Development of ethylcellulose based nanosponges of apremilast: In vitro and in vivo pharmacokinetic evaluation

The purpose of this study was to improve the bioavailability of the poorly water-soluble drug, apremilast (APT), by developing ethylcellulose (EC) based nanosponges. Three nanosponges (ANS1-ANS3) were prepared by varying the concentration of polymer, formulated nanosponges were optimized based on particle size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (%EE) and loading efficiency (%LE). The formulae ANS3 was selected as an optimized nanocarrier that showed the particle size = 324 nm, PDI = 0.253, ZP = -33 mV, %EE = 72.7%, %LE = 11.5%; SEM images reflects the porous-spongy surface. The ANS3 was further evaluated for FTIR, DSC, in vitro drug release and pharmacokinetic studies in male rats. A sustained release pattern of ANS3 nanosponges was observed with a burst drug release of 60.34% in the first hour. The pharmacokinetic profile ANS3 showed a 1.64-fold in- crease in bioavailability in comparison to pure apremilast suspension. Therefore, the ethylcellulose based apremilast loaded nanosponges could be used as an efficient nanocarrier for the effective treatment of pso-riasis and psoriatic arthritis condition.