Inflammation is a localized rejoinder towards cellular injury. Caffeine, the Xanthine alkaloid is reported to possess many beneficial properties but limited bioavailability and increased metabolic clearance limits its therapeutic applications. Mesoporous silica nanoparticles (MSN) are used as carrier for sustained drug release owing to its preferable biocompatibility, biodegradability and better loading efficiency. The present study addressed the efficiency of MSN as a delivery system of caffeine to limit inflammation in lipopolysaccharide (LPS) activated macrophage cells. Caffeine loaded silica nanoparticles (CSNP) were prepared and High Performance Liquid Chromatography (HPLC) was performed. Anti-inflammatory potential of free caffeine and CSNP was determined on LPS activated RAW 264.7 macrophage cells. Analysis of Cyclooxygenase (COX), Lipoxygenase (LOX), Myeloperoxidase (MPO), and Inducible nitric oxide synthase (iNOS) enzymes authenticate a comparable anti-inflammatory activity of CSNP over caffeine. In vitro scratch assay uncovered that CSNP has abridged the wound area radically when compared with caffeine and MSN (control). From the indirect ELISA, caffeine and CSNP produced merest COX 2 and TNF-α activity when related with LPS treated group but CSNP produced significant ( p< 0.001) decrease. RT-PCR results confirm a significant decrease in relative expression of COX-2 and TNF-α mRNA levels in CSNP groups in comparison with free caffeine, thereby proving CSNPs efficient inhibition in inflammatory response. The results suggest an increase in anti inflammatory activity can be attributed to sustained release of caffeine from MSN, prompting therapeutic significance.
Key words: Caffeine, Cyclooxygenase 2, TNF alpha, RAW 264.7, wound healing
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