Ascorbyl Glucoside Research Articles

Safety Assessment of Ascorbyl Glucoside and Sodium Ascorbyl Glucoside as Used in Cosmetics.

The Expert Panel for Cosmetic Ingredient Safety (Panel) reviewed the safety of Ascorbyl Glucoside and Sodium Ascorbyl Glucoside in cosmetic products. These ingredients are reported to have the following functions in cosmetics: antioxidant, and skin-conditioning agent-miscellaneous. The Panel reviewed data relevant to the safety of these ingredients in cosmetic formulations, and concluded that Ascorbyl Glucoside and Sodium Ascorbyl Glucoside are safe in cosmetics in the present practices of use and concentration described in this safety assessment.

A novel fluorescence sensor film for hydroquinone based on a graphene quantum dots-nano activated carbon composite

A novel film sensor, composed of graphene quantum dots-nano activated carbon, chitosan, and PVA, offers a simple and effective hydroquinone (HQ) detection. This film exhibits impressive HQ adsorption under ambient conditions (room temperature, pH 7, 3 h) and utilizes a readily observable fluorescence color change for quantification. Upon HQ binding, the film's fluorescence color shifts from yellow-green to blue, enabling a linear detection range of 1.0–150 mg⋅L−1 based on intensity analysis of the blue component (B value). Calibration curves generated on the same day (n = 3) exhibit high precision, with standard deviations of the linear equation parameters below 0.014 and a low detection limit of 0.5 mg⋅L−1. The film exhibits exceptional stability, retaining its color and performance for up to 20 days. This stability is further corroborated by recovery experiments utilizing HQ-spiked water samples at concentrations of 2.5 mg⋅L−1 and 40 mg⋅L−1, where recoveries of 106 % and 95 % were achieved, respectively. These results demonstrated the sensor's reliable quantification capabilities. Notably, the sensor exhibited insignificant interference from commonly co-existing substances such as ethanol, ascorbyl glucoside, arbutin, kojic acid, and methylene blue. However, Cu²⁺, Fe³⁺, and catechol did cause some interference. This versatility, coupled with its straightforward operation, makes the film sensor a promising candidate for on-site HQ detection in diverse environmental monitoring applications.

Tuning multiple enzyme-like activities by metal doping for identification and quantitation of antioxidants in cosmetics

Inspired by the hydrolysis behaviors of skin cells, we exquisitely designed and synthesized a class of hydrolase mimics to develop an analytical method that can both identify and quantity antioxidant components in skin-whitening cosmetics, including ascorbic acid (AA) and its glycoside and phosphate derivatives. A series of ultra-thin Cu1-xMnxO2 or Fe1-yMnyO2 with rich acid-base pairs were prepared via chemical deposition and in-situ CuI/FeII self-assembly. H218O and D216O isotopic labeling studies and density function theory (DFT) calculations were adopted to analyze the cleaving sites of ascorbyl phosphate (AAL)/ascorbyl glucoside (AAP) and confirm that H2O was involved in the new bonds. In-situ DRIFT NH3-IR and −TPD further confirmed that the Fe- or Cu-substitution could increase the quantity and strength of Brønsted and Lewis acid sites. A cascade catalytic fluorescence sensor was designed for selective recognition or quantification of AA and its derivatives, which presents ultra-high-precision (≤2.5 %), stability, and selectivity in testing the target ingredients of five cosmetics from the market. Our nanozymes exhibit higher catalytic efficiency of 17.1 s−1 for AA, 8.42 s−1 for AAL, and 3.32 s−1 for AAP, which are 5.6 ∼ 32.8-fold higher than those of their mimic proteases. This work provides a controllable methodology to design hydrolytic nanozymes, which sheds light on biomimetic engineering and paves the way for breakthroughs in cosmetics industrial applications in the future.

A Bayesian network meta-analysis of 14 molecules inhibiting UV daylight-induced pigmentation.

