Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Egypt.
Int J Pharm. 2017 Apr 30;522(1-2):157-164. doi: 10.1016/j.ijpharm.2017.03.005. Epub 2017 Mar 7.
The aim of this research was to encapsulate ciprofloxacin, a broad spectrum fluoroquinolone antibiotic, into Span 60 based nano-elastic vesicles, nano-spanlastics, for accomplishing improved non invasive trans-tympanic delivery, providing means for ototopical treatment of acute otitis media (AOM). To achieve this purpose, ciprofloxacin-loaded nano-spanlastics were prepared by thin film hydration (TFH) technique, using several non-ionic edge activators (EAs) according to full factorial design (3). The investigation of the effect of formulation variables on nano-spanlastic characteristics and selection of the optimum formula were performed using Design-Expert software. The selected formulation was also subjected to comparative ex-vivo permeation studies through tympanic membrane (TM) of rabbits. Results revealed that the optimal nano-spanlastic formulation (S-2; containing 20% Brij 35 as an EA) exhibited nano-sized spherical vesicles (287.55±9.97nm), relatively high entrapment efficiency percent (51.81±1.57%), and good physical stability after six months of storage at 4-8°C. Ex-vivo TM permeation studies demonstrated the superiority of the optimal nano-spanlastic formulation over the commercial Ciprocin drops. However, when compared to lipid-based elastic vesicles, nano-transfersomes, nano-spanlastics exhibited lower drug permeation through the TM. Concisely, the obtained results suggested that nano-spanlastics can be promising for improving trans-tympanic delivery of ciprofloxacin.
本研究旨在将广谱氟喹诺酮抗生素环丙沙星包封于 Span 60 基纳米弹性囊泡（纳米弹性体）中，以实现经鼓膜非侵入性递药，为急性中耳炎（AOM）的局部耳用治疗提供手段。为达到此目的，采用薄膜水化（TFH）技术，根据完全析因设计（3），使用几种非离子型边缘活性剂（EAs）制备载有环丙沙星的纳米弹性体。采用 Design-Expert 软件研究制剂变量对纳米弹性体特性的影响，并筛选出最佳配方。对选定的配方也进行了兔鼓膜（TM）体外渗透比较研究。结果表明，最佳纳米弹性体配方（S-2；包含 20% Brij 35 作为 EA）呈纳米级球形囊泡（287.55±9.97nm），包封率较高（51.81±1.57%），在 4-8°C 下储存 6 个月后物理稳定性良好。体外 TM 渗透研究表明，最佳纳米弹性体配方优于市售 Ciprocin 滴耳剂。然而，与脂质弹性囊泡相比，纳米传递体和纳米弹性体透过 TM 的药物渗透能力较低。总之，研究结果表明纳米弹性体可能是提高环丙沙星经鼓膜递药的有前途的制剂。
