Cationic Antiseptics Research Articles

Insights into bactericidal action of surface-attached poly(vinyl- N -hexylpyridinium) chains

The surface of polyethylene slides nanocoated with silica and derivatized with long-chain poly(vinyl-N-hexylpyridinium) becomes permanently bactericidal: it kills 90–99% of (both airborne and waterborne) wild-type and antibiotic-resistant strains of the human pathogen Staphylococcus aureus. The material created was similarly lethal to strains expressing multidrug resistance pumps, the only known mechanism of resistance to cationic antiseptics.

The effect of toothpaste on the propensity of chlorhexidine and cetyl pyridinium chloride to produce staining in vitro: a possible predictor of inactivation.

Cationic antiseptics such as chlorhexidine (CHX) and cetyl pyridinium chloride (CPC) interact with dietary chromogens to produce extrinsic stain, and this can be used as a measure of activity of products. The aim of these studies in vitro was to determine if toothpaste influenced the tea staining effects of CHX and CPC as a predictor of action in vivo. Clear acrylic specimens were soaked in pooled human saliva followed by sequential 2-min soaks in pairs of agents, namely 0.05% CHX, 0.05% CPC, 0.2% CHX, water (W) and toothpaste slurry (TP). The combinations were; TP/CHX, CHX/TP, TP/CPC, CPC/TP, W/CHX, CHX/W, W/CPC, CPC/W, TP/W, W/TP, W/W. These treatments were followed by a 60 min soak in tea. Optical density readings were taken at baseline and after each of 8 cycles. In the separate CHX and CPC studies by comparison with W/CHX, TP/0.05% CHX had little effect on staining, but TP/0.2% CHX showed a reduction in staining of 18%. 0.05% CHX/TP reduced staining by >40%, and 0.2% CHX by >78%. TP/CPC reduced staining by >26% and CPC/TP by 80%. Water after 0.2% CHX, 0.05% CHX and CPC reduced staining by 18%, 13% and 17% respectively. Little staining was seen with TP and W combinations. The data for CHX are in agreement with a study in vivo except TP followed by CHX reduced the activity of CHX. Toothpaste appears to adversely affect the activity of CHX and CPC particularly if used immediately after the antiseptics. The data further supports the concept of separating the use of antiseptics until sometime after the use of toothpaste, and the idea of developing mouthwash friendly toothpastes.

The effect of toothpaste on the propensity of chlorhexidine and cetyl pyridinium chloride to produce staining in vitro: a possible predictor of inactivation

AbstractBackground/aims: Cationic antiseptics such as chlorhexidine (CHX) and cetyl pyridinium chloride (CPC) interact with dietary chromogens to produce extrinsic stain, and this can be used as a measure of activity of products. The aim of these studies in vitro was to determine if toothpaste influenced the tea staining effects of CHX and CPC as a predictor of action in vivo.Method: Clear acrylic specimens were soaked in pooled human saliva followed by sequential 2‐min soaks in pairs of agents, namely 0.05% CHX, 0.05% CPC, 0.2% CHX, water (W) and toothpaste slurry (TP). The combinations were; TP/CHX, CHX/TP, TP/CPC, CPC/TP, W/CHX, CHX/W, W/CPC, CPC/W, TP/W, W/TP, W/W. These treatments were followed by a 60 min soak in tea. Optical density readings were taken at baseline and after each of 8 cycles.Results: In the separate CHX and CPC studies by comparison with W/CHX, TP/0.05% CHX had little effect on staining, but TP/0.2% CHX showed a reduction in staining of 18%. 0.05% CHX/TP reduced staining by >40%, and 0.2% CHX by >78%. TP/CPC reduced staining by >26% and CPC/TP by 80%. Water after 0.2% CHX, 0.05% CHX and CPC reduced staining by 18%, 13% and 17% respectively. Little staining was seen with TP and W combinations. The data for CHX are in agreement with a study in vivo except TP followed by CHX reduced the activity of CHX.Conclusion: Toothpaste appears to adversely affect the activity of CHX and CPC particularly if used immediately after the antiseptics. The data further supports the concept of separating the use of antiseptics until sometime after the use of toothpaste, and the idea of developing mouthwash friendly toothpastes.

Mechanisms of Stain Formation on Teeth, in Particular Associated with Metal Ions and Antiseptics

Much has been written on the subject of extrinsic tooth discoloration, but, except when the pigment is intentionally applied, the etiologies and mechanisms are poorly understood. Extrinsic stains have been classified as non-metallic or metallic. The pigment usually lies not on or in the dental tissues, but in surface deposits, particularly the acquired pellicle layer and at sites receiving limited cleaning. Whether pigments absorb, adsorb, or chemically interact with dental surfaces is unclear. Some stains merely seem to reflect the color of the apparent source, whereas others have been ascribed to a secondary chemical alteration of a substance at the tooth or pellicle surface. Theories of chromogenic bacteria and formation of metal sulfides are frequently propounded but without clear supportive evidence. Staining by cationic antiseptics and, to a lesser extent, metal salts has attracted research interest. Chlorhexidine and other cationic antiseptics, it is hypothesized, may catalyze browning reactions or facilitate metal sulfide formation in pellicle. Controlled clinical studies have repeatedly shown that dental and mucosal staining associated with the use of chlorhexidine and some metal salts is dependent upon volunteers' imbibing reasonable quantities of chromogenic beverages, such as tea. However, it must be appreciated that cationic antiseptics and polyvalent metals can precipitate chromogenic material from a large range of dietary compounds. The control of dental staining, at least that associated with chlorhexidine, can be achieved both in vitro and in vivo by the use of oxidizing agents which appear to remove the stain physically from the surfaces.