Hyperpigmentation disorders are very frequent, affect the quality of life and may become a psychological burden for afflicted patients. Many anti-pigmenting or depigmenting agents are available with various efficacy and almost no comparative data. 2-mercaptonicotinoyl glycine (2-MNG) was recently proposed as a viable candidate showing safe and effective results on hyperpigmentation control invitro and invivo. A Bayesian network meta-analysis (BNMA) was conducted to map and rank the anti-pigmenting and depigmenting efficacy of 2-MNG 0.5% on UV daylight (UVDL)-induced pigmentation together with 13 other reference molecules. A comparison in the kinetics of 2-MNG 0.5% was also performed. Fourteen studies were conducted, for each, on 15-30 women of skin phototype III in Shanghai, China and Paris, France. The products were applied on mini zone, in randomized and blinded protocol, on the back, 5 days a week during 6 weeks, at a dose of 4 mg/cm2. During the second week, volunteers were exposed under to varying minimum erythemal dose of UVDL during 4 consecutive days-adapted to obtain a similar induction of skin pigmentation regardless of the population. Assessments were performed instrumentally using Chromameter®. Ascorbic acid 7% was used as a positive control for all experiments. A Bayesian network meta-analysis was then established to map and follow the kinetics of 2-MNG 0.5% performance with 13 reference molecules (glutathione 2%, kojic acid 1%, hydroquinone 4%, ascorbyl glucoside 2%, niacinamide 4%, etc.). 2-MNG 0.5% dominated the ranking at all time points with a significant high probability of strong efficacy against UVDL-induced pigmentation. Ascorbic acid 7% ranks second after 4 days of irradiations (D12) whereas hydroquinone 4% ranks second 1 month after irradiations (D40). In the kinetics, 2-MNG at 0.5% was effective as from the end of irradiations (D12) to the study endpoint (D40). This suggested an immediate and persistent efficacy across all timepoints evaluated. The BNMA revealed a rapid and lasting efficacy of 2-MNG 0.5% on the anti-pigmenting and depigmenting phases of the clinical protocol. 2-MNG 0.5% ranked first, with immediate and lasting effect compared to 13 other references. This study is the first allowing comparison between reference anti-pigmenting and depigmenting agents and will help clinicians for proposing the most effective approach for their patients.

Comparative Studies on the Photoreactivity, Efficacy, and Safety of Depigmenting Agents.

Depigmenting products are increasingly used to counteract skin hyperpigmentation and related psychosocial issues. This study aimed to compare different depigmenting agents-4-butylresorcinol; bakuchiol; tranexamic acid; ascorbyl glucoside; α-arbutin; and ascorbic acid-for photoreactivity; tyrosinase inhibition; and safety. Photoreactivity was assessed using the Reactive Oxygen Species assay. In vitro tyrosinase inhibition was compared, and cell viability was assessed in B-16V melanocytes to evaluate safety. Results showed 4-butylresorcinol, ascorbyl glucoside, and α-arbutin are non-photoreactive, while for ascorbic acid and bakuchiol it was not possible to reach conclusive results due to the lack of specificity of the ROS assay. 4-Butylresorcinol, acting as a competitive inhibitor, displayed potent tyrosinase inhibition, followed by ascorbic acid and bakuchiol. Both 4-butylresorcinol and bakuchiol reduced cell viability in a concentration-dependent manner. The insights obtained in this work support the development of depigmenting products by providing useful scientific guidance on the photostability, tyrosinase inhibitory efficacy, and skin safety of depigmenting agents.

Metabolic profiles of Sri Lankan cassava mosaic virus-infected and healthy cassava (Manihot esculenta Crantz) cultivars with tolerance and susceptibility phenotypes

