Musa Siti Hajar, Basri Mahiran, Fard Masoumi Hamid Reza, Shamsudin Norashikin, Salim Norazlinaliza
Department of Chemistry, Faculty of Science.
Department of Medicine, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Malaysia.
Int J Nanomedicine. 2017 Mar 28;12:2427-2441. doi: 10.2147/IJN.S125302. eCollection 2017.
Psoriasis is a chronic autoimmune disease that cannot be cured. It can however be controlled by various forms of treatment, including topical, systemic agents, and phototherapy. Topical treatment is the first-line treatment and favored by most physicians, as this form of therapy has more patient compliance. Introducing a nanoemulsion for transporting cyclosporine as an anti-inflammatory drug to an itchy site of skin disease would enhance the effectiveness of topical treatment for psoriasis. The addition of nutmeg and virgin coconut-oil mixture, with their unique properties, could improve cyclosporine loading and solubility. A high-shear homogenizer was used in formulating a cyclosporine-loaded nanoemulsion. A D-optimal mixture experimental design was used in the optimization of nanoemulsion compositions, in order to understand the relationships behind the effect of independent variables (oil, surfactant, xanthan gum, and water content) on physicochemical response (particle size and polydispersity index) and rheological response (viscosity and -value). Investigation of these variables suggests two optimized formulations with specific oil (15% and 20%), surfactant (15%), xanthan gum (0.75%), and water content (67.55% and 62.55%), which possessed intended responses and good stability against separation over 3 months' storage at different temperatures. Optimized nanoemulsions of pH 4.5 were further studied with all types of stability analysis: physical stability, coalescence-rate analysis, Ostwald ripening, and freeze-thaw cycles. In vitro release proved the efficacy of nanosize emulsions in carrying cyclosporine across rat skin and a synthetic membrane that best fit the Korsmeyer-Peppas kinetic model. In vivo skin analysis towards healthy volunteers showed a significant improvement in the stratum corneum in skin hydration.
银屑病是一种无法治愈的慢性自身免疫性疾病。然而,它可以通过多种治疗方式得到控制,包括局部治疗、全身性药物和光疗。局部治疗是一线治疗方法,且受到大多数医生的青睐,因为这种治疗方式患者的依从性更高。引入一种纳米乳剂,将作为抗炎药物的环孢素输送到皮肤病的瘙痒部位,将提高银屑病局部治疗的效果。添加具有独特特性的肉豆蔻和初榨椰子油混合物,可以提高环孢素的负载量和溶解度。在制备负载环孢素的纳米乳剂时使用了高剪切均质器。采用D-最优混合实验设计来优化纳米乳剂的组成,以了解自变量(油、表面活性剂、黄原胶和含水量)对物理化学响应(粒径和多分散指数)和流变学响应(粘度和屈服值)影响背后的关系。对这些变量的研究表明,有两种优化配方,其特定的油含量(15%和20%)、表面活性剂(15%)、黄原胶(0.75%)和含水量(67.55%和62.55%),在不同温度下储存3个月具有预期的响应且稳定性良好,不会分离。对pH值为4.5的优化纳米乳剂进行了所有类型的稳定性分析:物理稳定性、聚结速率分析、奥斯特瓦尔德熟化和冻融循环。体外释放证明了纳米级乳剂在携带环孢素穿过大鼠皮肤和最符合Korsmeyer-Peppas动力学模型的合成膜方面的功效。对健康志愿者的体内皮肤分析表明,角质层的皮肤水合作用有显著改善。