Alpha Arbutin

As a dedicated manufacturer, we are proud to present our high-purity α-Arbutin, a naturally derived glucoside renowned for its exceptional skin-brightening and tone-evening properties. Backed by rigorous scientific research and advanced manufacturing processes, our α-Arbutin offers a superior alternative to traditional depigmenting agents, providing efficacy, stability, and a favorable safety profile for a wide range of skincare applications.

Main Effects And Functions

Whitening and Spot-Lightening
α-arbutin inhibits tyrosinase activity within melanocytes, reducing melanin production. This mechanism effectively achieves skin whitening and spot-lightening, supported by established scientific research.

Antioxidant
α-arbutin exhibits antioxidant properties by neutralizing free radicals. This activity helps mitigate oxidative stress, thereby contributing to the prevention of skin aging.

Melanin Inhibition
As a competitive inhibitor of tyrosinase, α-arbutin blocks melanin synthesis pathways, directly reducing skin pigmentation disorders.

Main Application Industries

Cosmetics Industry
Leveraging its proven whitening and antioxidant capabilities, α-arbutin is widely incorporated in skincare products. It targets skin aging and hyperpigmentation, such as freckles and melasma, aligning with regulatory safety guidelines (e.g., ≤2% concentration per CIR assessment).

Pharmaceutical Industry
Medical formulations containing α-arbutin, such as compound arbutin creams, are clinically used for treating pigmentary skin conditions. However, evidence for its efficacy in scar treatment remains limited.

Introduction

α-Arbutin and β-Arbutin are naturally occurring phenolic glycosides widely used as skin-brightening active ingredients in cosmetics and cosmeceuticals. Both are glucopyranoside derivatives of hydroquinone, where glucose and hydroquinone are linked via a glycosidic bond. However, due to the difference in the stereochemical configuration of the glycosidic linkage, they exhibit significant variations in their chemical properties, biological activities, stability, and safety profiles.

α-Arbutin (4-Hydroxyphenyl-α-D-glucopyranoside):

Chemical Structure: The glucose unit is linked to hydroquinone via an α-1,4-glycosidic bond. This α-glycosidic linkage configuration contributes to its higher stability under specific conditions.

Stability: Studies indicate that α-arbutin demonstrates good stability over a broad pH range, particularly under mildly acidic conditions (around pH 4.9), and is less prone to hydrolysis. Its stability under strong acid, strong base, and UV irradiation is also superior to that of β-arbutin. The reported half-life of approximately 77 months was determined under specific conditions, and formulation factors should be considered in practical applications.

Enzymatic Hydrolysis: While β-glucosidase can hydrolyze α-arbutin, the rate is generally much slower than that of β-arbutin hydrolysis, which helps minimize the risk of hydroquinone release.

β-Arbutin (4-Hydroxyphenyl-β-D-glucopyranoside):

Chemical Structure: The glucose unit is linked to hydroquinone via a β-1,4-glycosidic bond. The β-glycosidic linkage is relatively more susceptible to enzymatic or acid hydrolysis.

Stability: β-arbutin is more readily decomposed under strong acid, strong base, and UV irradiation, which limits its application in certain cosmetic formulations.

Enzymatic Hydrolysis: β-arbutin is a good substrate for β-glucosidase. In vitro experiments have shown that it readily releases hydroquinone upon interaction with β-glucosidase. Since β-glucosidase is also present in human skin, the use of β-arbutin carries a potential risk of hydroquinone release.

α-Arbutin:

Mechanism of Action: Primarily reduces melanin production by competitively inhibiting the activity of tyrosinase, a key enzyme in melanogenesis that catalyzes the oxidation of L-tyrosine to dopaquinone.

Inhibitory Strength: In vitro studies have demonstrated that α-arbutin exhibits significantly stronger tyrosinase inhibitory activity compared to β-arbutin, with reported values being approximately 10 times higher.

Anti-Melanogenic Activity: Cell-based assays and clinical studies have also confirmed that α-arbutin possesses a greater ability to inhibit melanin synthesis, about 15 times that of β-arbutin. This may be attributed to its more stable structure and potentially more effective cellular penetration.

β-Arbutin:

Mechanism of Action: Also exerts its whitening effect by inhibiting tyrosinase activity, but its efficacy is relatively weaker.

Safety Considerations: Due to its propensity to decompose and release hydroquinone, coupled with its weaker whitening effect, the application of β-arbutin in cosmetics is subject to more stringent restrictions.

α-Arbutin: Possesses multiple hydroxyl groups, contributing to its good water solubility, which is advantageous for its incorporation into water-based cosmetic formulations and absorption by the skin.

β-Arbutin: Similarly exhibits good water solubility, with no significant difference compared to α-arbutin in this aspect.

α-Arbutin:

Biosynthesis: The primary production method currently offering greater environmental friendliness and sustainability. Common approaches include:

Enzymatic Conversion: Utilizing specific glycosyltransferases (such as sucrose phosphorylase, α-glucosidase, etc.) to catalyze the reaction between hydroquinone and glucose or its derivatives, yielding α-arbutin. Optimization of enzyme sources and reaction conditions can enhance production efficiency and purity.

Microbial Transformation: Employing the metabolic pathways of certain microorganisms through fermentation processes to produce α-arbutin.

