Moghddam Seyedeh Raziyeh Mahdavi, Ahad Abdul, Aqil Mohd, Imam Syed Sarim, Sultana Yasmin
Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), M. B. Road, New Delhi 110062, India.
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Mater Sci Eng C Mater Biol Appl. 2016 Dec 1;69:789-97. doi: 10.1016/j.msec.2016.07.043. Epub 2016 Jul 20.
This research aimed towards the design of preparations of diacerein loaded cholesterol rich niosomes by employing a 3-factor, 3-level Box-Behnken design. Results indicated that Span 60 (90mg) and cholesterol (10mg), and 45min of hydration time were found to be optimum for niosomes preparation. The prepared cholesterol rich niosomes were uniform and spherical in size. Optimized formulation F2 entrapped the drug with 83.02% efficiency in the cholesterol rich niosomes of the size 477.8nm, presented the flux of 2.820μg/cm(2)/h, followed Higuchi model and non Fickian transport mechanism. The confocal laser scanning microscopy showed that niosomes accentuated the penetration of diacerein in the epidermal and dermal layer of rat skin. Stability study confirmed that cholesterol rich niosomes were stable for 2months at 4°C. Concisely, the results showed that targeted diacerein delivery might be achieved using topically applied niosomes for enhanced treatment of psoriasis, which might eliminate adverse side effects associated with systemic exposure.
本研究旨在采用三因素三水平的Box-Behnken设计,设计载有双醋瑞因的富含胆固醇的非离子表面活性剂囊泡制剂。结果表明,司盘60(90mg)和胆固醇(10mg)以及45分钟的水化时间对于非离子表面活性剂囊泡的制备是最佳的。所制备的富含胆固醇的非离子表面活性剂囊泡大小均匀且呈球形。优化后的制剂F2在大小为477.8nm的富含胆固醇的非离子表面活性剂囊泡中对药物的包封率为83.02%,通量为2.820μg/cm²/h,遵循Higuchi模型和非Fickian转运机制。共聚焦激光扫描显微镜显示,非离子表面活性剂囊泡增强了双醋瑞因在大鼠皮肤表皮和真皮层的渗透。稳定性研究证实,富含胆固醇的非离子表面活性剂囊泡在4°C下可稳定保存2个月。简而言之,结果表明,使用局部应用的非离子表面活性剂囊泡可实现双醋瑞因的靶向递送,以增强对银屑病的治疗,这可能消除与全身暴露相关的不良副作用。