Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Department of Dermatology, STD's and Andrology, Faculty of Medicine, Minia University, Al Minya, Egypt.
Int J Pharm. 2019 Sep 10;568:118556. doi: 10.1016/j.ijpharm.2019.118556. Epub 2019 Jul 23.
Tazarotene (TAZ) is a topical synthetic retinoid used in psoriasis treatment, however, it is extremely lipophilic and exhibits skin irritation. Research is in a state of continuous advancement in the field of nanocarriers fabrication, and in this regard, we investigated the formulation of novel topically oriented nanovesicles; representing a combination of spanlastics and penetration enhancer vesicles, to be termed (fluidized-SNs). TAZ-loaded fluidized SNs were physicochemically characterized, tested for ex vivo cutaneous retention, and the selected formulation was compared with the marketed product Acnitaz® regarding clinical antipsoriatic activity. The selected fluidized-SNs enriched with 1% cineole exhibited high entrapment for TAZ (76.19%), suitable size and zeta potential of 241.5 ± 5.68 nm and -36.10 ± 2.50 mV respectively, and retaining of stability after refrigeration storage for one month. As hypothesized, cineole enriched fluidized-SNs exhibited remarkable TAZ deposition amounting to a total of 81.51% in the different skin layers. Upon clinical assessment, the presented formulation displayed superior traits compared to the marketed product, in terms of dermoscopic imaging, morphometric analysis of psoriatic lesions, and statistical analysis of PASI scores. Results confirmed that the prepared novel fluidized spanlastics formulation holds great promise for the treatment of psoriasis, and its benefit should futuristically be investigated in other topical diseases.
他扎罗汀（TAZ）是一种用于治疗银屑病的局部合成维甲酸，但它具有极强的亲脂性，并表现出皮肤刺激性。在纳米载体制备领域，研究处于不断进步的状态，在这方面，我们研究了新型局部导向纳米囊泡的配方；代表了 spanlastics 和渗透增强囊泡的结合，被称为（流化-SN）。对载有 TAZ 的流化 SN 进行了物理化学特性分析，测试了其在体外皮肤保留情况，并将所选配方与市售产品 Acnitaz®进行了临床抗银屑病活性比较。用 1%桉叶油精强化的选定流化-SN 对 TAZ 的包封率高达 76.19%，合适的粒径和 Zeta 电位分别为 241.5±5.68nm 和-36.10±2.50mV，冷藏储存一个月后仍保持稳定。正如假设的那样，含有桉叶油精的流化-SN 显示出 TAZ 的显著沉积量，在不同的皮肤层中总共达到 81.51%。在临床评估中，与市售产品相比，所提出的制剂在皮肤镜成像、银屑病病变的形态计量学分析以及 PASI 评分的统计分析方面表现出更好的特性。结果证实，所制备的新型流化 spanlastics 制剂具有治疗银屑病的巨大潜力，其在未来应在其他局部疾病中进行研究。