BackgroundCassava mosaic disease (CMD) of cassava (Manihot esculenta Crantz) has expanded across many continents. Sri Lankan cassava mosaic virus (SLCMV; family Geminiviridae), which is the predominant cause of CMD in Thailand, has caused agricultural and economic damage in many Southeast Asia countries such as Vietnam, Loas, and Cambodia. The recent SLCMV epidemic in Thailand was commonly found in cassava plantations. Current understanding of plant–virus interactions for SLCMV and cassava is limited. Accordingly, this study explored the metabolic profiles of SLCMV-infected and healthy groups of tolerant (TME3 and KU50) and susceptible (R11) cultivars of cassava. Findings from the study may help to improve cassava breeding, particularly when combined with future transcriptomic and proteomic research.ResultsSLCMV-infected and healthy leaves were subjected to metabolite extraction followed by ultra-high-performance liquid chromatography high-resolution mass spectrometry (UHPLC-HRMS/MS). The resulting data were analyzed using Compound Discoverer software, the mzCloud, mzVault, and ChemSpider databases, and published literature. Of the 85 differential compounds (SLCMV-infected vs healthy groups), 54 were differential compounds in all three cultivars. These compounds were analyzed using principal component analysis (PCA), hierarchical clustering dendrogram analysis, heatmap analysis, and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway annotation. Chlorogenic acid, DL-carnitine, neochlorogenic acid, (E)-aconitic acid, and ascorbyl glucoside were differentially expressed only in TME3 and KU50, with chlorogenic acid, (E)-aconitic acid, and neochlorogenic acid being downregulated in both SLCMV-infected TME3 and KU50, DL-carnitine being upregulated in both SLCMV-infected TME3 and KU50, and ascorbyl glucoside being downregulated in SLCMV-infected TME3 but upregulated in SLCMV-infected KU50. Furthermore, 7-hydroxycoumarine was differentially expressed only in TME3 and R11, while quercitrin, guanine, N-acetylornithine, uridine, vorinostat, sucrose, and lotaustralin were differentially expressed only in KU50 and R11.ConclusionsMetabolic profiling of three cassava landrace cultivars (TME3, KU50, and R11) was performed after SLCMV infection and the profiles were compared with those of healthy samples. Certain differential compounds (SLCMV-infected vs healthy groups) in different cultivars of cassava may be involved in plant–virus interactions and could underlie the tolerance and susceptible responses in this important crop.

Design and development of raw clay-based formulations emulsions loaded with ascorbyl glucoside, in vitro evaluations on topical delivery and cell viability

Clays are layered materials with several unique features, which lead to many useful applications for natural products. In particular, raw clay has been increasingly utilized in skin care products and major advances have been achieved in the research and innovation related to these materials. This scientific manuscript addresses topical applications that include the development of O/W emulsions containing two types of raw clay such as kaolinite and sodium smectite associated with ascorbyl glucoside. The topical formulations were submitted to in vitro assays such as release, permeability using human cadaver skin as well as a skin retention study. The results of the release study showed that ascorbyl glucoside was delivered by the five formulations of this study. However, the skin permeation study of ascorbil glucoside showed that the formulation with smectite clay had a higher permeation and retention of AA2G in the skin layers suggesting that the smectitic clay (W4) acts as a promising permeation enhancer for this cosmetic active. Additionally, no cytotoxicity was detected in HaCaT and HDF cell lines, highlighting the safe character of the formulations, at least at short-term.

Preparation and evaluation of ascorbyl glucoside and ascorbic acid solid in oil nanodispersions for corneal epithelial wound healing

The objective of this study was to develop and evaluate an effective topical formulation to promote corneal epithelial wound healing. Ascorbyl glucoside (AA-2G), a stable prodrug of AA, was formulated in solid in oil (S/O) nanodispersions by emulsifying AA-2G solutions in cyclohexane using Span 85 as an emulsifying agent and freeze-drying emulsions to produce AA-2G – surfactant complex. The complexes were then dispersed in castor oil to produce S/O nanodispersions which were evaluated in terms of their particle size, polydispersity index, encapsulation efficiency, morphology, physical stability as well as the transcorneal permeation and accumulation of AA-2G. The same preparation procedure was used to prepare S/O nanodispersions of AA. S/O nanodispersions of AA and AA-2G were formulated into oily drops that were tested for efficacy in promoting wound healing after corneal epithelial depredation.AA-2G was loaded efficiently in S/O nanodispersions (EE > 99%) in the form of spherical nanoparticles. S/O nanodispersions were physically stable and resulted in improved permeation (18x) and accumulation (7x) of AA-2G in transcorneal diffusion experiments in comparison to AA-2G solutions. Oily eye drops of AA-2G and AA showed no irritation and significant improvement in epithelial healing in vivo in comparison to AA-2G and AA solutions.

