纤维素纳米晶体提升柚皮素抗氧化活性的研究

柚皮素是一种黄酮类化合物,具有广泛的药理活性,具有抗炎、抗氧化、抗癌、降血脂等药理作用。然而,柚皮素在水中溶解性能差,生物利用度低,限制了其在临床中的应用。本研究以纤维素纳米晶体(Cellulose nanocrystals,CNCs)为载体,以柚皮素为疏水药物模型,利用反溶剂重结晶法成功制备了CNCs/柚皮素纳米复合物,并表征了所得纳米复合物的性能,分析了纳米复合物中柚皮素的溶出性能和抗氧化活性。结果表明,形成CNCs/柚皮素纳米复合物后,柚皮素得到充分的纳米化和稳定分散,从结晶态转变为无定型态。负载CNCs的柚皮素在水中的溶出性能得到显著提升,120min时累积溶出度达到93.4%;经CNCs负载后,当柚皮素浓度为50μg/mL时,羟基自由基清除率达44.3%,柚皮素的体外抗氧化活性显著提高。

Cellulose Nanocrystals as Carriers for Hydrophobic Naringenin to Enhance Its Anti-oxidation Activity

As a typical flavonoid, naringenin exhibits attractive pharmacological activities, including anti-inflammatory, anti-oxidation, anti-cancer properties, and lowering lipids. However, due to its poor water solubility and low bioavailability in aqueous solutions, the pharmaceutical application of naringenin is very limited. In this study, cellulose nanocrystals (CNCs) were used as carriers for naringenin, and the CNCs/naringenin nanocomposite was prepared based on anti-solvent recrystallization method. The CNCs/naringenin nanocomposite was characterized and its dissolution and anti-oxidation activity in aqueous systems were investigated. The results showed that naringenin was effectively nanolized and well dispersed, as well as transformed from crystalline state to amorphous state in aqueous system based on the formation of CNCs/naringenin nanocomposite. The cumulative dissolution of naringenin in CNCs/naringenin nanocomposite obviously increased to 93.4% at 120 min. Furthermore, the in vitro anti-oxidation activity of naringenin was clearly enhanced based on the formation of CNCs/naringenin nanocomposite. The above results supported the conclusion that the use of CNCs as nanocarriers for naringenin was a promising technique to improve the bioavailability of naringenin in aqueous systems.