The use of an oxidising mouthwash to reduce staining associated with chlorhexidine

Discolouration of the teeth, tongue and dental restorative materials associated with the use of cationic antiseptics is still the limiting factor in long-term usage of antiplaque agents such as chlorhexidine. Oxidising agents have been used successfully to remove dental stain in animals, but products and regimens have not been evaluated in humans. These pilot studies in vitro and in vivo assessed a long-established oxidising mouthwash, based on peroxyborate, for stain removal from teeth and acrylic. The laboratory studies measured chlorhexidine tea stain removal from tooth and acrylic specimens. The oxidising agent markedly reduced staining on specimens. In a short-term clinical experiment, dental staining was forced over a 2 1/2-day period by reciprocal chlorhexidine and tea rinsing. 5 rinses with the oxidising mouthwash during the next 1 1/2 days dramatically reduced staining compared with water after rinses. Additionally, a single rinse with peroxyborate following the 5 water after rinses, again considerably reduced the residual staining. Effects on tongue staining were less impressive. Both experimental models produced findings consistent with those from the animal model. The results suggest proprietary oxidising mouthwashes could have a place in the control of dental stain associated with the use of chlorhexidine. Further studies to evaluate such products in a more conventional chlorhexidine regimen are indicated.

Comparative susceptibility of hospital isolates of Gram-negative bacteria to antiseptics and disinfectants

The sensitivity of hospital isolates of Gram-negative bacteria to cationic antiseptics, mercuric chloride and two organomercury compounds has been measured. A comparison was made with laboratory strains of known sensitivity which acted as standards. All strains of Escherichia coli showed a uniformly high sensitivity to chlorhexidine diacetate; other organisms tended to be less sensitive to the biguanide. Quaternary ammonium compounds were less effective than chlorhexidine. Resistance to mercuric chloride was observed frequently, but there was little evidence of organomercurial resistance except in Pseudomonas aeruginosa isolates.

The pattern of adsorption of cationic antiseptics to polymethylmethacrylate.

Few studies have reported the maximum potential of surfaces to adsorb the cationic antiseptics and few comparisons between antiseptics have been carried out. The purpose of this investigation was to measure the maximum uptake of alexidine, cetyl pyridinium chloride, chlorhexidine gluconate and chlorhexidine acetate to polymethylmethacrylate and by the construction of adsorption isotherms determine the pattern of molecular attachment to the recipient surface. The mean maximum adsorption findings for these antiseptics demonstrated significantly greater uptake of cetyl pyridinium chloride than the other antiseptics and significantly less uptake of alexidine compared with the other antiseptics. All four antiseptics showed a Langmuir type adsorption isotherm consistent with the formation of a monolayer of molecules on the recipient surface. For chlorhexidine preliminary studies demonstrated that the pattern of adsorption was not altered by saliva pre-treatment of surfaces. No evidence of molecular multilayering was observed even at higher concentrations of the antiseptics. However, the maximum uptake on to the surface was significantly increased when no post-treatment washings were carried out. It was concluded that this increased uptake would be unlikely to play an important role in antiplaque activity because of its relative instability. The pH dependency for the adsorption of these antiseptics was demonstrated such that as previously observed for chlorhexidine gluconate at low pH adsorption is almost completely, or completely, prevented.

The formation of stain on acrylic surfaces by the interaction of cationic antiseptic mouthwashes and tea.

Clinical and in vitro studies have implicated dietary components as major aetiological factors in staining of teeth and acrylic materials associated with chlorhexidine use, a local side effect not unique to this antiseptic. These experiments studied the precipitation and surface staining reactions of the cationic antiseptics alexidine, cetyl pyridinium chloride (CPC), chlorhexidine, and hexetidine, with the beverage tea. All of the antiseptics precipitated a standard tea solution and for alexidine and chlorhexidine acetate and gluconate, this was at concentrations greater than 100 mumol/L, for hexetidine greater than 200 mumol/L, and for CPC greater than 400 mumol/L. With the exception of CPC precipitation was reduced with decreasing pH and for chlorhexidine was inhibited below pH 3. The addition of polymethylmethacrylate (PMMA) to the antiseptic solutions increased the precipitation concentrations by an amount calculated to be adsorbed by polymer. Acrylic blocks treated with equimolar solutions of the antiseptics became progressively and significantly more stained by tea than control specimens over a 5-day period. Alexidine induced significantly greater staining and hexetidine significantly less than the other antiseptics. Staining was pH dependent and significantly reduced as the pH decreased. Both stain and precipitates were insoluble in strong acids and alkalis. It is concluded that staining observed clinically may represent a precipitation reaction with the complexing of antiseptics with dietary chromogenic material.

