In Vitro Bioactivities of Alcohol-Free Benzydamine Oromucosal Solutions

Suwipa Ungphaiboon, Sutasinee Ardhanwanich, Sonsawan Kongpuckdee, Duangkhae Maneenuan, Teerapol Srichana
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Abstract

Objective: This research aimedto evaluate the effects of chitosan and poloxamer 407 on in vitro cytotoxicity, anti-inflammatory, wound healing, and antimicrobial activities of 0.3% w/v benzydamine hydrochloride (HCl) oromucosal solutions.Material and Methods: The effects of three alcohol-free benzydamine HCl oromucosal formulations; containing: 1) 0.5% w/v chitosan, 2) 15% w/v poloxamer 407, and 3) a combination of 0.5% w/v chitosan and 15% w/v poloxamer 407, on in vitro cytotoxicity and biological activities were evaluated and compared to a commercial benzydamine HCl mouth spray, containing alcohol and 0.12% chlorhexidine solution.Results: All alcohol-free benzydamine HCl formulations and their vehicles were less cytotoxic to the macrophage RAW 264.7 cell line than the commercial spray and to the human gingival fibroblast cell line than chlorhexidine, respectively. The formulation containing 0.5% w/v chitosan exhibited the highest wound healing activity on the fibroblast cells among all tested products, and showed anti-inflammatory activity on macrophage cells, which is comparable to benzydamine HCl. Furthermore, from the time-kill assay, this formulation completely inhibited Streptococcus mutans within 1 minute, similar to 0.12% chlorhexidine solution, and reduced the cell number of Candida albicans more rapidly than the commercial spray.Conclusion: The alcohol-free benzydamine HCl solution containing 0.5% w/v chitosan as a mucoadhesive polymer is a promising oral care candidate, which is safe to be used, and has wound healing, anti-inflammatory, and antimicrobial activities.
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无醇苄胺口腔粘膜溶液的体外生物活性研究
目的:研究壳聚糖和波洛沙姆407对0.3% w/v盐酸苄胺(HCl)口腔黏膜溶液的体外细胞毒性、抗炎、伤口愈合和抗菌活性的影响。材料与方法:三种无醇盐酸苄胺颗粒剂对口腔黏膜的影响研究了1)0.5% w/v壳聚糖、2)15% w/v波洛沙姆407和3)0.5% w/v壳聚糖和15% w/v波洛沙姆407的组合对体外细胞毒性和生物活性的影响,并与含酒精和0.12%氯己定溶液的盐酸苄胺口腔喷雾剂进行了比较。结果:所有无醇盐酸苄胺制剂及其载体对巨噬细胞RAW 264.7细胞系的细胞毒性均低于市售喷剂,对人牙龈成纤维细胞系的细胞毒性均低于氯己定。含0.5% w/v壳聚糖的制剂对成纤维细胞的创面愈合活性最高,对巨噬细胞的抗炎活性与盐酸苄胺相当。此外,从时间杀伤试验来看,该配方在1分钟内完全抑制变形链球菌,与0.12%氯己定溶液相似,并且比市售喷雾更快地减少白色念珠菌的细胞数量。结论:含0.5% w/v壳聚糖的无醇盐酸苄胺溶液作为黏附聚合物是一种有前景的口腔护理药物,使用安全,具有伤口愈合、抗炎和抗菌活性。
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