Abdelgawad Rana, Nasr Maha, Moftah Noha H, Hamza Manal Yassin
Pharmaceutics Lab, National organization for drug control and research NODCAR, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Eur J Pharm Sci. 2017 Apr 1;101:258-268. doi: 10.1016/j.ejps.2017.02.030. Epub 2017 Feb 21.
Nanotechnology and material surface modification have provided a functional platform for the advancement of several medical fields such as dermatology. Furthermore, the smart choice of preparation material was proven to confer unique properties to the developed nanosystems. In this context, we focused on the sphingolipid "ceramide", whose deficiency was found to negatively affect psoriasis. Ceramide was doped into surfactant based vesicular phospholipid systems to create tubulated vesicles "cerosomes" loaded with a model anti-psoriatic drug "tazarotene", and their properties were tested as compared to ceramide free vesicles. Cerosomes were characterized for their drug entrapment, viscosity, in vitro drug release, morphology, ex vivo drug skin deposition, thermal behavior, and were clinically tested on psoriatic patients. The factorial design study revealed that the surfactant type, the ceramide: surfactant ratio, and the presence of ethanol in the hydration buffer affected the entrapment efficiency and the viscosity of the vesicles. Ceramide increased the entrapment of tazarotene, decreased its release while enhancing its deposition within the skin, correlating with better clinical therapeutic outcome compared to the topical marketed product. Ceramide was also able to cause significant membrane tubulation in the vesicles, causing them to deviate from the conventional spherical morphology. As a conclusion, cerosomes present a new functional treatment modality for psoriasis which is worthy of future experimentation.
纳米技术和材料表面改性为皮肤病学等多个医学领域的发展提供了一个功能平台。此外，制备材料的明智选择被证明能赋予所开发的纳米系统独特的性能。在此背景下，我们聚焦于鞘脂类“神经酰胺”，发现其缺乏会对银屑病产生负面影响。将神经酰胺掺入基于表面活性剂的囊泡磷脂系统中，以制备负载模型抗银屑病药物“他扎罗汀”的管状囊泡“神经酰胺体”，并与不含神经酰胺的囊泡相比测试其性能。对神经酰胺体进行了药物包封、粘度、体外药物释放、形态、离体药物皮肤沉积、热行为等方面的表征，并在银屑病患者身上进行了临床试验。析因设计研究表明，表面活性剂类型、神经酰胺与表面活性剂的比例以及水合缓冲液中乙醇的存在会影响囊泡的包封效率和粘度。神经酰胺增加了他扎罗汀的包封率，降低了其释放速率，同时增强了其在皮肤内的沉积，与市售局部用药产品相比，临床治疗效果更好。神经酰胺还能够使囊泡产生显著的膜管状化，使其偏离传统的球形形态。总之，神经酰胺体为银屑病提供了一种新的功能治疗方式，值得未来进行实验。
