Abstract: Meloxicam (MLX) is widely applied as a therapy for rheumatoid arthritis (RA); however,\nit takes far too long to reach its peak plasma concentration for a quick onset effect, and gastrointestinal\ntoxicity has been observed in RA patients taking it. To solve these problems, we designed MLX\nsolid nanoparticles (MLX-NPs) by the bead mill method and used them to prepare new oral\nformulations. The particle size of the MLX-NPs was approximately 20-180 nm, and they remained\nin the nano-size range for 1 month. The tmax of MLX-NPs was shorter than that of traditional\nMLX dispersions (MLX-TDs), and the intestinal penetration of MLX-NPs was significantly higher in\ncomparison with MLX-TDs (P < 0.05). Caveolae-dependent endocytosis (CavME), clathrin-dependent\nendocytosis (CME), and micropinocytosis (MP) were found to be related to the high intestinal\npenetration of MLX-NPs. The area under the plasma MLX concentration-time curve (AUC) for\nMLX-NPs was 5-fold higher than that for MLX-TDs.......................
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