Production of PEA composite microparticles with polyvinylpyrrolidone and luteolin using Supercritical Assisted Atomization

Palmitoylethanolamide (PEA) has anti-inflammatory, pain controlling and neuroprotective properties, but its use is limited by its low water solubility and corresponding bioavailability. In this work, Supercritical Assisted Atomization (SAA) coprecipitation is used to reduce PEA tendency to crystallize, using polyvinylpyrrolidone (PVP) and luteolin (LUT) and operating at different process parameters. Spherical microparticles were produced at PEA/PVP ratio 1:8 wt/wt in ethanol, with D50 of 400 nm and with the best result as particle morphology. X-ray analysis reveals that these PEA-PVP particles are amorphous and PEA loading efficiency reaches 100%. In the case of PEA-LUT coprecipitates, very small quantities of LUT stabilized the microparticles, inhibiting PEA crystallization process. Indeed, quasi spherical microparticles were produced at 10:1 wt/wt PEA/LUT ratio, with D50 of 970 nm and PEA loading efficiency over 99%. To explain how very small quantities of LUT can modify PEA crystallization behavior, specific PEA-LUT interactions were evidenced by FT-IR analysis.