Department of Pharmaceutics, The University of Minia, Main Road, Minia, 19623, Egypt.
AAPS PharmSciTech. 2018 Nov;19(8):3490-3500. doi: 10.1208/s12249-018-1166-1. Epub 2018 Sep 14.
Thymoquinone, the major constituent of Nigella sativa oil has been found to have a promising topical anti-inflammatory activity; however, exaggerated heat and photo-sensitivity and lipophilicity prevent the best use of this promising product. The present work aimed to formulate an ideal thymoquinone liposomal system for topical delivery. Different liposomal systems were developed using thin film hydration method by applying different cholesterol molar concentrations, different total lipid molar concentrations, and different drug-to-lipid ratios. Morphological characterization of the prepared formulae was performed using polarized light, scanning electron microscope, and transmission electron microscope. The optimized formula (F12) was selected on the basis of enhanced permeation through the skin and was incorporated into chitosan gel for topical application. The gel formulation was clear with suitable skin permeation and exhibited acceptable rheological properties. Using carrageenan-induced paw edema in rats, the developed chitosan gel (F12) showed significant superior in vivo anti-inflammatory activity over the chitosan gel of the TQ (p < 0.05) and comparable effect to the marketed indomethacin gel. As a conclusion, results revealed the potential of formulating thymoquinone as liposomal formulation in enhancing the anti-inflammatory effect compared to the TQ solution.
姜黄色素是黑种草籽油的主要成分，已被发现具有有前景的局部抗炎活性；然而，其过度的热和光敏感性以及亲脂性阻碍了该有前景产品的最佳应用。本工作旨在为局部递送来构建理想的姜黄色素脂质体系统。通过应用不同的胆固醇摩尔浓度、不同的总脂质摩尔浓度和不同的药物与脂质比，采用薄膜水化法开发了不同的脂质体系统。使用偏光显微镜、扫描电子显微镜和透射电子显微镜对制备的配方进行形态学表征。根据皮肤渗透增强的情况选择了优化的配方（F12），并将其纳入壳聚糖凝胶中用于局部应用。该凝胶制剂澄清透明，具有合适的皮肤渗透性，并表现出可接受的流变学性质。通过在大鼠中用角叉菜胶诱导足肿胀，与姜黄色素溶液相比，所开发的壳聚糖凝胶（F12）显示出显著优越的体内抗炎活性（p<0.05），与市售的吲哚美辛凝胶相当。总之，结果表明，与姜黄色素溶液相比，将姜黄色素制成脂质体制剂可增强抗炎效果。
