Agarose Stearate-Carbomer940 as Stabilizer and Rheology Modifier for Surfactant-Free Cosmetic Formulations.

Some commonly used surfactants in cosmetic products raise concerns due to their skin-irritating effects and environmental contamination. Multifunctional, high-performance polymers are good alternatives to overcome these problems. In this study, agarose stearate (AS) with emulsifying, thickening, and gel properties was synthesized. Surfactant-free cosmetic formulations were successfully prepared from AS and carbomer940 (CBM940) mixed systems. The correlation of rheological parameter with skin feeling was determined to study the usability of the mixed systems in cosmetics. Based on rheological analysis, the surfactant-free cosmetic cream (SFC) stabilized by AS-carbomer940 showed shear-thinning behavior and strongly synergistic action. The SFC exhibited a gel-like behavior and had rheological properties similar to commercial cosmetic creams. Scanning electron microscope images proved that the AS-CBM940 network played an important role in SFC's stability. Oil content could reinforce the elastic characteristics of the AS-CBM940 matrix. The SFCs showed a good appearance and sensation during and after rubbing into skin. The knowledge gained from this study may be useful for designing surfactant-free cosmetic cream with rheological properties that can be tailored for particular commercial cosmetic applications. They may also be useful for producing medicine products with highly viscous or gel-like textures, such as some ointments and wound dressings.

Cell Penetrating Peptide as a High Safety Anti-Inflammation Ingredient for Cosmetic Applications.

Cosmeceutical peptides have become an important topic in recent decades in both academic and industrial fields. Many natural or synthetic peptides with different biological functions including anti-ageing, anti-oxidation, anti-infection and anti-pigmentation have been developed and commercialized. Current cosmeceutical peptides have already satisfied most market demand, remaining: "cargos carrying skin penetrating peptide with high safety" still an un-met need. To this aim, a cell-penetrating peptide, CPPAIF, which efficiently transported cargos into epithelial cells was exanimated. CPPAIF was evaluated with cell model and 3D skin model following OECD guidelines without using animal models. As a highly stable peptide, CPPAIF neither irritated nor sensitized skin, also did not disrupt skin barrier. In addition, such high safety peptide had anti-inflammation activity without allergic effect. Moreover, cargo carrying activity of CPPAIF was assayed using HaCaT cell model and rapid CPPAIF penetration was observed within 30 min. Finally, CPPAIF possessed transepidermal activity in water in oil formulation without disruption of skin barrier. All evidences indicated that CPPAIF was an ideal choice for skin penetrating and its anti-inflammatory activity could improve skin condition, which made CPPAIF suitable and attractive for novel cosmeceutical product development.

Synthesis of Daidzein Glycosides, α-Tocopherol Glycosides, Hesperetin Glycosides by Bioconversion and Their Potential for Anti-Allergic Functional-Foods and Cosmetics.

Daidzein is a common isoflavone, having multiple biological effects such as anti-inflammation, anti-allergy, and anti-aging. α-Tocopherol is the tocopherol isoform with the highest vitamin E activity including anti-allergic activity and anti-cancer activity. Hesperetin is a flavone, which shows potent anti-inflammatory effects. These compounds have shortcomings, i.e., water-insolubility and poor absorption after oral administration. The glycosylation of bioactive compounds can enhance their water-solubility, physicochemical stability, intestinal absorption, and biological half-life, and improve their bio- and pharmacological properties. They were transformed by cultured Nicotiana tabacum cells to 7-ß-glucoside and 7-ß-gentiobioside of daidzein, and 3'- and 7-ß-glucosides, 3',7-ß-diglucoside, and 7-ß-gentiobioside of hesperetin. Daidzein and α-tocopherol were glycosylated by galactosylation with ß-glucosidase to give 4'- and 7-ß-galactosides of daidzein, which were new compounds, and α-tocopherol 6-ß-galactoside. These nine glycosides showed higher anti-allergic activity, i.e., inhibitory activity toward histamine release from rat peritoneal mast cells, than their respective aglycones. In addition, these glycosides showed higher tyrosinase inhibitory activity than the corresponding aglycones. Glycosylation of daidzein, α-tocopherol, and hesperetin greatly improved their biological activities.

Cornus mas L. extract as a multifunctional material for manufacturing cosmetic emulsions.

