Feng Weiwei, Guo Xinyu, Yang Guang, Yao Yao, Zhao Lixia, Gao Shuang, Ye Fei, Fu Ying
Department of Chemistry, Northeast Agricultural University, Harbin 150030, China.
Department of Chemistry, Northeast Agricultural University, Harbin 150030, China.
Int J Biol Macromol. 2024 Jun;270(Pt 1):132344. doi: 10.1016/j.ijbiomac.2024.132344. Epub 2024 May 14.
Hydroxypropyl-gamma-cyclodextrin (HPγCD) inclusion complex nanofibers (Lut/HPγCD-IC-NF) containing Luteolin (Lut) were prepared by electrospinning technology. Fourier transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD) spectra confirmed the formation of Lut/HPγCD-IC-NF. Scanning electron microscopy (SEM) images showed that the morphology of Lut/HPγCD-IC-NF was uniform and bead-free, suggesting that self-assembled aggregates, macromolecules with higher molecular weights, were formed by strong hydrogen bonding interactions between the cyclodextrin inclusion complexes. Confocal laser scanning microscopy (CLSM) images showed that Lut was distributed in Lut/HPγCD-IC-NF. Proton nuclear magnetic resonance (H NMR) spectroscopy revealed the change in chemical shift of the proton peak between Lut and HPγCD, confirming the formation of inclusion complex. Thermogravimetric analysis (TGA) proved that Lut/HPγCD-IC-NF had good thermal stability. The phase solubility test confirmed that HPγCD had a solubilizing effect on Lut. When the solubility of HPγCD reached 10 mM, the solubility of Lut increased by 15-fold. The drug loading test showed that the content of Lut in fibers reached 8.57 ± 0.02 %. The rapid dissolution experiment showed that Lut/HPγCD-IC-NF dissolved within 3 s. The molecular simulation provides three-dimensional evidence for the formation of inclusion complexes between Lut and HPγCD. Antibacterial experiments showed that Lut/HPγCD-IC-NF had enhanced antibacterial activity against S. aureus. Lut/HPγCD-IC-NF exhibited excellent antioxidant properties with a free radical scavenging ability of 89.5 ± 1.1 %. In vitro release experiments showed Lut/HPγCD-IC-NF had a higher release amount of Lut. In conclusion, Lut/HPγCD-IC-NF improved the physicochemical properties and bioavailability of Lut, providing potential applications of Lut in the pharmaceutical field.
采用静电纺丝技术制备了含木犀草素（Lut）的羟丙基 - γ - 环糊精（HPγCD）包合物纳米纤维（Lut/HPγCD - IC - NF）。傅里叶变换红外（FTIR）光谱和X射线衍射（XRD）光谱证实了Lut/HPγCD - IC - NF的形成。扫描电子显微镜（SEM）图像显示Lut/HPγCD - IC - NF的形态均匀且无珠，表明通过环糊精包合物之间强烈的氢键相互作用形成了自组装聚集体，即分子量更高的大分子。共聚焦激光扫描显微镜（CLSM）图像显示Lut分布在Lut/HPγCD - IC - NF中。质子核磁共振（H NMR）光谱揭示了Lut与HPγCD之间质子峰化学位移的变化，证实了包合物的形成。热重分析（TGA）证明Lut/HPγCD - IC - NF具有良好的热稳定性。相溶解度试验证实HPγCD对Lut具有增溶作用。当HPγCD的溶解度达到10 mM时，Lut的溶解度增加了15倍。载药试验表明纤维中Lut的含量达到8.57±0.02%。快速溶解实验表明Lut/HPγCD - IC - NF在3秒内溶解。分子模拟为Lut与HPγCD之间包合物的形成提供了三维证据。抗菌实验表明Lut/HPγCD - IC - NF对金黄色葡萄球菌具有增强的抗菌活性。Lut/HPγCD - IC - NF表现出优异的抗氧化性能，自由基清除能力为89.5±1.1%。体外释放实验表明Lut/HPγCD - IC - NF具有更高的Lut释放量。总之，Lut/HPγCD - IC - NF改善了Lut的理化性质和生物利用度，为Lut在制药领域的潜在应用提供了可能。
