Enhancement of ocular efficacy of aceclofenac using biodegradable PLGA nanoparticles: formulation and...

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.