Dogwood fruits are a valuable source of active ingredients, such as phenolic compounds, vitamin C, iridoids, flavonoids and anthocyanins. Plant extracts and substances derived from latin Cornus mas L. exhibit not only strong antibacterial but also antioxidant and tonicity properties, effectively preventing the development of inflammation in living organisms. In the present study, we attempted to obtain the innovative, multi-functional plant extract from the fruit of dogwood (Cornus mas L.). During the extraction process a mixture of water, glycerol, and vegetable oil were used as an extractant. The usage of such mixtures of solvents enabled us to extract a variety of active substances, soluble in both water and oils. The obtained extracts were analyzed for their physicochemical and biochemical properties, in order to apply the extract in a body nutrient lotion. The results clearly showed that such extract could be an innovative and multi-functional raw material used in cosmetics industry.

Design and Characterization of Topical Formulations: Correlations Between Instrumental and Sensorial Measurements.

The interaction between cosmetic emulsions and the skin's surface is an important factor to consider in the development of topical formulations. Two important ingredients in cosmetic formulations are waxes and polymers. The physical and mechanical properties of formulations directly impact the interface skin-formulation. To evaluate this interaction, it is important to study the rheology, texture, and sensory properties. In this context, the aim of the study was to evaluate the influence of waxes and polymers on the rheological behavior, texture profile, and sensorial properties of topical formulations and the correlation between these parameters. The best combination of a wax and a polymer was determined by full factorial design of experiments and applied to develop eight formulations that were tested in relation to rheological, mechanical, and sensorial properties. The polymer helps with the spreadability of the formulation, and the wax had a strong influence on the parameters related to the structure of emulsions. A correlation between these parameters was observed. This way, it was possible to compare theoretical and practical data, except between the flow index and the work of shear. Finally, it was possible to predict sensorial aspects from rheological and texture parameters, making the formulation process easier and more integrated with all stages of the development of new topical formulations. Thus, the present study introduces a new proposal in the development of cosmetics.

Ecodesign of cosmetic formulae: methodology and application.

OBJECTIVE: This article describes an easy-to-use ecodesign methodology developed and applied since 2014 by the L'Oréal Group to improve the sustainable performance of its new products without any compromise on their cosmetic efficacy. METHODS: Cosmetic products, after being used, are often discharged into the sewers and the aquatic compartment. This discharge is considered as dispersive and continuous. A consistent progress in reducing the environmental impact of cosmetic products can be achieved through focusing upon three strategic indicators: biodegradability, grey water footprint adapted for ecodesign (GWFE) and a global indicator, complementary to these two endpoints. Biodegradability represents the key process in the removal of organic ingredients from the environment. GWFE is defined herein as the theoretical volume of natural freshwater required to dilute a cosmetic formula after being used by the consumer, down to a concentration without any foreseeable toxic effects upon aquatic species. Finally, the complementary indicator highlights a possible alert on formula ingredients due to an unfavourable environmental profile based on hazard properties: for example Global Harmonization System/Classification, Labelling and Packaging (GHS/CLP) H410 classification or potential very persistent and very bioaccumulative (vPvB) classification. RESULTS: The ecodesign of a new cosmetic product can be a challenge as the cosmetic properties and quality of this new product should at least match the benchmark reference. As shown in the case studies described herein, new methodologies have been developed to maximize the biodegradability of cosmetic formulae, to minimize their GWFE and to limit the use of ingredients that present an unfavourable environmental profile, while reaching the highest standards in terms of cosmetic efficacy. CONCLUSION: By applying these methodologies, highly biodegradable products (≥ 95% based on ingredient composition) have been developed and marketed, with a low GWFE. This new ecodesign approach shows that embedding sustainability in developing new cosmetic products can also open up new innovative opportunities.

Development of highly potent melanogenesis inhibitor by in vitro, in vivo and computational studies.

The present work describes the synthesis of few hydroxylated amide derivatives as melanogenesis inhibitors. In vitro, in vivo and computational studies proved that compound 6d is a highly potent melanogenesis inhibitor compared to standard kojic acid. The title amides 4a-e and 6a-e were synthesized following simple reaction routes with excellent yields. Most of the synthesized compounds exhibited good mushroom tyrosinase inhibitory activity, but compound 6d showed excellent activity (IC50 0.15 µM) compared to standard kojic acid (IC50 16.69 µM). Lineweaver-Burk plots were used for the determination of kinetic mechanism, and it was found that compounds 4c and 6d showed non-competitive inhibition while 6a and 6b showed mixed-type inhibition. The kinetic mechanism further revealed that compound 6d formed irreversible complex with the target enzyme tyrosinase. The Ki values determined for compounds 4c, 6a, 6b and 6d are 0.188, 0.84, 2.20 and 0.217 µM respectively. Results of human tyrosinase inhibitory activity in A375 human melanoma cells showed that compound 6d exhibited 91.9% inhibi-tory activity at a concentration of 50 µg/mL. In vivo cytotoxicity evaluation of compound 6d in zebrafish embryos showed that it is non-toxic to zebrafish. Melanin depigmentation assay performed in zebrafish indicated that compound 6d possessed greater potential in decreasing melanin contents compared to kojic acid at the same concentration. Computational studies also supported the wet lab findings as compound 6d showed a highest binding affinity with the target protein (PDBID: 2Y9X) with a binding energy value of -7.90 kcal/mol. Molecular dynamic simulation studies also proved that amide 6d formed the most stable complex with tyrosinase. Based upon our in vitro, in vivo and computational studies, we propose that compound 6d is a promising candidate for the development of safe cosmetic agent.

