晶化。FTIR结果证实,橙皮苷与SDS复合材料的组分之间的相互作用是由于分子间氢键的形成而发生的。在pH = 1.2、4.5和6.8的缓冲介质中的体外释放动力学研究表明,离心形成的SDSs中橙皮苷的释放速率明显高于纯橙皮苷的溶解速率。因此,本研究结果证实离心纤维形成是制备高溶性橙皮苷SDSs的一种简单有效的方法。