Journal
COLLOIDS AND SURFACES B-BIOINTERFACES
Volume 130, Issue -, Pages 23-30Publisher
ELSEVIER
DOI: 10.1016/j.colsurfb.2015.03.059
Keywords
Itraconazole; Polymeric micelles; In situ gel; Ex vivo transcorneal permeation; In vitro corneal hydration; Histology
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The aim of this article is to investigate the role of amphiphilic block copolymer-based polymeric micelles of itraconazole for the management of fungal keratitis to overcome the limitations of the conventional dosage form. The polymeric micelles were made using pluronics above critical micelle concentration. Itraconazole-loaded polymeric micelles prepared by rotary evaporation method were characterized and the optimized micellar formulation (M5) was selected on the basis of least micelle size (79.99 nm), maximum entrapment efficiency (91.32% +/- 1.73%) and in vitro permeation (90.28% +/- 0.31%) in 8 h, that best fitted zero-order kinetics. M5 was developed as pH sensitive in situ gel and characterized for various parameters. The optimized in situ gel (F5) proved to be superior in its ex vivo transcorneal permeation when compared with Itral (R) eye drop and pure drug suspension, exhibiting 41.45% +/- 0.87% permeation with zero-order kinetics (r(2) = 0.994) across goat cornea. Transmission electron microscopy revealed spherical polymeric micelles entrapped in the gel matrix. A spectrum of tests revealed hydration capability, non-irritancy, and histologically safe gel formulation that had appropriate handling characteristics. Conclusively, a controlled release pH-sensitive ocular formulation capable of carrying drug to the anterior segment of the eye via topical delivery was successfully developed for the treatment of fungal keratitis. (C) 2015 Published by Elsevier B.V.
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