α-Arbutin (CAS: 84380-01-8)：Its PhysioChemical Properties and Application Scenarios

Seebio biotech, in its pursuit of skin whitening and healthcare solutions, strives to discover high-quality ingredients that exhibit remarkable efficacy, safety, and gentleness. α-Arbutin, in comparison to traditional hydroquinone-based whitening agents, possesses outstanding advantages. Boasting excellent whitening capabilities, high safety standards, and a gentle nature, it has emerged as a widely utilized agent in the cosmetics and pharmaceutical industries.

 

 

 

 

 

Product Advantages

 

Remarkable Whitening Effect: Alpha arbutin, a distinct isomer of arbutin, possesses a whitening effect approximately 10 times greater than β-arbutin. It can significantly inhibit tyrosinase activity at minimal concentrations, thereby preventing melanin formation and achieving a noteworthy whitening effect.

 

High Safety: Alpha arbutin maintains its safety and efficacy even at higher concentrations, surpassing β-arbutin. The EU's Scientific Committee on Consumer Safety (SCCS) recently affirmed its safety in facial care products at concentrations no greater than 2% and in body care products at 0.5% or less.

 

Gentle Nature: The molecular structure of Alpha arbutin ensures a relatively mild effect with minimal irritation. It can be effective even at low concentrations, without causing severe irritation to skin tissue.

 

Antioxidant and Anti-Inflammatory Properties: Alpha arbutin also possesses mild antioxidant and anti-inflammatory qualities, further contributing to skin health.

 

Wide Applicability: Alpha arbutin is suitable for incorporation in high-end cosmetics and can be formulated into skin creams, freckle creams, premium pearl creams, and more. It not only enhances skin care but also provides anti-inflammatory and anti-irritant benefits.

 

Excellent Stability: Though Alpha arbutin decomposes in acidic environments, it retains good stability and is not prone to hydrolysis. It blends effortlessly with other formula ingredients, both in warm (70°C) and cold conditions. Within a pH range of 4-6.5, it remains more stable than other whitening ingredients in various dosage forms, including liquids, emulsions, ointments, gels, films, and aerosols.

 

 

Advantages over Hydroquinone Whitening Agent

 

Superior Safety: α-Arbutin exhibits low toxicity and minimal irritation upon application. Conversely, while hydroquinone offers significant depigmenting effects, it poses potential chronic adverse reactions like exogenous Chloasma, cataracts, and DNA damage, rendering its use potentially hazardous.

 

Exceptional Whitening Effect: α-Arbutin has proven to deliver excellent whitening results. Although hydroquinone possesses a robust depigmenting effect, α-Arbutin can achieve comparable outcomes while circumventing undesirable side effects.

 

 

 

Cosmetics Industry Application

 

Enhanced Stability: α-arbutin generally exhibits greater stability in cosmetic formulations, thereby ensuring the product's long-term efficacy and stability.

 

α-arbutin is a pivotal ingredient in a range of whitening and spot-reducing formulations, spanning serums, creams, and lotions. This composition is meticulously formulated with a blend of components, including nicotinamide, ascorbyl glucoside, and tranexamic acid, to achieve a multi-faceted synergistic whitening effect. Among these, α-arbutin stands out for its unique ability to reduce melanin production and pigmentation by inhibiting tyrosinase activity.

 

 

When α-arbutin collaborates with nicotinamide, tranexamic acid, and ascorbyl glucoside, it synergistically inhibits the production and transportation of melanin granules. This results in a significant reduction in pigmentation, the dilution of existing spots, and an improvement in the overall brightness of the skin. This comprehensive whitening and spot-reducing mechanism grants the composition a distinct advantage in the field of skin care.

