It was developed to solve the instability problem of 4-Butyl Resorcinol and to make it easy to use. It can be dissolved directly in water. Can be absorbed into the skin well. and has good stability

13.5% 4-Butyl Resorcinol encapsulated in liposome

Nano size : 40-100nm

4-Butyl Resorcinol is one of the whitening substances that helps whiten the skin. with high efficiency But there are usage limitations. Because it's not very stable. When in the formula There is often a problem with discoloration.

Encapsulated 4-Butyl Resorcinol (Liposome, Nano Size) was developed to solve the instability problem of 4-Butyl Resorcinol and to allow for easy use. It can be dissolved directly in water. Can be absorbed into the skin well. and has good stability

4-Butyl Resorcinol was tested to compare its whitening efficiency (anti-tyrosinase inhibition) compared to hydroquinone and other whitening substances at the clinical test level.

Please see additional research results in the attached document.

Methods: The researchers compared the following compounds:

• 4-n-butylresorcinol
• Hydroquinone
• Arbutin
• Kojic acid

They evaluated the compounds using:

1. A biochemical assay measuring inhibition of human tyrosinase activity
2. Inhibition of melanin production in MelanoDerm artificial skin models
3. Clinical studies on human subjects with age spots

Results:

Human Tyrosinase Inhibition Assay:

• 4-n-butylresorcinol was by far the most potent inhibitor with an IC50 of 21 μmol/L
• Kojic acid was moderately effective with an IC50 of ~500 μmol/L
• Arbutin and hydroquinone were weak inhibitors with IC50 values in the millimolar range

MelanoDerm Skin Model Assay:

• 4-n-butylresorcinol was most potent, inhibiting melanin production with an IC50 of 13.5 μmol/L
• Hydroquinone was surprisingly effective with an IC50 < 40 μmol/L, despite weak tyrosinase inhibition.
• Kojic acid had an IC50 > 400 μmol/L.
• Arbutin was least effective with an IC50 > 5000 μmol/L

Clinical Studies: Study 1:

• Compared 0.3% 4-n-butylresorcinol, 0.3% 4-hexylresorcinol, and 0.5% 4-phenylethylresorcinol applied to age spots twice daily
• 4-n-butylresorcinol showed significant lightening effects after 8 weeks
• The other compounds showed significant effects only after 12 weeks.

Study 2:

• Applied 1% 4-n-butylresorcinol to age spots using a spot applicator.
• Visible lightening was observed after 4 weeks of treatment
• Improvement continued over 16 weeks, with some spots becoming indistinguishable from surrounding skin
• Lightening effects persisted for at least 4 weeks after stopping treatment

Discussion of Individual Compounds:

Hydroquinone:

• Considered the "gold standard" for hyperpigmentation treatment, but has safety concerns
• Banned in EU cosmetics, still available OTC in US up to 2% concentration
• Very weak human tyrosinase inhibitor in this study
• Effective in skin models, likely due to cytotoxic effects rather than enzyme inhibition

Arbutin:

• Considered a tyrosinase inhibitor, but showed very weak effects in this study
• Activity depends on release of hydroquinone, raising safety concerns
• EU Scientific Committee considers it unsafe for cosmetic use

Kojic Acid:

• Moderately effective tyrosinase inhibitor
• Shows steep dose-response curve in skin models, explaining limited in vivo efficacy
• Now considered safe up to 1% in cosmetics by EU and US regulators

4-n-butylresorcinol:

• Most potent inhibitor of human tyrosinase and melanin production in this study
• Part of a class of 4-substituted resorcinols known to be powerful tyrosinase inhibitors
• Showed fastest onset and highest degree of age spot lightening in clinical studies
• Continued improvement over 16 weeks of treatment
• Effects persisted for weeks after stopping treatment

Key Conclusions:

1. 4-n-butylresorcinol is a highly effective inhibitor of human tyrosinase, far exceeding the potency of hydroquinone, arbutin, and kojic acid.
2. It shows strong efficacy for lightening age spots and other hyperpigmentation in clinical studies.
3. The in vitro potency of tyrosinase inhibitors does not always correlate with in vivo efficacy, as seen with hydroquinone.
4. Many published tyrosinase inhibition studies use mushroom tyrosinase, which does not accurately predict effects on human tyrosinase.
5. Safety concerns exist for hydroquinone and arbutin due to potential release of hydroquinone.
6. 4-n-butylresorcinol appears to be a promising and effective ingredient for managing skin hyperpigmentation disorders.

Limitations and Considerations:

• The study was conducted by researchers employed by Beiersdorf AG, a skincare company.
• Long-term safety data for 4-n-butylresorcinol is not presented.
• The clinical studies had relatively small sample sizes.
• Direct comparisons to hydroquinone were not made in the clinical studies.

In conclusion, this research suggests that 4-n-butylresorcinol is a highly effective tyrosinase inhibitor with demonstrated clinical efficacy for treating hyperpigmentation. It appears to be more potent than several commonly used skin lightening agents. However, as with any cosmetic ingredient, further research on long-term safety and efficacy in larger populations would be beneficial. The study provides valuable data on the comparative effectiveness of several skin lightening compounds and highlights the importance of using human enzyme and skin models when evaluating potential ingredients for hyperpigmentation treatments.

Usage: Can be used in all types of Whitening products.

Mixing method: Dissolve in water.

Usage rate: 1.0-10.0%

Product appearance: Light yellow-brown liquid.

Solubility: Can dissolve in water

Storage: For long-term storage Store in the refrigerator at 6 °C -8 °C, avoid light and moisture. At least 2 years old

INCI Name : Water(Aqua), PEG-20 Hydrogenated Castor Oil, 4-Butylresorcinol (13.5%), Butylene Glycol, Lecithin, 1,2-Hexanediol, Tocopheryl Acetate