期刊
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
卷 63, 期 -, 页码 -出版社
ELSEVIER
DOI: 10.1016/j.jddst.2021.102507
关键词
Raw 264.7 macrophages; Lipopolysaccharide-stimulation; Nitric oxide; TNF-alpha; Prostaglandin E2; Meloxicam solid dispersions; Hot melt extrusion
The study investigates the anti-inflammatory and cytoprotective potentials of MELOX from SDs on LPS-stimulated cells, showing that HME-prepared SDs provide stronger inhibition of inflammatory mediators while maintaining normal cell growth. The findings highlight the impact of SDs preparation techniques on MELOX treatment performance.
The present study investigates the anti-inflammatory and cytoprotective potentials of a selective COX-II inhibitor, Meloxicam (MELOX) from solid-dispersions (SDs), using lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages cell line. MELOX/SDs were prepared by fusion (FM) & hot-melt-extrusion (HME) techniques using Soluplus/Lutrol F127 as mixed-polymers. SDs were physicochemically evaluated by SEM, XRD and solubility-testing. Viability of cell-growth was determined by MTT assay. Evaluation of inflammation was based on production of nitric oxide (NO), tumor necrosis factor-alpha (TNF-alpha) and prostaglandin E2 (PGE2). MELOX Solubility increased by 3- and 4- folds from SDs prepared by FM and HME, respectively, compared to pure drug. XRD/SEM analyses confirmed drug-dispersion within mixed-polymers. Exposure of normal-cells to different MELOX-treatments maintained the integrity of cell-growth. LPS-stimulated cells treated with MELOX/SDs exhibited higher viabilities compared to cells treated with pure MELOX. The prepared MELOX/SDs showed statistically stronger inhibition of inflammatory-mediators with respect to pure drug. Only, MELOX/SDs prepared by HME, successfully restored LPS-induced TNF-alpha level to that of normal-cells. SDs prepared by HME provided superior reduction of NO, TNF-alpha and PGE2, while maintaining normal cell-growth. The present study highlights the effect of SDs preparation techniques, on MELOX treatment performance.
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