Biosynthesis of zinc oxide nanoparticles by petals extract of Rosa indica L., its formulation as nail paint and evaluation of antifungal activity against fungi causing onychomycosis.

Aim: The authors report the biological synthesis of zinc oxide nanoparticles (ZnO-NPs) from the petals extract of Rosa indica L. (rose). Its efficacy was evaluated against two dermatophytes: namely: Trichophyton mentagrophytes and Microsporum canis which cause onychomycosis. The activity of antibiotics against the tested dermatophytes was enhanced, when evaluated in combination with ZnO-NPs. Methods and results: The synthesised ZnO-NPs were preliminary detected by using ultraviolet UV visible spectroscopy, which showed specific absorbance. The ZnO-NPs were further characterised by nanoparticle tracking analysis (NTA), Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), X-ray diffraction and Zetasizer. Moreover, nanoparticles containing nail paint (nanopaint) was formulated and its antifungal activity was also assessed against T. mentagrophytes and M. canis. ZnO-NPs and formulated nanopaint containing ZnO-NPs, both showed significant antifungal activity. The maximum activity was noted against M. canis and lesser against T. mentagrophytes. Minimum inhibitory concentration of ZnO-NPs was also determined against the dermatophytes causing onychomycosis infection. Conclusion: ZnO-NPs can be utilised as a potential antifungal agent for the treatment of onychomycosis after more experimental trials.

Present Global Situation of Amino Acids in Industry.

At present, amino acids are widely produced and utilized industrially. Initially, monosodium glutamate (MSG) was produced by extraction from a gluten hydrolysate. The amino acid industry started using the residual of the lysate. The discovery of the functions of amino acids has led to the expansion of their field of use. In addition to seasoning and other food use, amino acids are used in many fields such as animal nutrients, pharmaceuticals, and cosmetics. On the other hand, the invention of the glutamate fermentation process, followed by the development of fermentation methods for many other amino acids, is no less important. The supply of these amino acids at a low price is very essential for their industrial use. Most amino acids are now produced by fermentation. The consumption of many amino acids such as MSG or feed-use amino acids is still rapidly increasing.

Designing new functional cosmetic ingredients from polyglycerol, a versatile bio-based platform for improved sustainability.

Polyglycerol (PG) is a well-known cosmetic ingredient and important precursor for the synthesis of a variety of cosmetic ingredients, such as surfactants, emulsifiers, and conditioning agents for hair and skin. When derived from renewable resources, PG can provide a more sustainable platform for the development of new ingredients with improved performance in cosmetic applications. This paper will discuss recent advances in the utilization of bio-based PG ingredients as alternatives to traditional ethoxylate chemistries for mild nonionic surfactants, substantive humectants, and micellar thickeners.

Enzymatic synthesis of bioactive compounds with high potential for cosmeceutical application.

Cosmeceuticals are cosmetic products containing biologically active ingredients purporting to offer a pharmaceutical therapeutic benefit. The active ingredients can be extracted and purified from natural sources (botanicals, herbal extracts, or animals) but can also be obtained biotechnologically by fermentation and cell cultures or by enzymatic synthesis and modification of natural compounds. A cosmeceutical ingredient should possess an attractive property such as anti-oxidant, anti-inflammatory, skin whitening, anti-aging, anti-wrinkling, or photoprotective activity, among others. During the past years, there has been an increased interest on the enzymatic synthesis of bioactive esters and glycosides based on (trans)esterification, (trans)glycosylation, or oxidation reactions. Natural bioactive compounds with exceptional theurapeutic properties and low toxicity may offer a new insight into the design and development of potent and beneficial cosmetics. This review gives an overview of the enzymatic modifications which are performed currently for the synthesis of products with attractive properties for the cosmeceutical industry.