Rapid determination of 22 functional components in cosmetics using ultra-high performance liquid chromatography-linear ion trap/orbitrap high resolution mass spectrometry

建立了超高效液相色谱-线性离子阱/静电场轨道阱高分辨质谱法同时测定化妆品中的22种功效成分。样品采用甲醇超声提取,C18色谱柱(100 mm×2. 1 mm, 1. 8 μm)分离,以0.1%(v/v)甲酸水溶液和乙腈为流动相进行梯度洗脱。在正离子模式下,以保留时间和一级母离子精确质量数进行定量分析,以高能碰撞诱导解离获得的二级碎片离子精确质量数进行确证。结果表明,该方法线性关系良好,检出限(LOD)为0.003~2.01 mg/kg;定量限(LOQ)为0.02~4.36 mg/kg;水、乳、霜3种基质中3个添加水平的回收率范围为63.2%~125.1%,相对标准偏差为0.18%~10.9%。对标示含有烟酰胺、抗坏血酸葡糖苷、咖啡因、泛醇及甘草类(光果甘草根茎叶、甘草根、胀果甘草根)、麦冬根、人参根、黄芪根、虎杖根、苦参根、地黄根、积雪草、茶叶提取物的54批样品进行检测,标示单体功效成分的样品均有检出,标示不同植物提取物的46批样品中,24批检出植物提取物的功效成分。该方法简便快速、定性定量可靠,适用于化妆品中22种功效成分的定量测定。

Spectroscopic and tensiometric considerations on anionic surfactants (SDS) and ascorbic acid/ascorbates interactions

The cosmetics and personal care products market is developing dynamically and the formulations of products are subject to numerous modifications due to consumer expectations and market trends. An increase in demand for products containing ascorbic acid or its more stable forms has been observed for several years. In this study, the correlation between SDS and ascorbic acid or its derivatives in aqueous solutions was assessed using spectroscopic and tensiometric methods. The influence of SDS interactions on the total antioxidant capacity of ascorbic acid/ascorbic acid derivatives was analyzed. The highest FRAP values of SDS-AA2G and SDS-EAC systems (0.17 and 2.71 mmol Fe2+/g, respectively) were at SDS concentration of 0.40 mM and were much higher than the ones of pure ascorbic acid derivatives. Based on the surface tension isotherms and Szyszkowski's equation, it was found that for the tested SDS/ascorbic acid, ascorbyl glucoside and 3-O-ethyl ascorbic acid systems, the CMC values were: 3.85, 2.54 and 3.31 mmol/dm3. There was also an influence on the values of the adsorption parameters, i.e. the surface excess at the saturated interface, the minimum molecular area in the adsorption layer at the saturated interface and the Gibbs free energy of adsorption. Moreover, in most of the analyzed cases, the tested systems had better wetting properties, which resulted in lower values of the contact angle than in the case of pure SDS solution.

Study of interaction between cationic surfactant (CTAB) and ascorbic acid/ascorbic acids derivatives by tensiometric and spectroscopic methods

The interactions between the cationic surfactant-cetyltrimethylammonium bromide (CTAB) and ascorbic acid and its derivatives in an aqueous media were investigated by using tensiometric and spectroscopic methods. On the basis of the surface tension isotherms, the values of the critical micelle concentration were determined also the adsorption parameters (the Gibbs free energy of adsorption, the surface excess at the saturated interface, the minimum molecular area in the adsorption layer at the saturated interface) were calculated using the Szyszkowski equation. The charged pseudophase model was adopted for define the Gibbs free energy of micellization. The infrared analysis (FTIR) contributed to the estimation of the possibility of the existence of interactions prevailing in the analyzed systems. The effect of CTAB-ascorbic acid/ascorbic acid derivatives interactions on their antioxidant activity was analyzed. Sets of ascorbic acid, 3-O-ethyl ascorbic acid and ascorbyl glucoside solutions differing in CTAB concentration were prepared. For the total antioxidant capacity determination, the Ferric Reducing Antioxidant Power (FRAP) assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH•) assay were used. The results obtained for CTAB - ascorbic acid/ascorbic acid derivatives systems were compared with the ones obtained for pure antioxidants.

Design and Characterization of Ascorbyl Glucoside loaded Solid Lipid Nanoparticles to improve skin penetration

Design and Characterization of Ascorbyl Glucoside loaded Solid Lipid Nanoparticles to improve skin penetration

18708 Comparative pharmacokinetic evaluation of delivery of three different vitamin C molecules in target tissues: Ascorbyl glucoside, nanoencapsulated vitamin C, and acid ascorbic

Background: Ascorbyl glucoside is a vitamin C precursor. It is an ascorbic acid (AA) molecule with an additional C2-glucose, more chemically stable, metabolized into AA by alpha-glucosidase in dermis and epidermis, with a considerable reservoir effect, and associated with gradual delivery.

