期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 522, 期 1-2, 页码 157-164出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2017.03.005
关键词
Span 60; Elastic vesicles; Thin film hydration; Tympanic membrane permeation; Hydrophilic edge activator
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(2)). The investigation of the effect of formulation variables on nano-spanlastic characteristics and selection of the optimum formula were performed using Design-Expert (R) 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 +/- 9.97 nm), relatively high entrapment efficiency percent (51.81 +/- 1.57%), and good physical stability after six months of storage at 4-8 degrees C. Ex-vivo TM permeation studies demonstrated the superiority of the optimal nano-spanlastic formulation over the commercial Ciprocin (R) 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. (C) 2017 Elsevier B.V. All rights reserved.
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