Apremilast

Apremilast, an oral phosphodiesterase-4 (PDE-4) inhibitor, is widely used in the treatment of inflammatory diseases such as psoriasis and psoriasis arthritis. However, its poor water solubility to formulate and evaluate a Nanoemulsion (NE) system for Apremilast to enhance its solubility, stability, and bioavailability. A Nanoemulsion was developed using a high energy emulsification method, with a combination of oil, surfactant, and co-surfactant carefully selected based on solubility studies and construction of pseudo-ternary phase diagrams. Various formulations were prepared and evaluated for droplet size, polydispersity index (PDI), zeta potential, and drug encapsulation efficiency. The optimized formulation exhibited a droplet size of below 600 nm, a low PDI, and a stable zeta potential, confirming its stability. According to this report, the Nanoemulsion based delivery system for Apremilast drug could offer significant clinical advantages, particularly in terms of improved pharmacokinetics and enhanced therapeutics outcomes, paving the way for more effective treatment of inflammatory diseases such as psoriasis and psoriatic arthritis. Further in vivo studies are recommended to confirm the observed benefits and to evaluate long term safety and efficacy.

A simple, rapid and sensitive liquid chromatography / electro spray ionization tandem mass spectrometry (LC–ESI–MS/MS) assay method has been proposed for the determination of apremilast in human plasma samples using apremilast d5 as internal standard (IS). Analyte and the IS were extracted from the 200 µL of human plasma via simple solid–phase extraction. The Chromatographic separation was obtained on a C18 column operating at a flow rate of 1.0 mL/min by using a mobile phase comprising of mixture of 5mm ammonium acetate in 0.2% formic acid buffer (15:85, v/v) and acetonitrile. A linear (r2 ³ 0.99) of the calibration curve was obtained over the concentration range of 2.03–808 ng/mL.  As per FDA guidelines method validation was performed and the results met the acceptance criteria. The intra–day and inter–day precision (%CV) and accuracy results in five validation batches across five concentration levels were well within the acceptance limits. To analyze the more number of samples in short time, thus increasing the productivity a short run time of 2.25 min for each sample was applied and this was made possible. The method was successfully applied to a pharmacokinetic study in humans.