Pharmaceutics Department, Faculty of Pharmacy, Damanhour University, Cairo, Egypt.
Pharmaceutical Technology Department, Pharmaceutical Industry Division, National Research Centre, Cairo, Egypt.
J Liposome Res. 2020 Mar;30(1):45-53. doi: 10.1080/08982104.2019.1580721. Epub 2019 Mar 7.
This study was aiming to improve the effect of the water-insoluble drug, resveratrol, by encapsulating it in surfactant-based elastic vesicles (spanlastics). Spanlastics (SLs) were prepared by thin film hydration method using different ratios of Span 60 (S60) and edge activators (EAs). The prepared SLs were subjected to full evaluation. All the SLs showed improved properties compared to the drug suspension ( < 0.05). SL5 composed of S60: Brij 35 (7:3) attained the highest drug entrapment efficiency (79.10%±5.56), the smallest particle size (201.30 nm ± 2.45), the best anti-oxidant effect and a fast drug release pattern, thus was selected for further investigation. Based on the Draize test, the selected spanlastics (SL5), as well as the drug suspension, showed to be safe to be applied on the skin (PII <2). studies were done to test the photoprotective effect of the designed nanovesicles compared to the drug suspension. Evaluation was done based on visual examination and analysis of some anti-oxidant markers (CAT, GSH and SOD), anti-inflammatory markers (IL-6, IL-8 and NF-κB) and anti-wrinkling markers (MMP-1 and GM-CSF) after UVB-irradiation. The drug showed a good prophylactic effect, however, that of SL5 was superior compared to that of the drug suspension as recorded by the level of all biochemical markers ( < 0.05). These results were also confirmed by histopathological examination. This study proves that elastic nanovesicles seem to be a promising approach to overcome the low drug solubility and to improve its efficacy.
本研究旨在通过将难溶性药物白藜芦醇包封在基于表面活性剂的弹性囊泡（弹性纳米囊泡）中来提高其效果。采用薄膜水化法，用不同比例的司盘 60（Span 60，S60）和边缘活性剂（edge activators，EAs）制备弹性纳米囊泡。对所制备的弹性纳米囊泡进行全面评估。与药物混悬剂相比（P < 0.05），所有弹性纳米囊泡均显示出改善的性质。由 S60：Brij 35（7：3）组成的 SL5 达到了最高的药物包封效率（79.10%±5.56）、最小的粒径（201.30nm ± 2.45nm）、最佳的抗氧化效果和快速的药物释放模式，因此被选为进一步研究的对象。根据 Draize 试验，所选的弹性纳米囊泡（SL5）和药物混悬剂对皮肤应用均安全（PII < 2）。进行了研究以测试与药物混悬剂相比设计的纳米囊泡的光保护作用。评价基于视觉检查和一些抗氧化标志物（CAT、GSH 和 SOD）、抗炎标志物（IL-6、IL-8 和 NF-κB）和抗皱标志物（MMP-1 和 GM-CSF）的分析。与药物混悬剂相比，药物显示出良好的预防作用，但 SL5 的效果更优，所有生化标志物的水平均有记录（P < 0.05）。这些结果也得到了组织病理学检查的证实。本研究证明，弹性纳米囊泡似乎是克服药物低溶解度和提高其疗效的有前途的方法。
