Department of Pharmacology, Faculty of Pharmacy, Universidad de Sevilla, 41012 Sevilla, Spain.
Department of Pharmacology, Faculty of Pharmacy, University of Valencia, 46010 Valencia, Spain.
Mar Drugs. 2017 Dec 25;16(1):2. doi: 10.3390/md16010002.
Chronic inflammatory skin diseases such as psoriasis have a significant impact on society. Currently, the major topical treatments have many side effects, making their continued use in patients difficult. Microalgae have emerged as a source of bio-active molecules such as glycolipids with potent anti-inflammatory properties. We aimed to investigate the effects of a glycolipid () and a glycolipid fraction () obtained from the microalga on a TPA-induced epidermal hyperplasia murine model. In a first set of experiments, we examined the preventive effects of and dissolved in acetone on TPA-induced hyperplasia model in mice. In a second step, we performed an in vivo permeability study by using rhodamine-containing cream, ointment, or gel to determinate the formulation that preserves the skin architecture and reaches deeper. The selected formulation was assayed to ensure the stability and enhanced permeation properties of the samples in an ex vivo experiment. Finally, -containing cream was assessed in the hyperplasia murine model. The results showed that pre-treatment with acetone-dissolved glycolipids reduced skin edema, epidermal thickness, and pro-inflammatory cytokine production (TNF-α, IL-1β, IL-6, IL-17) in epidermal tissue. The in vivo and ex vivo permeation studies showed that the cream formulation had the best permeability profile. In the same way, -cream formulation showed better permeation than acetone-dissolved preparation. -cream application attenuated TPA-induced skin edema, improved histopathological features, and showed a reduction of the inflammatory cell infiltrate. In addition, this formulation inhibited epidermal expression of COX-2 in a similar way to dexamethasone. Our results suggest that an -containing cream could be an emerging therapeutic strategy for the treatment of inflammatory skin pathologies such as psoriasis.
慢性炎症性皮肤病,如银屑病,对社会有重大影响。目前,主要的局部治疗方法有许多副作用,使患者难以持续使用。微藻已成为生物活性分子的来源,如具有强大抗炎特性的糖脂。我们旨在研究从微藻中获得的糖脂()和糖脂馏分()对 TPA 诱导的表皮增生小鼠模型的影响。在一组实验中,我们研究了溶解在丙酮中的和对 TPA 诱导的小鼠增生模型的预防作用。在第二步中,我们通过使用含有罗丹明的乳膏、软膏或凝胶进行体内通透性研究,以确定保留皮肤结构并达到更深层次的配方。选择的配方进行了测试,以确保样品在体外实验中的稳定性和增强的渗透性。最后,在增生的小鼠模型中评估了含有乳膏。结果表明,丙酮溶解的糖脂预处理可减少皮肤水肿、表皮厚度和表皮组织中促炎细胞因子(TNF-α、IL-1β、IL-6、IL-17)的产生。体内和体外渗透研究表明,乳膏配方具有最佳的渗透性。同样,乳膏制剂的渗透性能优于丙酮溶解制剂。含有乳膏的制剂可减轻 TPA 诱导的皮肤水肿,改善组织病理学特征,并减少炎症细胞浸润。此外,该制剂以类似于地塞米松的方式抑制表皮中 COX-2 的表达。我们的结果表明,含有乳膏的制剂可能成为治疗银屑病等炎症性皮肤疾病的新兴治疗策略。