Anin vitro study on the cytotoxicity of chlorhexidine digluconate to human gingival cells

Abstract

Chlorhexidine digluconate is the active ingredient in mouthrinses used to prevent dental plaque and gingivitis. The in vitro cytotoxicity of chlorhexidine was evaluated with the Smulow-Glickman (S-G) gingival epithelial cell line. The potency of chlorhexidine was dependent on the length of exposure and composition of the exposure medium. The midpoint cytotoxicity values for 1-, 24-, and 72-h exposures were 0.106, 0.011, and 0.0045 mmol/L, respectively. S-G cells exposed for 2 h to chlorhexidine and then maintained for 48 h in chlorhexidine-free medium were unable to recover from the initial insult. The adverse effects of chlorhexidine on the plasma membrane were suggested by the leakage of lactic acid dehydrogenase from chlorhexidine-treated S-G cells and by the increased permeability of chlorhexidine-treated liposomes to Ca2+. The toxicity of a 24-h exposure to chlorhexidine to the S-G cells was progressively lessened as the content of fetal bovine serum (FBS) in the exposure medium was increased from 2% to 8%. The potency of a 1-h exposure to chlorhexidine was reduced in medium amended with albumin, lecithin, and heat-killed Escherichia coli. These reductions in toxicity were presumably due to the binding of the cationic chlorhexidine to the negatively charged chemical moieties of the components of FBS and of albumin and lecithin and of sites on the surfaces of bacteria. Combinations of chlorhexidine and carbamide peroxide were additive in their cytotoxicities.

Cytotoxicity of chlorhexidine digluconate to murine macrophages and its effect on hydrogen peroxide and nitric oxide induction

“…*P < 0.05 compared to control (ANOVA). Table 1 effects of chlorhexidine as other cell types and that the cytotoxic potential of the substance is dependent on the concentration and time of exposure (14). It is important to note that chlorhexidine digluconate is toxic to macrophages in vitro at concentrations 100 times below those used in clinical practice, usually 0.2-0.5% (15).…”

“…Chlorhexidine may adversely affect the eukaryotic plasma membrane by nonspecific electrostatic binding to negative moieties (protein and phospholipid components), causing alteration in the structure of the cell membrane and in the osmotic equilibrium of the cell (6,14). PMA is a soluble stimulus that acts directly on protein kinase C (present in cytoplasm) activating the production of the superoxide anion, which is subsequently converted to H 2 O 2 (17).…”

Antimicrobial activity of ethylene-vinyl acetate containing bioactive filler against oral bacteria

“…This antiseptic agent can be used for the sterilization and inhibition of oral microorganism growth. However, CHX exhibits cytotoxicity against human gingival fibroblasts and gingival epithelial cells in vitro 40) . Moreover, the longterm use of CHX might cause staining of the teeth, taste alteration, and even anaphylactic reactions 41,42) .…”

Cyclodextrin modulates the cytotoxic effects of chlorhexidine on microrganisms and cellsin vitro

“…This antimicrobial drug has toxic effects on cultured of alveolar bone (Cabral & Fernandes, 2007) and gingival epithelial cells (Babich et al, 1995) and was able to induce a dose-dependent reduction of human gingival fibroblast proliferation and reduces both collagen and non-collagen protein production (Mariotti & Rumpf, 1999;Flemingson et al, 2008).…”