肠溶性白藜芦醇电纺纤维的制备、性能及其体外抗氧化活性

Preparation,Characterization and in Vitro Antioxidant Activity of Resveratrol-Loaded Enteric Electrospun Fibers

目的:利用静电纺丝技术制备负载白藜芦醇(resveratrol,Res)的具有稳定抗氧化活性的电纺纤维,提高Res的水溶性和热稳定性,促进Res在模拟肠液中的释放。方法:探讨电纺前驱液中聚乙烯吡咯烷酮(polyvinyl pyrrolidone,PVP)、羟丙基-β-环糊精(hydroxypropyl-beta-cyclodextrin,HB-β-CD)添加量和Res的投料比(占固形物总质量的比例)对电纺纤维形貌特征的影响,确定Res电纺纤维的优化配方,并以水杨酸(salicylic acid,SA)为敏感剂制备肠溶性Res电纺纤维(SA/NFs-Res),利用扫描电子显微镜、傅里叶变换红外光谱、差示扫描量热等技术对其性能进行表征,研究其水溶性、抗氧化活性以及在模拟生理条件下的释放效果。结果:Res电纺纤维的优化配方为PVP 2.00 g、HB-β-CD 1.00 g和Res的投料比10.00%,制备的SA/NFs-Res中Res的包封率为96.32%,负载率为9.63%,水中溶解度为18.88 mg/mL,溶解度较纯Res提高近630倍;SA/NFs-Res为表面光滑的纳米纤维结构,热力学性质稳定,抗氧化能力与纯Res一致;SA/NFs-Res具有一定的pH值敏感性,能在模拟胃液中缓慢释放,而在模拟肠液中实现快速释放。结论:通过静电纺丝技术制备的SA/NFs-Res具有提高Res的水溶性和稳定性、保持Res的抗氧化能力和促进Res在模拟肠液中快速释放的作用,有利于其在功能食品、保健品和药物运输载体方面的应用。

Objective:The electrostatic spinning technique was used to prepare resveratrol(Res)-loaded electrospinning fibers with stable antioxidant activity in order to improve the water solubility,thermal stability,and release of resveratrol in simulated intestinal juice.Methods:The effect of the concentration of polyvinyl pyrrolidone(PVP)and HB-β-CD in electrospinning precursor solution and the proportion of Res in the total amount of solids on the morphological characteristics of electrostatic spinning fibers was studied,and the formulation was optimized.Then,enteric resveratrol-loaded electrospinning fibers(SA/NFs-Res)were prepared with salicylic acid as a sensitive agent and were characterized by scanning electron microscopy(SEM),Fourier transform infrared(FTIR)spectroscopy and differential scanning calorimetry(DSC).Subsequently,the water solubility,antioxidant activity and release behavior of SA/NFs-Res under different pH conditions were also investigated.Results:The optimal formulation was found to contain 2.00 g of PVP,1.00 g of HB-β-CD and 10.00%of Res.The envelopment rate of Res in the resulting SA/NFs-Res was 96.32%,the loading rate of Res was 9.63%,and water solubility was 18.88 mg/mL,which was nearly 630 times higher than that of pure Res.SA/NFs-Res showed nano-fiber structure with smooth surface,stable thermodynamic properties and antioxidant capacity equivalent to pure Res.SA/NFs-Res had certain pH sensitivity and could release Res slowly in simulated gastric juice but rapidly in simulated intestinal juice.Conclusion:The electrostatic spinning technique can be used to prepare SA/NFs-Res to increase water solubility and stability of Res,maintain its antioxidant capacity and promote its quick release in simulated intestinal juice,which are beneficial for the application of electrospinning fibers in functional foods,health products and drug carriers.