17129 Comparative analysis of clinical benefits provided by two facial daily care regimens with the antioxidants ascorbyl glucoside and tocopheryl glucoside for 8 weeks in Brazilian women

Background: The well known instability of vitamin C to thermal and oxidative degradation stimulated the research for more stable molecules with gradual release and effect on the skin. Ascorbyl glucoside is a vitamin C precursor. It is an ascorbic acid molecule with an additional C2-glucose, more chemically stable which prevents the low effectiveness of vitamin C in the presence of different degradation mechanisms. In addition, tocopheryl glucoside is a vitamin E precursor metabolized into free tocopherol in the skin, with a considerable reservoir effect, associated with gradual delivery.

Simultaneous Analysis of Hydroquinone, Arbutin, and Ascorbyl Glucoside Using a Nanocomposite of Ag@AgCl Nanoparticles, Ag2S Nanoparticles, Multiwall Carbon Nanotubes, and Chitosan.

A nanocomposite comprising Ag nanoparticles on AgCl/Ag2S nanoparticles was decorated on multi-walled carbon nanotubes and used to modify a glassy carbon electrode. Chitosan was also formulated in the nanocomposite to stabilize Ag2S nanoparticles and interact strongly with the glucose moiety of arbutin (AR) and ascorbyl glucoside (AA2G), two important ingredients in whitening lotion products. The modified electrode was characterized by Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), and scanning electron microscopy (SEM) and cyclic voltammetry and used for the simultaneous analysis of hydroquinone (HQ), AR, and AA2G. The electrode showed excellent electrocatalysis towards the analytes by shifting the anodic peak potential to a negative direction with ≈5-fold higher current. The sensor displayed a linearity of 0.91–27.2 μM for HQ, 0.73–14.7 μM for AR, and 1.18–11.8 μM for AA2G, without cross-interference. A detection limit was 0.4 μM for HQ, 0.1 μM for AR, and 0.25 μM for AA2G. The sensor was applied to determine HQ, AR, and AA2G spiked in the whitening lotion sample with excellent recovery. The measured concentration of each analyte was comparable to that of the high performance liquid chromatographic (HPLC) method.

Simultaneous determination of magnesium ascorbyl phosphate, ascorbyl glucoside, kojic acid, arbutin and hydroquinone in skin whitening cosmetics by HPLC

A high performance liquid chromatographic method was developed for simultaneous determination of 5 whitening ingredients: magnesium ascorbyl phosphate, ascorbyl glucoside, kojic acid, arbutin and hydroquinone decomposed from arbutin in cosmetics. Samples were extracted with 0.05 M KH2PO4 buffer solution (pH 2.5) and analyzed using a Cosmosil 5 C18-AR-II column. A mixture of 0.05 M KH2PO4 buffer solution (pH 2.5) and methanol (99:1, v/v) was used as mobile phase. The UV detector was set at 280 nm. Pyridoxine was used as an internal standard. The related coefficients, R2, of regression equations of the 5 standard curves were 0.9998-1.0000. The relative standard deviations of the 5 ingredients for intraday and interday analysis were less than 2.4%. The average recoveries of these 5 ingredients spiked in sample ranged from 93.5% to 103.3%. The relative standard deviations of average recoveries were less than 1.3%. The limits of quantitation in cosmetics were 80.0, 20.0, 3.0, 15.0 and 10.0 μg/mL for magnesium ascorbyl phosphate, ascorbyl glucoside, kojic acid, arbutin and hydroquinone, respectively.