Chemical Synthesis: While chemical synthesis methods exist, they are less commonly employed due to complex procedures, higher costs, and the potential for byproduct formation.

β-Arbutin:

Chemical Synthesis: The main production method, typically involving the use of protecting groups and deprotection steps, with relatively harsh reaction conditions and the potential for isomer impurities.

α-Arbutin: Generally priced higher than β-arbutin due to its superior whitening efficacy, better stability, and the relatively higher production costs associated with biosynthesis.

β-Arbutin: The more established chemical synthesis methods result in lower production costs, hence its lower price point.

α-Arbutin:

Safety Assessment: The Cosmetic Ingredient Review (CIR) Expert Panel has assessed the safety of α-arbutin and concluded that it is safe for use in cosmetics at concentrations up to 2%, with no significant release of hydroquinone.

Toxicological Studies: Extensive toxicological studies support the safe application of α-arbutin within the recommended concentration range. Its structural stability minimizes the risk of hydroquinone release, thereby reducing potential skin irritation and uneven pigmentation.

β-Arbutin:

Safety Risks: Due to its greater susceptibility to hydrolysis and subsequent release of hydroquinone, a substance with potential skin irritancy and cytotoxicity, long-term or high-concentration use of β-arbutin may lead to adverse reactions, including skin inflammation, allergies, and abnormal pigmentation (e.g., leukoderma).

Regulatory Restrictions: In some countries and regions, stricter concentration limits have been imposed on the use of β-arbutin in cosmetics due to safety concerns.

In summary, α-arbutin demonstrates significant advantages over β-arbutin in terms of chemical structural stability, tyrosinase inhibitory potency, whitening efficacy, and safety profile. The adoption of biosynthesis methods for α-arbutin also aligns with sustainable development trends. Consequently, α-arbutin has become a more preferred and advantageous choice in the cosmetic industry, particularly for high-efficacy and safe skin-brightening products. However, the final selection should still consider factors such as product positioning, cost constraints, and regulatory requirements.

The stability of α-arbutin is primarily influenced by several key factors, including:

1. pH Value:

α-Arbutin exhibits greater stability in neutral to mildly acidic environments. Research indicates that optimal stability is achieved at a pH of 4.9, with a reported half-life of approximately 77 months. At a pH of 5.0, both the synthesis efficiency and stability of α-arbutin are also favorable. Conversely, exposure to strongly acidic or alkaline conditions may compromise its stability to some extent.

2. Light Exposure:

α-Arbutin demonstrates relative stability under daylight irradiation, as evidenced by the consistent chromatographic peak area over increasing exposure times. However, under ultraviolet (UV) irradiation, the chromatographic peak area of α-arbutin gradually decreases with prolonged exposure. Notably, hydroquinone formation was not detected in these experiments. Furthermore, higher concentrations of α-arbutin solutions (e.g., mass fraction of 0.06% and above) are susceptible to phenol decomposition under UV irradiation.

3. Temperature:

α-Arbutin is generally stable at room temperature, with temperature having a minimal impact on its stability within the range of 20°C to 60°C. Reaction conditions at 25°C have been found to yield the best synthesis efficiency and stability of α-arbutin.

4. Chemical Substances:

α-Arbutin demonstrates good stability in the presence of several common cosmetic matrix ingredients, such as methylparaben, fatty alcohol polyether-20, K3Na, and glycerin. Nevertheless, certain chemical substances or environmental conditions can affect its stability. For instance, exposure to strongly acidic, strongly alkaline, or strongly oxidizing environments may lead to a reduction in α-arbutin's stability.

5. Enzymatic Activity:

The synthesis and stability of α-arbutin are closely related to enzyme activity. For example, sucrose phosphorylase plays a crucial role in α-arbutin synthesis, and its activity is influenced by factors such as pH and temperature. During the biosynthesis process, the correct folding and conformation of the enzyme are essential for maintaining its activity, which directly impacts the synthesis efficiency and stability of α-arbutin.

Shaanxi Jiuyuan Biotechnology Co., Ltd. focuses on the production of plant extracts, health food raw materials, fruit and vegetable powders, food additives, and feed additives. The factory covers an area of more than 70,000 square meters, with 4 production workshops, 6 production lines, 1 R&D technology center, and multiple advanced testing equipment, from raw materials to finished products, to the greatest extent possible to ensure the quality of the product.
The company operates in strict accordance with GMP operating specifications and has multiple international certifications, which greatly reduces the risk of customers choosing us. We always adhere to technological innovation as the driving force, relying on a high-quality R&D team and advanced and sophisticated equipment, and are committed to providing customers with high-quality products and services.

As a dedicated manufacturer, we offer:

Competitive Pricing: Benefit from our efficient production processes and economies of scale.

Reliable Supply Chain: Ensure consistent and timely delivery for your production needs.

Comprehensive Technical Support: Our team of experts provides formulation guidance and technical assistance.

Stringent Quality Control: We are committed to delivering α-Arbutin of the highest purity and quality.

Global Regulatory Compliance: Our product meets international quality standards and regulatory requirements.

Partner with us to formulate innovative and effective skin-brightening products with our premium α-Arbutin. Contact us today for pricing, samples, and technical specifications. We look forward to building a successful partnership with you.

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