OCTOPIROX 10 g

Octopirox as an antimicrobial and antibacterial additive against dandruff and acne

Octopirox is a well-known Piroctone Olamine, which has a high antibacterial and antimicrobial activity, but shows a low level of toxicity and environmental pollution compared to the same Zinc pyrithione. In cosmetics Octopirox acts as a highly effective antiperspirant and anti-acne active additive, is used for the treatment and prevention of acne, has a wide range of activity not only against fungi and yeasts, but also against bacteria.

Characteristics of components and features of use

INCI: Piroctone Olamine

Dosage (recommended concentration): 0.05 - 0.5 - in non-washable products; up to 1% - in washable products.

Solubility:

• in water, alcohol, aqueous solutions of surfactants
• is well soluble in alcohol (10%),
• soluble in aqueous solutions of surfactants
• is soluble in mixtures of water/alcohol (1-10%)
• is slightly soluble in water (about 0,05%)
• and oils (0,05 - 0,1%).

Peculiarities of application: the component is stable at pH of the finished product from 3.0 to 9.0 and at temperatures up to 80 °C. Octopirox solubility depends significantly on pH. In aqueous formulations, its solubility is greater in neutral and slightly alkaline environments than in acidic ones. The pH value has a significant effect on the solubility of this product in surfactants. The solubility in most surfactants increases in the pH range from 5 to 8.

We give several variants of Octopirox introduction into cosmetics:

• prepare Octopirox/water mixture, disperse and add to the surfactant mixture, then heat up
• prepare Octopirox/water mixture and heat to about 80°C with stirring, then cool and add to surfactant mixture.
• dissolve Octopirox in alcohol (propylene glycol) and add to the surfactant mixture.
• when preparing an emulsion, add Octopirox to the oil phase together with the emulsifier.
• It is not recommended to add Octopirox to surfactants without prior dissolution, this may lead to clumping and slower dissolution.

Storage: in a tightly closed container in a dry dark place at a temperature not exceeding 25˚C. Keep out of direct sunlight.

Antibacterial activity of Piroctone Olamine

Piroctone Olamine is a highly effective fungicide and antiperspirant active ingredient that has been used in the cosmetic industry for over 30 years. It has a high level of antimicrobial activity, expressed as the minimum inhibitory concentration (MIC) of Octopirox for most known Gram-positive and Gram-negative bacteria. The data are summarized in the figure below.

The effect on fungi and yeasts, also represented by the minimum inhibitory concentration (MIC), was determined in Sabouraud's medium with dextrose at pH 6.5. Octopirox was dissolved in ethanol/water mixture. The results shown in the figure indicate that the MIC for the major fungal species is between 0.5 and 4.0 μg/mL.

A new level of effectiveness against dandruff

Pyroctonolamine or trade name Octopirox is one of the most effective and non-toxic anti-dandruff agents on the market today. Specifically formulated to treat dandruff, seborrheic dermatitis and dry scalp, Pyroctonolamine has many benefits:

• environmentally friendly
• multifunctional (also acts as a co-preservative)
• Can be used in various cosmetics (including antibacterial soaps or cosmetics for problem skin).

Octopyrox helps to get rid of dandruff and scales on the scalp, eliminates itching, but it acts gently and does not irritate the skin. It is widely used in anti-dandruff shampoos as well as in hair care products such as toners and conditioners. The low input percentage of the component ensures low production cost of the finished formula, and the low toxicity does not pollute the environment and does not require special labeling.

A scalp free of dandruff and scaling

Microorganisms such as Malassezia furfur produce enzymes that break down fats into their corresponding fatty acids. These and other breakdown products, such as lipid peroxides, irritate the scalp. As a result, mitosis and keratinocyte production increase, leading to dandruff and parakeratosis.

Octopirox effectively controls microbial growth and directly targets the cause of dandruff. The concentration used can range from 0.1 to 1.0% depending on the finished product. For permanent products, the concentration can be reduced to 0.05-0.1%.

Below you can see the effectiveness of an anti-dandruff shampoo. In a 1.5-month study, a prescription with Octopirox at a concentration of 0.75% showed a significant reduction in dandruff compared to a placebo shampoo.

