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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 current study, polylactide-co-glycolide (PLGA) nanoparticles entrapping both clozapine (CLZ) and risperidone (RIS) were formulated by spray-drying using Buchi Nano Spray Dryer B-90 (Flawil, Switzerland). Parameters such as inlet temperature, spray mesh diameter, sample flow rate, spray rate and applied pressure were optimized to produce nanoparticles having desired release profile using both low- and high-molecular weight PLGA polymer. Smallest size nanoparticle of size around 248 nm could be prepared using a 4.0 μm mesh diameter with low-molecular weight polymer. The load of CLZ and RIS was 126.3 and 58.2 μg/mg of polymer particles, respectively. Entrapment efficiency of drugs in PLGA nanoparticles was 94.74% for CLZ and 93.12% for RIS. Both the drugs released continuously from the nanoparticle formulations. PLGA nanoparticles formulated using low-molecular weight polymer released around 80% of the entrapped drug over 10 days of time. Nature of drug inside polymer particles was amorphous, and there was no chemical interaction of CLZ and RIS with polymer. Polymeric nanoparticles were found to be non-toxic in nature using PC12 cell line. This nanospray drying process proved to be suitable for developing polymeric nanoformulation delivering dual drugs for the treatment of Schizophrenia.