In Vitro Bioactivities of Alcohol-Free Benzydamine Oromucosal Solutions

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.

Keywords

• alcohol-free
• benzydamine
• bioactivity
• chitosan
• poloxamer 407
• oromucosal solution