Topical formulations

Topical formulations

Quats are well-known antiseptics and have a long history of use in topical products such as hand sanitizers, antiseptic liquids, creams and gels. They act on a wide range of microorganisms, including enveloped viruses, from gram+ and gram- bacteria, moulds and yeasts. Our FeF Quats are colourless and odourless in finished product formulation, and their effectiveness in all pH ranges combined with their ability to mix well in both aqueous and oily phases, make them an ideal antimicrobial ingredient.

Applications

No matter the application, for formulations coming into contact with healthy or damaged epithelial tissue, it is necessary to utilize only the purest and safest ingredients.

All our FeF Quats products are widely used in both human and veterinary topicals. Skin cleansing solutions: FeF Benzalkonium Chloride (BKC) are used for cleansing skin, mucous membranes, and wounds with a concentration of 0.01 to 0.1%.

Hand sanitizers: Typically the concentration of FeF Benzalkonium Chloride (BKC) in hand sanitizers is maximum 2% w/w. Standard concentrations in finished products normally vary between 0.5% and 1.5% w/w, and more dilute solutions are suitable for irrigation of deep wounds.

Antiseptic creams: FeF Benzalkonium Chloride (BKC), FeF Cetrimide  is often found in antiseptic creams used in the treatment of nappy rash, eczema, psoriasis, acne and other dermatoses at concentrations varying from 0.1 to 1%.

Hair products: FeF Quats are also used in hair products, or example to treat seborrheic dermatitis. Spermicide: FeF Benzalkonium Chloride (BKC) is widely used in spermicides in foams, creams and ampoules.

Safety and efficacy

Since Quats act on the surface and not on the content of cells, they do not trigger antibiotic resistance. Quats should not be classified as skin sensitizers but as skin irritants. Bromides are less irritating to the skin than chlorides. Quats are relatively non-toxic in use concentrations and only considered harmful in concentrated forms.

Tertiary amines are used in the manufacture of Quats; free amine is a possible impurity and can be responsible for skin irritation. FeF Quats are carefully manufactured with synthetic raw materials from qualified suppliers, and our validated processes are fully controlled to obtain the lowest possible content of impurities.

Product characteristics

Solubility: Quats are miscible with water or lower alcohols, such as methanol, ethanol and propanol in all ratios. Quats are not miscible with benzene or ether.

Compatibility: Quats can be combined with e.g. alcohol and chlorhexidine and with the most commonly used compounds in topical formulations. Mixing Quats with ordinary soaps and/or with anionic detergents may decrease the activity. As Quats are cationic compounds, they should not be mixed with anionic compounds which would have a neutralizing effect. Quats can be inhibited by Tween™ and by lecithin. Avoid mixing Benzalkonium Chloride (BKC) with citrates, iodides, nitrates, perman ganates, salicylates, silver salts and tartrates. Incompatibilities have also been reported with other substances including aluminium, fluorescin sodium, hydrogen peroxide, kaolin and some sulfonamides.

Stability: 5 years shelf life.

Other: Colourless and odourless in finished product formulation, Easy to formulate, Surface active / adhesive, Non-volatile and very stable.

Antimicrobial effect

FeF Quats are effective at all pH levels. However their effectiveness increases when the pH increases. The higher the pH, the lower the concentration needed to obtain an antimicrobial effect. As opposed to bacteriostatic/fungistatic compounds which only prevent micro-organisms from dividing (growing), Quats are bactericidal/fungicidal, meaning they will kill micro-organisms, whether they are in a growth phase or not.

Some antibiotics under given conditions are more effective than antimicrobials. However, in general, they only work if the micro-organism is in a growth phase and so, cannot be used as an antimicrobial. FeF Quats have been tested against several relevant microbial strains, and shown to be effective against a wide range of micro-organisms at low concentrations. In Table 1, FeF Quats are compared here with ethanol and with a positive control containing Meropenem (a broad-spectrum antibiotic).

Benzalkonium Chloride is also effective in inactivating enveloped viruses such as herpes, hepatitis, corona and influenza, at very low concentrations. Several publications support the use of BKC as an effective anti-viral, for example against SARS-CoV, M31yxo- and related viruses, type A influenza, herpes simplex, adenovirus type 5, measles, canine distemper, feline pneumonitis, meningopneumonitis agents, HIV-1 and more. (Please see references below)

Table 1: Minimal Inhibitory Concentrations. Mean results in % or μg/ml.

References:

• Saknimit M, Inatsuki I, Sugiyama Y, Yagami K. (1988). Virucidal efficacy of physico-chemical treatments against coronaviruses and parvoviruses of laboratory animals. Jikken Dobutsu. 37:341-5.
• Centers for Disease Control and Prevention. (2008) Guideline for Disinfection and Sterilization in Healthcare Facilities, U.S. Centers for Disease Control and Prevention.
• Dellanno C1, Vega Q, Boesenberg D. The antiviral action of common household disinfectants and antiseptics against murine hepatitis virus, a potential surrogate for SARS coronavirus. American Journal of Infection Control.2009 Oct;37(8):649-52.
• A. Armstrong and E.J. Froelich. Inactivation of Viruses by Benzalkonium Chloride. Applied Microbiology Vol. 12. No. 2,132-137 March 1964.
• Manfred H.Wolff, Syed A. Sattar, Olusola Adegbunrin and Jason Tetro. Environmental survival and microbicide inactivation of coronaviruses. Coronaviruses with Special Emphasis on First Insights Concerning SARS 201 ed. by A. Schmidt, M.H. Wolff and O. Weber, 2005, p.201-212.
• Mark A. Wainberg, Bonnie Spira, Gilles Bleau and Rejean Thomas. Inactivation of Human Immunodeficiency Virus Type 1 in Tissue Culture Fluid and in Genital Secretions by the Spermicide Benzalkonium Chloride. Journal of Clinical Microbiology, Jan. 1990. p. 156-158