Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy.
Institute on Membrane Technology (ITM-CNR), Via Pietro BUCCI, c/o University of Calabria, Cubo 17C, 87036 Rende, Italy.
Molecules. 2022 Apr 3;27(7):2319. doi: 10.3390/molecules27072319.
α-tocopherol (α-T) has the highest biological activity with respect to the other components of vitamin E; however, conventional formulations of tocopherol often fail to provide satisfactory bioavailability due to its hydrophobic characteristics. In this work, α-tocopherol-loaded nanoparticles based on chitosan were produced by membrane emulsification (ME). A new derivative was obtained by the cross-linking reaction between α-T and chitosan (CH) to preserve its biological activity. ME was selected as a method for nanoparticle production because it is recognized as an innovative and sustainable technology for its uniform-particle production with tuned sizes and high encapsulation efficiency (EE%), and its ability to preserve the functional properties of bioactive ingredients operating in mild conditions. The reaction intermediates and the final product were characterized by HNMR, Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC), while the morphological and dimensional properties of the nanoparticles were analyzed using electronic scanning microscopy (SEM) and dynamic light scattering (DLS). The results demonstrated that ME has high potential for the development of α-tocopherol-loaded nanoparticles with a high degree of uniformity (PDI lower than 0.2), an EE of almost 100% and good mechanical strength, resulting in good candidates for the production of functional nanostructured materials for drug delivery. In addition, the chemical bonding between chitosan and α-tocopherol allowed the preservation of the antioxidant properties of the bioactive molecule, as demonstrated by an enhanced antioxidant property and evaluated through in vitro tests, with respect to the starting materials.
α-生育酚(α-T)在维生素 E 的其他成分中具有最高的生物活性;然而,由于其疏水性特征,常规的生育酚制剂往往无法提供令人满意的生物利用度。在这项工作中,通过膜乳化(ME)制备了基于壳聚糖的α-生育酚负载纳米粒子。通过α-T 与壳聚糖(CH)之间的交联反应获得了新的衍生物,以保持其生物活性。选择 ME 作为纳米颗粒生产方法,是因为它被认为是一种创新且可持续的技术,具有均匀的颗粒生产、可调的粒径和高包封效率(EE%),并且能够在温和条件下保持生物活性成分的功能特性。通过 HNMR、傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)对反应中间体和最终产物进行了表征,通过电子扫描显微镜(SEM)和动态光散射(DLS)对纳米颗粒的形态和尺寸特性进行了分析。结果表明,ME 具有很高的潜力,可以开发具有高均匀度(PDI 低于 0.2)、接近 100%的 EE 和良好机械强度的α-生育酚负载纳米粒子,是用于生产用于药物输送的功能性纳米结构材料的良好候选物。此外,壳聚糖和α-生育酚之间的化学键合允许生物活性分子的抗氧化性能得以保留,通过体外测试评估,与起始材料相比,抗氧化性能得到了增强。