Department of Pharmaceutical Sciences, University of Calabria, 87036 Arcavacata di Rende (CS), Italy.
Colloids Surf B Biointerfaces. 2013 Sep 1;109:273-9. doi: 10.1016/j.colsurfb.2013.04.005. Epub 2013 Apr 22.
In this study, stearic acid- and stearyl ferulate-based solid lipid nanoparticles containing trans-ferulic acid (SLN-FA and SLN-SF-FA, respectively), were prepared and characterized for loading efficiency, size and shape. In addition, by using rat brain microsomes, we evaluated in vitro the antioxidant activity of these formulations against three well known initiators of lipid peroxidation, such as AAPH, NADPH/ADP-Fe(3+) and SIN-1 which in turn generate the peroxyl and perferryl radicals as well as peroxynitrite, respectively. Commercially available FA and its ethyl ester (FAEE) were used as comparators. Both SLN-FA and SLN-SF-FA dose-dependently reduced lipid peroxidation induced by the three oxidants. Interestingly, SLN-SF-FA displayed greater efficacy (EC50) and potency (maximal activity) against AAPH- and NADPH/ADP-Fe(3+)-induced lipid peroxidation. Our results support the idea that this new formulations could facilitate the uptake of FA by the cells because of their lipophilic structure, thus increasing FA bioavailability. Furthermore, stearyl ferulate-based nanoparticles could prevent the degradation of FA entrapped on their structure, making FA almost entirely available to explicate its antioxidant power once released.
在这项研究中，制备并表征了基于硬脂酸和硬脂酰阿魏酸的载反式阿魏酸的固体脂质纳米粒（分别为 SLN-FA 和 SLN-SF-FA），以评估其载药量、粒径和形态。此外，我们还使用大鼠脑微粒体，评估了这些制剂对三种已知的脂质过氧化引发剂（AAPH、NADPH/ADP-Fe(3+)和 SIN-1）的体外抗氧化活性，这三种引发剂分别生成过氧自由基、过氧自由基和过亚硝酸根。我们还使用了市售的阿魏酸及其乙酯（FAEE）作为对照。SLN-FA 和 SLN-SF-FA 均能剂量依赖性地抑制三种氧化剂诱导的脂质过氧化。有趣的是，SLN-SF-FA 对 AAPH 和 NADPH/ADP-Fe(3+)诱导的脂质过氧化显示出更高的功效（EC50）和效力（最大活性）。我们的研究结果支持这样一种观点，即由于这些新制剂具有亲脂性结构，因此可以促进 FA 被细胞摄取，从而提高 FA 的生物利用度。此外，基于硬脂酰阿魏酸的纳米粒可以防止其结构中包封的 FA 的降解，使得 FA 在释放后几乎全部可以发挥其抗氧化作用。