 

Moreover, α-arbutin plays a crucial role in another specialized repair solution focused on whitening and freckle removal. This solution employs α-arbutin and sodium ascorbyl phosphate as the primary anti-freckle ingredients, complemented by tocopherol and dipotassium glycyrrhizinate, to create a robust whitening and anti-freckle system. The solution possesses a soft and luxurious texture that significantly enhances the transdermal absorption of anti-freckle actives. α-Arbutin penetrates deeply into the skin, maximizing its whitening and freckle-reducing effects, thereby significantly amplifying the overall whitening efficacy of the repair solution.

 

 

Pharmaceutical Industry Application

 

Anti-Inflammatory Function

Arbutin possesses notable anti-inflammatory properties, demonstrating strong anti-inflammatory effects across various experimental models. In studies focusing on anti-ovalbumin-induced allergic rhinitis (AR) in mice, arbutin significantly reduced nose rubbing and sneezing frequencies, lowered IgE, histamine, and malondialdehyde levels, and noticeably improved tissue structure and inflammation.

 

Moreover, arbutin enhances autophagy by activating Sirt1, thus effectively inhibiting inflammation and apoptosis. A study on adult retinal pigment epithelial (ARPE-19) cells revealed that arbutin significantly increased cell viability and autophagy mediators, reduced the expression of pro-inflammatory proteins, and decreased apoptosis under high glucose exposure. This effect was confirmed to be mediated by Sirt1.

 

Additionally, α-arbutin has been proven to alleviate lipopolysaccharide (LPS)-induced lung injury. Through the Sirt1/Nrf2/NF-κBp65 pathway, α-arbutin can decrease the levels of inflammatory cytokines like tumor necrosis factor α (TNF-α), interleukin 1β (IL-1β), and interleukin 6 (IL-6). Furthermore, α-arbutin lowers oxidative stress markers (such as malondialdehyde (MDA)) and elevates the activity of superoxide dismutase (SOD), indicating its dual antioxidant and anti-inflammatory benefits.

 

Antioxidative Stress Function

Arbutin exhibits remarkable anti-oxidative stress and neuroprotective effects, particularly in response to cortical neuron damage induced by hypoxia and glucose deficiency in rats. Studies have shown that under conditions of ischemic injury from hypoxia/glucose deprivation (OGD) and reoxygenation (R), rat cortical neurons experience significant damage to their antioxidant defense system, leading to lipid peroxidation and inflammatory factors, thereby compromising neuronal survival. Arbutin can prevent peroxidation, mitigate inflammatory reactions, and enhance the antioxidant activity of OGD/R-cultured neurons, for instance, by increasing levels of antioxidants like glutathione, superoxide dismutase, and catalase.

 

A separate study further underscores arbutin's antioxidant properties, effectively mitigating ischemia/reperfusion injury in rat testes. Using an experimental testicular torsion (T/D)-induced testicular injury model, researchers explored the effects of arbutin administration on oxidative stress, inflammation, endoplasmic reticulum (ER) stress, and apoptosis. In the T/D group, levels of oxidative stress, inflammation, ER stress, and apoptosis were significantly elevated compared to the control group. However, upon administering various doses of arbutin, testicular I/R injury was notably reduced in a dose-dependent manner. Histological data further validated these biochemical findings.

 

 

 

References:

 

1. Tao Zhang, et al.Anti-inflammatory and antiallergic activity of arbutin against ovalbumin-induced allergic rhinitis in mice through the modulation of inflammatory responses. Pulmonary Pharmacology & Therapeutics

2. Chaoting Ma, et al.Arbutin Inhibits Inflammation And Apoptosis By Enhancing Autophagy Via Sirt1. Tissue and Cell

3. Jinyan Ye, et al.Arbutin attenuates LPS-induced lung injury via Sirt1/ Nrf2/ NF-κBp65 pathway.. Acta Pharmaceutica

4. Elif Ayazoglu Demir, et al.Arbutin Abrogates Testicular Ischemia/Reperfusion Injury in Rats Through Repression of Inflammation. Tissue and Cell

5. Jingjing Tan, et al.Neuroprotective Effects Of Arbutin Against Oxygen And Glucose Deprivation-Induced Oxidative Stress. Acta Pharmaceutica