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Benzalkonium chloride is a cationic surfactant of quaternary ammonium salts and also a chlorine-containing disinfectant, which is composed of dimethyl benzyl ammonium chloride homolog substituted by normal alkyl. Benzalkonium chloride is a dual-function disinfectant that can kill bacteria/fungi and inactivate viruses. In addition, this kind of disinfectant is widely used in skin and environment disinfection because of its low toxicity, little irritation, good water solubility, convenient use and storage. Currently approved by NMPA include patches, solutions, sprays, eye drops, etc.
A large number of domestic and foreign literatures have confirmed that benzalkonium chloride has the following pharmacological effects：
Broad-spectrum killing of pathogenic bacteria: In vitro studies have confirmed that benzalkonium chloride can significantly kill Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Enterococcus faecalis, with a minimum bactericidal concentration of 0.0125% and a minimum bactericidal concentration of 0.00625%, and a bactericidal rate of 100% within 24 hours [4].
Broad-spectrum fungicidal action: Benzalkonium chloride can significantly kill candida albicans, Aspergillus Niger and other fungi, with a minimum bactericidal concentration of 0.0125%[4] and a bactericidal rate of 100% within 24 hours.
Broad-spectrum inhibition kills/suppresses viruses: A number of foreign studies have confirmed that benzalkonium chloride has in vitro effects on SARS, MERSr-CoV, influenza virus (A, B), parainfluenza virus (PSV-1, 2, 3), avian influenza virus (H7N9), Newcastle disease virus, bursal disease virus, adenovirus, HIV virus, HSV-2, Enterovirus, cytomegalovirus, BK virus, poliovirus (PV), Coxsackie virus and Ebola virus, with a minimum killing concentration of 0.00125%, co-incubated with the above viruses in vitro for 1-5min, the virus killing rate exceeds 95%, and the action for 5min can inactivate the replication activity of SARS CoV. Its antiviral activity is significantly better than sodium hypochlorite (84 disinfectant) [5-6].
For coated pathogenic microorganisms: Benzalkonium chloride can change the permeability of viral cytoserous membrane, make viral cytoplasmic substances extravasate, hinder their metabolism and thus play a killing role [4].
For uncoated pathogenic microorganisms: Benzalkonium chloride has positive cationic charge and directly interferes with the metabolism of pathogenic microorganisms after contact with the virus, denatoriating the protein, thereby inhibiting or even killing the virus and controlling the infectivity of the virus [6].
Use of benzalkonium chloride for skin and mucosa disinfection: A clinical study involving 378 dog bite patients [7] showed that the incidence of infection was lower when benzalkonium chloride was used for disinfection of dog bite wounds than when iodophos solution was used (7.43%vs14.21%, P=0.021). Another study involving 60 parineal lateral resection women [8] showed that benzalkonium chloride had a higher bacterial clearance rate when flushing the vulva compared with iodophor + alcohol (80%vs46.6%, P< 0.05). Another foreign study on the reduction of instantaneous staphylococcus aureus on the skin of medical personnel with benzalkonium chloride hand sanitizer showed [9] that compared with 70% ethanol hand washing, the number of instantaneous staphylococcus aureus on the fingertips of medical personnel using benzalkonium chloride hand sanitizer for one week was significantly reduced. It is further indicated that benzalkonium chloride has better disinfection effect on skin than iodophor and alcohol, and is more suitable for hand-washing disinfection in the current epidemic prevention environment.
Benzalkonium chloride for surgery and wound disinfection: In a study of 60 patients with open fractures, benzalkonium chloride was used to clean the wound, and the infection rate was lower than that of traditional 3% hydrogen peroxide and POvidone iodine (3.33%vs16.67%, P< 0.05), and less painful stimulation during irrigation [10]. A clinical study involving 30 burn patients showed [11] that one side of the wound was rinsed with benzalkonium chloride, and the other side was rinsed with 0.5% iodoprene. The 7-day wound healing rates of the two groups were as follows: Benzalkonium chloride group (78.4 + 6.0) %, iodine volts group (65.8 + 6.9) %, comparing the two groups statistically difference (P< 0.05). Benzalkonium chloride is used in surgical wound areas, the infection rate is lower, the healing quality is higher, and the pain irritation is less and more mild.
Benzalkonium chloride for disinfection of articles: A study on biofilm formation of microorganisms extracted from fresh agricultural products (lettuce, lettuce and cucumber) with benzalkonium chloride on stainless steel test plates showed [12] that treatment of biofilm with benzalkonium chloride at 0.01, 0.1 and 1.0g/l, respectively, could promote significant changes in biofilm formation and reduce bacterial biofilm formation. A study from the Japanese Institute of Chemotherapy suggested [5] that after treatment with benzalkonium chloride, SARS, MERSr-CoV, influenza virus (A, B), parainfluenza virus (PSV-1, 2, 3), avian influenza virus (H7N9), etc., were significantly inactivated without human damage, which was significantly better than sodium hypochlorite (84 disinfectant). Therefore, it is highly recommended for inactivation of vaccine production equipment.
Benzalkonium chloride for environmental disinfection: An experimental study used benzalkonium chloride to inhibit microbial fouling in a regenerative water source heat pump system [13]. Benzalkonium chloride, a fungicide with different mass fractions, was used to soak the fouling for 10 minutes every day to investigate its scale inhibition effect. The results showed that benzalkonium chloride had an inhibitory effect on microbial fouling and could kill most of the bacterial cells in the fouling. The effect was enhanced with the increase of its mass fraction. A comparison of the killing activity of peracetic acid, benzalkonium chloride and phthalaldehyde against 77 strains of bacteria in an industrial environment showed that [14] benzalkonium chloride had better antibacterial activity than phthalaldehyde (Dettol). A study from Brussels Hospital in Paris [6] suggested that the inactivation rate of CMV, RSV and ADV virus in HSV-2 was over 95% after 5min treatment with benzalkonum chloride, and the lowest inactivation concentration was 0.0025%; the inactivation rate of ENV, BKV and ADV virus was over 99% after 1min treatment.
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