The Use of Polymethylmethacrylate to Compare the Adsorption and Staining Reactions of Some Cationic Antiseptics

This study assessed the value of acrylic, in powder and optically clear forms, to measure the adsorption and staining properties of some cationic antiseptics. The uptake of chlorhexidine gluconate, chlorhexidine acetate, alexidine and cetyl pyridinium chloride onto acrylic powder was measured spectrophotometrically. Similarly, tea staining of perspex blocks exposed twice daily to the antiseptics and hexetidine, was measured over a 5 day period. The adsorption of chlorhexidine gluconate and acetate was similar and greater than alexidine but less than cetyl pyridinium chloride. Desorption of the adsorbed antiseptics was minimal after 48 hours soaking in water. Acid produced a variable desorption of antiseptics. Tea staining of blocks was significantly greater with antiseptic treated specimens compared to control specimens. However, staining resulting from alexidine was greater than cetyl pyridinium chloride which was greater than chlorhexidine. Hexetidine produced the least staining. Saliva treatment of specimens only increased the tea staining of control blocks. The results indicated that adsorption levels alone would not explain the differences in antiplaque and staining activity reported for the cationic antiseptics.

Antiseptic and antibiotic resistance in gram-negative bacteria causing urinary tract infection in spinal cord injured patients.

Fifty-seven isolates of Gram-negative bacterial species from urinary tract infections in spinal cord injured patients were tested for their sensitivity to chlorhexidine, cetrimide, glutaraldehyde, phenyl mercuric nitrate (PMN), a phenolic disinfectant (Hycolin) and a proprietary antiseptic containing a mixture of picloxydine, octylphenoxypolyethoxyethanol and benzalkonium chloride (Resiguard). None of the isolates were resistant to glutaraldehyde, Hycolin or PMN but a substantial percentage were resistant to chlorhexidine (44 per cent), cetrimide (26 per cent) and Resiguard (42 per cent). The resistant organisms were members of the genera Proteus, Providencia and Pseudomonas and they were also generally resistant to five, six or seven antibiotics. Significant correlations were observed between multiplicity of antibiotic resistance and the minimum inhibitory concentrations of the three cationic antiseptics. It is suggested that an antiseptic policy for the bladder management of spinal cord injured patients that relies on the extensive use of cationic agents might lead to the selection of a flora of notoriously drug-resistant species.

Sensitivity of Providence to antiseptics and disinfectants.

Seventy isolates of Providence were obtained from urinary tract infections in patients from five hospitals. They were all identified as Providence B (Providencia stuartii). A typing system was devised for these organisms based on their production of and sensitivity to bacteriophage and bacteriocins. Using this system, 27 distinct strains were recognized, and it was clear that many patients had been infected with the same strain. The minimum inhibitory concentrations of six antiseptics and disinfectants for these strains were determined. Many of the strains were up to 300-fold more resistant to the cationic antiseptics chlorhexidine, cetrimide, and Resiguard than the control strain Escherichia coli NCTC 10418. The sensitivities of the Providence strains to Hycolin, glutaraldehyde, and phenyl mercuric nitrate, however, were similar to those of the control organism. There were significant correlations between the sensitivities of the strains to the three cationic antiseptics. The loss of chlorhexidine resistance from a Providence strain after exposure of the cells to N-methyl-N' nitro N nitrosoguanidine resulted in a concomitant loss of resistance to cetrimide and Resiguard, but there was no significant increase in the sensitivity of the mutants to the other three antibacterials.

Emergency Sterilization of Drinking Water with Heteropolar Cationic Antiseptics

Emergency Sterilization of Drinking Water with Heteropolar Cationic Antiseptics

Emergency Sterilization of Drinking Water with Heteropolar Cationic Antiseptics

Although there are many practical uses for antiseptics which are effective against cysts of Endamoeba histolytica, one of the most important and difficult is the emergency sterilization of drinking water under military combat conditions. Various halogen preparations have not been entirely satisfactory because they tend to be inactivated by organic nitrogenous material and by alkalinity. Since natural waters encountered in the field may sometimes contain very high concentrations of organic nitrogenous material or may be alkaline, and since military emergency conditions in the field require uniform dosage, it is necessary to use the halogens in high initial concentrations under all conditions so that they may prove effective even under the worst conditions. These high concentrations of the halogens are distasteful and may not be entirely without toxicity.The antiseptic activity of certain heteropolar cationic compounds, or synthetic, cationic detergents, was described in 1935 by Domagk (1) and Katz and Lipsitz (2).