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Ocular inflammatory diseases, such as uveitis, scleritis, episcleritis and dry eye syndrome are commonly treated with eye drop formulations. In the present study, attempts were made to prepare aceclofenac oil formulations to evaluate its transcorneal permeation and anti-inflammatory effect. Ophthalmic solutions of aceclofenac with or without (0.5% v/v) benzyl alcohol were formulated in different vegetable oils and permeation studies were carried out. Aceclofenac ophthalmic solution in linseed oil containing benzyl alcohol exhibited maximum permeation (4.42% in goat, 4.26% in sheep and 3.94% in buffalo) through corneas under study. The partition characteristics of aceclofenac in linseed oil reinforced the results of permeation studies. The optimized formulation (linseed oil containing benzyl alcohol) showed better stability profile. Linseed oil aceclofenac formulation showed significant inhibitory effect on ocular inflammation induced by arachidonic acid in rabbit eyes (p < .05) and hence it can be considered as a potential approach for treatment of ocular inflammatory conditions.

The aim of the present study was to develop and evaluate positively charged nanoparticles of aceclofenac for ocular delivery. The nanoparticles were prepared by the nanoprecipitation method using Eudragit RS 100. The optimized nanoparticles were found to have narrow particle size range (238.9 ± 8 nm) with nearly spherical shape, positive zeta potential (40.3 ± 3.8). Higher entrapment efficiency of aceclofenac (94.53 ± 1.0%) with prolonged in vitro drug release profiles was also observed. Powder X-ray diffraction and differential scanning calorimetry studies indicated decrease in crystallinity of drug within the nanoparticulate polymeric matrix. The formulation was found to have higher permeation as compared to aceclofenac aqueous solution. Nanoparticle formulation was found to be quite stable and well tolerated with no signs of corneal damage. The in vivo studies involving the arachidonic acid-induced ocular inflammation in rabbits showed optimal efficacy of the nanoparticles with significantly higher inhibition of polymorphonuclear leukocytes migration (p < 0.05) and lid closure scores. [ABSTRACT FROM AUTHOR]