This study aims to improve the antifungal effects of eugenol through low-energy self-assembly fabrication and optimization of eugenol-casein nanoparticles (EC-NPs). Optimized EC-NPs (eugenol/casein ratio of 1:5) were obtained with a mean size of 307.4 ± 2.5 nm and entrapment efficiency of 86.3% ± 0.2%, and showed high stability under incubated at 20 and 37 °C for 48 h. EC-NPs exhibited satisfactory sustained-release effect at 20 °C or 37 °C, with remaining eugenols amounts of 79.51% and 53.41% after 72 h incubation, respectively, which were significantly higher than that of native eugenol (only 26.40% and 19.82% after the first 12 h). EC-NPs exhibited a greater antifungal activity (>95.7%) against spore germination of fungus that was greater than that of native eugenol, showed 100% inhibition of the anthracnose incidence in postharvest pear after 7 d. EC-NPs is potential as an environmental-friendly preservatives in the food industry.

This study aims to stabilize loaded celecoxib (CX) by modifying the structure of casein nanoparticles through phosphatidylcholine. The results show that Egg yolk phosphatidylcholine PC_98T (PC) significantly increased the stability of CX-PC-casein nanoparticles (NPs) (192.6 nm) from 5 min (CX-β-casein-NPs) to 2.5 h at 37 °C. In addition, the resuspended freeze-dried NPs (202.4 nm) remained stable for 2.5 h. Scanning electron microscopy indicated that PC may block the micropore structures in nanoparticles by ultrasonic treatment and hence improve the physicochemical stability of CX-PC-casein-NPs. The stability of the NPs was positively correlated with their inhibiting ability for human malignant melanoma A375 cells. The structural modification of CX-PC-casein-NPs resulted in an increased intracellular uptake of CX by 2.4 times than that of the unmodified ones. The pharmacokinetic study showed that the Area Under Curve (AUC) of the CX-PC-casein-NPs was 2.9-fold higher in rats than that of the original casein nanoparticles. When CX-PC-casein-NPs were intravenously administrated to mice implanted with A375 tumors (CX dose = 16 mg/kg bodyweight), the tumor inhibition rate reached 56.2%, which was comparable to that of paclitaxel (57.3%) at a dose of 4 mg/kg bodyweight. Our results confirm that the structural modification of CX-PC-casein-NPs can effectively prolong the remaining time of specific drugs, and may provide a potential strategy for cancer treatment.