Itch Relief

Many people suffer from itching and constant scratching of the scalp. This condition can be caused by nervous disorders, but in most cases it is caused by dandruff. When the scalp is irritated by dandruff, it sheds its top layer in an attempt to get rid of the irritant. At this point, the scalp can become itchy. Studies have tracked the reduction in itching after using a shampoo containing 0.5% Octopirox compared to a placebo for 54 days. 

Use in cosmetics for problem skin in anti-acne products

In the fight against acne and pimples, Octopirox has shown high effectiveness because the component has a wide range of activity not only against fungi and yeasts, but also against bacteria. Propionibacterium acnes contribute to the emergence and spread of acne due to the release of enzymes (lipase) in the process of its vital activity in the secretions of skin secretion and the breakdown of triglycerides of sebum (release of free fatty acids). Minimum inhibitory concentration (MIC) of Octopirox against propionibacterial acne 3 - 6 mcg/mL. Another fact is that according to Hahn et al (Dermatol. Monatsschr. 168 (1982) 842 - 843) yeast can also activate the development of acne: Octopirox may also be useful here because of its activity against this type of microorganism.

Studies have shown that after 4 weeks of using an emulsion containing 0.3% octopirox, the amount of free fatty acids in skin secretions decreased by 40-45%. Many famous world brands such as Vichy Normaderm, Uriage, Biodroga, Sans Soucis (German brands) contain Octopirox in their formulas.

Comparison of Octopirox with Zinc Pyrithione and its advantages

Octopirox is an easier-to-use powder form that dissolves readily in aqueous surfactant solutions or water/alcohol mixtures. It does not require any special manufacturing processes, whereas Zinc Pyrithione requires a stabilizer and a special dissolving agent.

Octopirox allows to reduce the amount of thickeners in the formula due to its ability to increase the viscosity of shampoos. Octopirox also allows for a more transparent finished formula, whereas zinc pyrithione cannot be used for transparent products. 

Octopirox, unlike zinc pyrithione, has a positive effect on hair thickness (Pierard-Franchimont, Int. J. of Cosmetic
Science 2002, 24, 249-256)

A visualization of the comparative performance of Octopirox & Zinc Pyrithione is shown in the graph below.

Peculiarities of the use of Octopirox in different formulations

1.Effect on pH: Aqueous or alcoholic water solutions of Octopirox are characterized by a pH of 8.5 to 10. Organic acids such as citric acid or lactic acid are very suitable for adjusting the pH to the commercially required ranges of 4 to 7. It should be noted that the solubility of Octopirox decreases at acidic pH.

2.Compatibility with most surfactants, additives and active ingredients used in cosmetics. Regarding compatibility with perfume oils, compatibility with those containing aldehyde and ketone groups may be limited. Octopyrox itself is anionic in nature, but is compatible with most cationic products. In some cases, undesirable interactions with cationic surfactants may occur. Each time a new formulation is created, compatibility should be verified by testing the safety of your particular formulation.

3. Effect on formula viscosity: Studies have shown that Octopirox increases the viscosity of most surfactant systems, especially at dosages between 0.5% and 1%. This very useful property (saving on consistency modifiers, thickeners) should be taken into account when developing or improving appropriate formulations and possibly reducing the dosage of the latter.

4. Combination with dyes: When selecting dyes for coloring formulations, it should be noted that in the presence of traces of iron (1 ppm Fe), the formulation will become yellow (due to the formation of intensely yellow iron complexes). It is recommended that blue or pale green colored formulations be pre-tested for color change. Yellow, orange or red dyes are appropriate. If blue or green dyes are used, make sure that the raw materials do not contain traces of iron.
5. Storage stability: Exposure of cosmetics containing octopirox to direct sunlight may cause undesirable changes in the active ingredient. Therefore, it is recommended to use colored or opaque packaging materials. If transparent packaging materials are used, product stability tests should be performed.

The following dosages are recommended for various cosmetic formulations

• Hair shampoos 0.3 - 1.0%.

• Hair tonics 0.05 - 0.1
• Hair conditioners 0.1 - 0.3
• Hair styling lotions/gels 0.05 - 0.2
• Hair foams 0.1 - 0.3
• Deodorants, including foot deodorants 0.1 - 0.3
• Hand soaps 0.1 - 0.3
• Anti-acne products (gels and foams, lotions) up to 0.5

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