Center of Natural Products, Faculty of Chemistry, University of Havana, Havana, Cuba.
Carbohydr Polym. 2013 Jan 30;92(1):856-64. doi: 10.1016/j.carbpol.2012.10.005. Epub 2012 Oct 13.
Synthetic O6-succinylated chitosan and commercial glycol chitosan were covalently linked to dl-α-tocopheryl monoesters for controlled release of vitamin E. These conjugates formed self-assembled nanoparticles in aqueous solution with 254-496 nm mean diameters and dl-α-tocopherol contents between 27 and 39% (w/w). The particles appeared as 40-75 nm almost spherical nanoparticles when studied by scanning and transmission electron microscopy upon drying. Drug linking to chitosan matrix was confirmed by FTIR spectroscopy and proton NMR. Conjugates were also characterized by differential scanning calorimetry and wide-angle X-ray diffraction. In vitro tocopherol release studies performed in water at acid pH indicated a drug release dependence on drug content, hydrated particle sizes and employed chitosan derivative. Almost constant release rates were observed the first 7h. The obtained nanoparticles exhibited radical scavenging activity in DPPH essay. The potential of these nanoparticles was also demonstrated by the enhancement of HMVEC cell proliferation.
合成 O6-琥珀酰化壳聚糖和商业乙二醇壳聚糖通过共价键与 dl-α-生育酚单酯连接,用于维生素 E 的控制释放。这些共轭物在水溶液中形成自组装纳米粒子,平均粒径为 254-496nm,dl-α-生育酚含量为 27-39%(w/w)。通过扫描和透射电子显微镜在干燥时研究,发现这些颗粒在 40-75nm 时几乎呈球形纳米颗粒。通过傅里叶变换红外光谱和质子 NMR 证实了药物与壳聚糖基质的连接。通过差示扫描量热法和广角 X 射线衍射对共轭物进行了表征。在酸性 pH 下的水中进行的体外生育酚释放研究表明,药物释放取决于药物含量、水合颗粒大小和所用壳聚糖衍生物。在最初的 7 小时内观察到几乎恒定的释放速率。这些得到的纳米粒子在 DPPH 试验中表现出自由基清除活性。这些纳米粒子的潜力也通过增强 HMVEC 细胞增殖得到了证明。