| Autor: |
Kashikar R; Department of Pharmaceutics and Drug Delivery, University of Mississippi, Mississippi, USA., Senapati S; Department of Pharmaceutics and Drug Delivery, University of Mississippi, Mississippi, USA., Dudhipala N; Department of Pharmaceutics and Drug Delivery, University of Mississippi, Mississippi, USA., Basu SK; Department of Ophthalmology, The University of Tennessee Health Science Center, Hamilton Eye Institute, Memphis, Tennessee, USA., Mandal N; Department of Ophthalmology, The University of Tennessee Health Science Center, Hamilton Eye Institute, Memphis, Tennessee, USA.; Department of Anatomy and Neurobiology, The University of Tennessee Health Science Center, Memphis, Tennessee, USA., Majumdar S; Department of Pharmaceutics and Drug Delivery, University of Mississippi, Mississippi, USA.; Research Institute of Pharmaceutical Sciences, University of Mississippi, Mississippi, USA. |
| Abstrakt: |
Purpose: Fingolimod (FTY720; FT), a structural analog of sphingosine, has potential ocular applications. The goal of this study was to develop an FT-loaded nanoemulsion (NE; FT-NE) formulation for the efficient and prolonged delivery of FT to the posterior segment of the eye through the topical route. Methods: FT-NE formulations were prepared using homogenization followed by the probe sonication method. The lead FT-NE formulations (0.15% and 0.3% w/v loading), comprising soybean oil as oil and Tween ® 80 and Poloxamer 188 as surfactants, were further evaluated for in vitro release, surface morphology, filtration sterilization, and stability at refrigerated temperature. Ocular bioavailability following topical application of FT-NE (0.3%) was examined in Sprague-Dawley rats. Results: The formulation, at both dose levels, showed desirable physicochemical characteristics, a nearly spherical shape with homogenous nanometric size distribution, and was stable for 180 days (last time point checked) at refrigerated temperature postfiltration through a polyethersulfone (0.22 µm) membrane. In vitro release studies showed prolonged release over 24 h, compared with the control FT solution (FT-S). In vivo studies revealed that effective concentrations of FT were achieved in the vitreous humor and retina following topical application of FT-NE. Conclusions: The results from these studies demonstrate that the FT-NE formulation can serve as a viable platform for the ocular delivery of FT through the topical route. |
