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Glutaryl Melatonin Niosome Gel for Topical Oral Mucositis: Anti- Inflammatory and Anticandidiasis

Author(s):

Teerasak Damrongrungruang*, Panjaree Panpitakkul, Jirachaya Somudorn, Pimpitchaya Saengchart, Pramote Mahakunakorn, Prangthip Uthaiwat, Jureerat Daduang, Panyada Panyatip, Pleontip Puthongking and Aroonsri Priprem   Pages 1 - 12 ( 12 )

Abstract:


Background: Glutaryl melatonin, which is synthesized from melatonin and is a pineal gland-derived neurohormone with anti-inflammatory and anti-oxidant properties, was comparatively investigated for its potential use as a topical anti-inflammatory agent.

Objective: Glutaryl melatonin, synthesized and screened for in vitro anti-candidiasis and in vitro and in vivo anti-inflammatory activities, was formulated as a niosome gel for topical oral evaluation in 5-fluorouracil-induced oral mucositis in mice.

Method: In vitro anti-fungal activity in Candida albicans, in vitro anti-inflammatory activity in Escherichia coli liposaccharide-induced RAW cells and in vivo anti-inflammatory activity using a croton oil-induced ear edema model in ICR mice were investigated. Mucositis in mice (n = 6/group, 10-week-old mice) was induced by intraperitoneal injections of 5-fluorouracil, and the mice were subjected to a topical oral application of niosome gel containing melatonin (2% w/w) or glutaryl melatonin (2% w/w) and were compared with mice subjected to blank, fluocinolone acetonide (0.5% w/w) and control conditions.

Results: Glutaryl melatonin, at a 14. 2 mM concentration, showed the highest fungicidal effect on C. albicans using the broth dilution method, indicating a nonsignificant difference for 1 µM of nystatin (p = 0.05). Nitric oxide, interleukin-6 and tumor necrosis factor-α were analyzed by ELISA. Liposaccharide-induced RAW cells were significantly reduced by glutaryl melatonin (p < 0.01). Ear edema inhibition of glutaryl melatonin was significant 1 h after application compared with that of melatonin (p = 0.03). Food consumption and body weights of the 5-fluorouracil-treated mice were significantly lower than those of the normal mice before all treatments (p < 0.05). Differences in the amount of licking behavior, which was observed in the control group for 5 min, were noticeable in the 5-fluorouracil-treated mice but not in the mice treated with the glutaryl melatonin niosome gel.

Conclusion: Glutaryl melatonin exhibited mild anti-candidiasis and anti-inflammatory properties. The incorporation of glutaryl melatonin in a niosome gel formulation, demonstrated the potential for topical oral applications to reduce oral discomfort caused by 5-fluorouracil treatment in mice.

Keywords:

glutaryl melatonin, anti-candidiasis, anti-inflammation, 5-fluorouracil , niosome gel, anti-fungal

Affiliation:

Division of Oral Diagnosis, Department of Oral Biomedical Sciences, Faculty of Dentistry, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Bachelor degree program in Dentistry, Faculty of Dentistry, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Bachelor degree program in Dentistry, Faculty of Dentistry, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Doctoral degree program in Research and Development of Pharmaceutical Science, Faculty of Pharmaceutical Science, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Faculty of Pharmaceutical Science, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Doctoral degree program in Biomedical Science, the Graduate School, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Department of Clinical Chemistry, Faculty of Associated Medical Science, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Doctoral degree program in Research and Development of Pharmaceutical Science, Faculty of Pharmaceutical Science, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Faculty of Pharmaceutical Science, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002, Faculty of Pharmaceutical Science, Khon Kaen University, 123 Mittraphap Road, Amphur Muang, Khon Kaen, 40002



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