Abstract
The low oral bioavailability of active pharmaceutical ingredients in aqueous media causes to partial absorption through the gastrointestinal tract. Increasing surface area by particle size reduction has been accomplished to overcome these challenges. In this study, Aprepitant (APT) nanoparticles were prepared using a green solvent anti-solvent precipitation method based on subcritical water (SW) technology. Effects of three different parameters such as SW temperature (368.15–388.15 K), anti-solvent temperature (273.15–293.15 K), and polyethylene glycol concentration (0.02–0.04 wt%) were studied on the size and morphology of the produced nanoparticles. As the next step, optimization of the process was performed using the response surface Box-Behnken design (BBD), and optimum operational conditions were obtained as follows: SW temperature (388.15 K), anti-solvent temperature (283.15 K), and polyethylene glycol concentration (0.04 wt%). The results revealed a significant decline in the size of the precipitated particle by subcritical water-based technologies (5.0 nm, on average), as compared to the unprocessed drug particles (30 μm, on average). Green SW-based technologies are proposed for the preparation of APT nanoparticles with no requirement for organic solvents and post-processing purification stages.
Published Version
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