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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.

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.

In the present study, an effort was made to design poly (D, L-lactide-co-glycolide) acid nanoparticles of aceclofenac by direct precipitation method. The nanoparticles were found to have adequate particle size range for ocular administration of 162.6 to 244.13 nm with nearly spherical shape and with zeta potential of - 21.5 to - 25.5 mV. Drug entrapment efficiency of nanoparticle formulations ranged from 42.9 to 92.68%. Differential scanning calorimetric (DSC) and powder X-ray diffraction (PXRD) studies depicted that the drug incorporated in nanoparticles was found to be in amorphous state. Moreover, nanoparticles showed prolonged in vitro drug release profile and followed Higuchi-square-root release kinetics. Nanoparticles showed two folds higher permeation than aqueous solution of aceclofenac. Nanoparticles were well tolerated with no signs of corneal damage in in vitro transcorneal permeation studies. The formulation was quite stable. In vivo ocular anti-inflammatory study in the rabbit eyes confirmed better efficacy of nanoparticles as compared with the aqueous solution and its potential application in ocular inflammatory conditions.

The purpose of this study was to prepare Eudragit RL 100-based nanoparticles of aceclofenac by nanoprecipitation and evaluate the particle size, zeta potential, drug entrapment, particle morphology; in vitro drug release and in vivo efficacy. Change in drug-polymer ratio from 1:5 to 1:20 increased the particle size and entrapment efficiency. The particles showed sustained in vitro drug release which followed the Higuchi square-root kinetics. The results indicate that the nanoparticles release the drug by a combination of dissolution and diffusion. Based on the particle size (134.97 nm) and entrapment efficiency (95.73%), the formulation made with 1:10 drug-polymer ratio was selected for further studies. The particles were spherical with a polydispersity index of 0.186 and zeta potential of +30.5 mV. Powder X-ray diffraction and differential scanning calorimetry indicated decrease in crystallinity of drug in the nanoparticle formulation. In the in vitro permeation study, the nanoparticle formulation showed 2-fold higher permeation of drug through excised cornea compared to an aqueous solution of drug with no signs of corneal damage. The in vivo studies involving arachidonic acid-induced ocular inflammation in rabbits revealed significantly higher inhibition of polymorphonuclear leukocytes migration (p<0.05) and lid closure scores by the nanoparticle formulation compared with the aqueous solution. The formulation was quite stable to ensure two year shelf life at room temperature., (Copyright © 2012 Elsevier B.V. All rights reserved.)

In this study, diclofenac-loaded Eudragit S100-based nanosuspension was prepared by nanoprecipitation method and characterised for particle size, morphology, in vitro release, and for its in vivo ocular anti-inflammatory activity. The diclofenac-loaded Eudragit S100 nanosuspension was found to have a particle size of 172 nm, polydispersibility index of 0.14 and zeta potential of -23.7 +/- 6.07 mV, indicating that the nanosuspension is fairly stable. The nanosuspended particles were found to be spherical in shape. The nanosuspension was found to provide a sustained in vitro release, following the Higuchi square-root release kinetics. The results indicated that the nanosuspension released the drug by combination of dissolution and diffusion. The in vivo evaluation of nanosuspension in PGE(2)-induced ocular inflammation in rabbit model revealed a significantly (p  <  0.05) higher inhibition of PGE(2)-induced polymorphonuclear leukocytes migration and lid-closure scores as compared with the aqueous solution of diclofenac.