期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 492, 期 1-2, 页码 28-39出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2015.07.010
关键词
Ocular drug delivery; Single and mixed nanomicellar systems; Lornoxicam; Confocal laser scanning microscopy; Histopathological studies
Polymeric micelles that can deliver drug to intended sites of the eye have attracted much scientific attention recently. The aim of this study was to evaluate the aqueous-based formulation of drug-loaded polymeric micelles that hold significant promise for ophthalmic drug delivery. This study investigated the synergistic performance of mixed polymeric micelles made of linear and branched poly(ethylene oxide)-poly(propylene oxide) for the more effective encapsulation of lornoxicam (LX) as a hydrophobic model drug. The co-micellization process of 10% binary systems combining different weight ratios of the highly hydrophilic poloxamers; Synperonic (R) PE/P84, and Synperonic (R) PE/F127 and the hydrophobic poloxamine counterpart (Tetronic (R) T701) was investigated by means of photon correlation spectroscopy and cloud point. The drug-loaded micelles were tested for their solubilizing capacity towards LX. Results showed a sharp solubility increase from 0.0318 mg/mL up to more than 2.34 mg/mL, representing about 73-fold increase. Optimized formulation was selected to achieve maximum drug solubilizing power and clarity with lowest possible particle size, and was characterized by (HNMR)-H-1 analysis which revealed complete encapsulation of the drug within the micelles. Further investigations by histopathological and confocal laser studies revealed the non-irritant nature and good corneal penetrating power of the proposed nano-formulation. (C) 2015 Elsevier B.V. All rights reserved.
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