基于疏水性海藻酸盐衍生物的纳米粒子的制备及表征作为维生素 D3 缓释载体。

Preparation and characterization of nanoparticles based on hydrophobic alginate derivative as carriers for sustained release of vitamin D3.

机构信息

College of Marine Life Sciences, Ocean University of China, Qingdao 266003, People's Republic of China.

出版信息

J Agric Food Chem. 2011 Mar 9;59(5):1962-7. doi: 10.1021/jf1020347. Epub 2011 Feb 2.

DOI:10.1021/jf1020347

Abstract

Hydrophobic alginate derivative was prepared by modification of alginate by acid chloride reaction using oleoyl chloride without organic solvents. The conjugate of oleoyl alginate ester (OAE) was confirmed by FT-IR and (1)H NMR. The degree of substitution (DS) of OAE was determined by (1)H NMR, and it ranged from 0.84 to 3.85. In distilled water, OAE formed self-assembled nanoparticles at low concentrations in aqueous medium, and nanoparticles retained their structural integrity both in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The loading and release characteristics of nanoparticles based on OAE were investigated using vitamin D(3) as a model nutraceutical. As the concentration of vitamin D(3) increased, the loading capacity (LC) increased, whereas the loading efficiency (LE) decreased. Nanoparticles could release vitamin D(3) at a sustained rate in gastrointestinal fluid. These results revealed the potential of OAE nanoparticles as oral carriers for sustained release of vitamin D(3).

摘要

通过酰氯反应，在没有有机溶剂的情况下用油酰氯对海藻酸盐进行修饰，制备了疏水性海藻酸盐衍生物。通过傅里叶变换红外光谱（FT-IR）和（1）H 核磁共振（NMR）确认了油酰化海藻酸盐酯（OAE）的结合物。通过（1）H NMR 确定了 OAE 的取代度（DS），其范围为 0.84 至 3.85。在蒸馏水中，OAE 在低浓度的水介质中形成自组装纳米颗粒，并且纳米颗粒在模拟胃液（SGF）和模拟肠液（SIF）中都保持其结构完整性。使用维生素 D（3）作为模型营养药物研究了基于 OAE 的纳米颗粒的负载和释放特性。随着维生素 D（3）浓度的增加，载药量（LC）增加，而载药效率（LE）降低。纳米颗粒可以在胃肠道液中以持续的速度释放维生素 D（3）。这些结果表明 OAE 纳米颗粒作为维生素 D（3）口服缓释载体的潜力。