Ex vivo evaluation of the penetration and content of L-ascorbic acid and ascorbyl glucoside of a novel topical facial serum

Ex vivo evaluation of the penetration and content of L-ascorbic acid and ascorbyl glucoside of a novel topical facial serum

Enhanced vitamin C skin permeation from supramolecular hydrogels, illustrated using in situ ToF-SIMS 3D chemical profiling

Vitamin C (ascorbic acid) is a naturally occurring, powerful anti-oxidant with the potential to deliver numerous benefits to the skin when applied topically. However, topical use of this compound is currently restricted by an instability in traditional formulations and the delivery and eventual fate of precursor compounds has been largely unexplored. Time of flight secondary ion mass spectrometry (ToF-SIMS) is an emerging technique in the field of skin research and offers detailed chemical analysis, with high mass and spatial resolution, as well as profiling capabilities that allow analysis as a function of sample depth. This work demonstrates the successful use of ToF-SIMS to obtain, in situ, accurate 3D permeation profiles of both ascorbic acid and a popular precursor, ascorbyl glucoside, from ex vivo porcine skin. The significant permeation enhancing effect of a supramolecular hydrogel formulation, produced from an amphiphilic gemini imidazolium-based surfactant, was also demonstrated for both compounds. Using ToF-SIMS, it was also possible to detect and track the breakdown of ascorbyl glucoside into ascorbic acid, elucidating the ability of the hydrogel formulation to preserve this important conversion until the targeted epidermal layer has been reached. This work demonstrates the potential of ToF-SIMS to provide 3D permeation profiles collected in situ from ex vivo tissue samples, offering detailed analysis on compound localisation and degradation. This type of analysis has significant advantages in the area of skin permeation, but can also be readily translated to other tissue types.

Effectiveness and safety of a novel topical depigmenting agent in epidermal pigmentation: an open-label, non-comparative study

<p class="abstract"><strong>Background:</strong> Active compounds isolated from plants are known to inhibit melanogenesis without melanocytotoxicity. The aim of this study was to assess the effectiveness and safety of a cream containing a combination of niacinamide, glycolic acid, vitamin E acetate, kojic acid, soy isoflavones, arbutin, pterowhite, licorice and ascorbyl glucoside for the treatment of epidermal pigmentation.</p><p class="abstract"><strong>Methods:</strong> Sixty subjects (between 18-45 years) with epidermal pigmentation were enrolled in this 12-week, open-label, non-comparative study. Clinical/dermoscopic aspects (grade-1: <25%; grade-2: 25-50%; grade-3: 50-75%; grade-4: >75% reduction in the amount of epidermal pigment); melanin index/erythema measure (Dermacatch); extent, depth and density of pigmentation (FotoFinder) and safety were assessed.<strong></strong></p><p class="abstract"><strong>Results:</strong> Out of 60 enrolled subjects, 53 completed the study. Overall percentage of melanin and erythema improvement (Dermacatch) was 24.2% and 7.4% respectively (p<0.05). Based on Fotofinder images, 13% had grade 4 improvement, 47% had grade 3 improvement, 30% had grade 2 improvement while 9% subjects had grade 1 improvement. On the basis of clinical photographic images, 15% had grade 4 improvements in the skin colour, 41% had grade 3, 34% had grade 2 and 9% subjects had grade 1 improvement. Adverse effect of skin irritation was reported in one subject, which resolved after discontinuing the treatment.</p><p class="abstract"><strong>Conclusions:</strong> Cream containing a combination of niacinamide 4.0%, glycolic acid 2.0%, vitamin E acetate 0.1%, kojic acid dipalmitate 2.0%, soy isoflavones 0.5%, arbutin 2.0%, pterowhite 0.12%, licorice 40% CA 0.12%, ascorbyl glucoside 0.1% was found to be safe and effective in the treatment of epidermal pigmentation.</p>

Real time and in vivo pharmaceutical and environmental studies with SpiderMass instrument

Remote Infrared Matrix Assisted Laser Desorption Ionization (Remote IR MALDI) system (SpiderMass) with endogenous water as matrix allows to perform real-time DMPK in vivo. In this work, SpiderMass was used to analyze the impact on metabolite production or release of invalidated pro-protein PC1/3 macrophages by Short RNA (shRNA) versus scramble shRNA with Paclitaxel. Time course in vivo experiments were then performed on the inner and outer faces of patients’ forearms or comedo treated with Melascreen (Ducray) containing ascorbyl glucoside. Finally, the impact of car pollution (emitted soot) on skin was also investigated. Taken together, we demonstrate that the SpiderMass instrument opens the door to clinical, pharmaceutical and environmental domains for real-time, in vivo pharmacokinetic (Drug Metabolism and PharmacoKinetics, DMPK) analysis.