Abstract：
Nanoemulsions have carved their position in topical delivery owing to their peculiar features of forming a uniform film on the skin and conquering stratum corneum barrier and hence fostering dermal penetration and retention. The present work developed syringic acid nanoemulsion (SA-NE) by spontaneous emulsification as an anti-psoriatic remedy via the dermal route. SA-NE were prepared with either lauroglycol90, limonene or their combination (oil phase) and tween80 (surfactant) with variable concentrations. The physicochemical characteristics of SA-NE were assessed together with Ex-vivo skin deposition and dermal toxicity. The effectiveness of optimal formula in psoriatic animal model and psoriatic patients was investigated using PASI scoring and dermoscope examination. Results showed that, SA-NE containing mixture of lauroglycol 90, limonene and 10 % tween80 (F5), was selected as the optimal formula presenting stable nanoemulsion for 2-month period, showing droplet size of 177.6 ± 13.23 nm, polydispersity index of 0.16 ± 0.06, zeta potential of -21.23 ± 0.41 mV. High SA% in different skin strata and no dermal irritation was noticed with limonene-based SA-NE also it showed high in-vitro anti- inflammatory potential compared to the blank and control formulations. A preclinical study demonstrated that limonene-based SA-NE is effective in alleviating psoriasis-like skin lesions against imiquimod-induced psoriasis in rats. Clinically, promising anti-psoriatic potential was asserted as all patients receiving F5 experienced better clinical improvement and response to therapy, achieving ≥ 50 % reduction in PASI scores versus only 35 % responders in the Dermovate® cream group. Collectively, the practical feasibility of limonene-based SA-NE topical delivery can boost curative functionality in the treatment of psoriatic lesions.
摘要：
纳米乳液由于其在皮肤上形成均匀膜和克服角质层屏障并因此促进皮肤渗透和保留的独特特征而在局部递送中占据了它们的位置。本工作通过自发乳化开发了丁香酸纳米乳液（SA-NE），作为通过皮肤途径的抗牛皮癣药物。SA-NE用不同浓度的月桂基乙醇90，柠檬烯或其组合（油相）和tween80（表面活性剂）制备。评估SA-NE的物理化学特性以及离体皮肤沉积和皮肤毒性。使用PASI评分和皮肤镜检查研究最佳配方在银屑病动物模型和银屑病患者中的有效性。结果表明,含SA-NE的月桂二醇90，柠檬烯和10％tween80（F5）的混合物，被选为表现出2个月稳定纳米乳液的最佳配方，显示液滴尺寸为177.6±13.23nm，多分散指数为0.16±0.06，zeta电位为-21.23±0.41mV。与空白和对照制剂相比,基于柠檬烯的SA-NE在不同皮肤层中的高SA%和没有观察到皮肤刺激,它也显示出高的体外抗炎潜力。临床前研究表明，基于柠檬烯的SA-NE可有效缓解大鼠咪喹莫特诱导的牛皮癣样皮肤病变。临床上,有希望的抗银屑病潜力被断言为所有患者接受F5经历了更好的临床改善和对治疗的反应，在Dermovate®乳膏组中，PASI评分降低≥50%，而响应者仅为35%。总的来说，基于柠檬烯的SA-NE局部给药的实际可行性可以提高银屑病病变治疗的疗效.