Dermatitis alérgica de contacto a cosméticos, estudio clínico-epidemiológico en un hospital terciario / Allergic contact dermatitis due to cosmetics: A clinical and epidemiological study in a tertiary hospital

La dermatitis alérgica de contacto (DAC) a cosméticos es una dolencia con una incidencia creciente en la población, paralelamente a la generalización del uso de cosméticos en la sociedad, así como a su proliferación y diversificación. El objetivo del estudio es determinar la prevalencia de DAC a cosméticos en nuestro medio, analizar su evolución temporal y sus características clínico-epidemiológicas, así como definir los alérgenos y los cosméticos implicados. Se ha realizado un estudio prospectivo durante los años 2005-2013 en la Unidad de Alergia Cutánea del Hospital General Universitario de Valencia, y se ha comparado de forma retrospectiva con el periodo previo de 1996-2004. Se ha incluido a 5.419 pacientes estudiados con pruebas epicutáneas durante el periodo total del estudio. La prevalencia media de DAC a cosméticos ha aumentado de 9,8% en el periodo 1996-2004 a 13,9% en el periodo 2005-2013. La DAC a cosméticos se ha correlacionado con el sexo femenino, pero no con la atopia. El kathon CG (mezcla de metilcloroisotiazolinona y metilisotiazolinona), las fragancias y la parafenilendiamina (PPDA) se han mantenido como las causas más frecuentes, aunque en los últimos años los acrilatos y los filtros solares han sido alérgenos emergentes

The incidence of allergic contact dermatitis (ACD) to cosmetics in the general population is rising with the increasing use of cosmetic products and their proliferation and diversification. The aims of this study were to determine the prevalence of ACD to cosmetics in our setting, analyze changes over time, describe the clinical and epidemiological features of this allergic reaction, and identify the allergens and cosmetics involved. We performed a prospective study at the skin allergy unit in Hospital General Universitario de Valencia in Spain between 2005 and 2013 and compared our findings with data collected retrospectively for the period 1996 to 2004. The 5419 patients who underwent patch testing during these 2 periods were included in the study. The mean prevalence of ACD to cosmetics increased from 9.8% in the first period (1996-2004) to 13.9% in the second period (2005-2013). A significant correlation was found between ACD to cosmetics and female sex but not atopy. Kathon CG (blend of methylchloroisothiazolinone and methylisothiazolinone), fragrances, and paraphenylenediamine were the most common causes of ACD to cosmetics during both study periods, and acrylates and sunscreens were identified as emerging allergens during the second period

Eccema de labios. Experiencia en la Unidad de Eccema de Contacto de un centro terciario español / Lip eczema. Experience in the Contact Dermatitis Unit of a Spanish tertiary hospital

Fundamento: El eccema labial es un problema poco frecuente en las Unidades de Eccema de Contacto (UEC). Hasta el momento han sido publicadas escasas series que muestren el perfil de estos pacientes y las causas de su eccema, ninguna de ellas española. El objetivo de este estudio fue el de analizar el perfil epidemiológico de los pacientes que acuden a la UEC en nuestro entorno, los diagnósticos principales y los alérgenos relevantes. Material y métodos: Se realizó una revisión retrospectiva de los pacientes remitidos a la UEC en el periodo 2005-2014. Se realizaron pruebas epicutáneas con la serie estándar ampliada del Grupo Español de Investigación en Dermatitis Alérgica de contacto (GEIDAC), productos propios y otras baterías complementarias. Resultados: En los 78 pacientes estudiados, los diagnósticos más frecuentes fueron la dermatitis de contacto alérgica y la dermatitis atópica. Los alérgenos relevantes más frecuentes fueron los cosméticos y los fármacos tópicos. Conclusiones: Es fundamental estudiar a los pacientes con eccema labial con pruebas epicutáneas para poder filiar correctamente su etiología y según esto, realizar un tratamiento más adecuado (AU)

Background: Lip eczema is an infrequent problem in Contact Dermatitis Units (CDU). Very few series have been published to date that show the profiles of such patients and the causes of their eczemas, and none are Spanish. The goal of this study was to analyze the epidemiological profile of the patients who attend a CDU in our setting, the main diagnoses and the relevant allergens. Methods: A retrospective review was made of the patients referred to the CDU in the 2005-2014 period. Patch tests were carried out with the extended standard series of the Spanish Research Group on Allergic Contact Dermatitis (Grupo Español de Investigación en Dermatitis Alérgica de contacto - GEIDAC), our own products and other complementary sets. Results: The most frequent diagnoses in the 78 patients studied were allergic contact dermatitis and atopic dermatitis. The most frequent relevant allergens were cosmetics and topical medications. Conclusions: It is essential to study the patients with lip eczema with patch tests to be able to correctly determine their etiology and accordingly to carry out the most suitable treatment (AU)

Design Space Approach for Preservative System Optimization of an Anti-Aging Eye Fluid Emulsion.

The use of preservatives must be optimized in order to ensure the efficacy of an antimicrobial system as well as the product safety. Despite the wide variety of preservatives, the synergistic or antagonistic effects of their combinations are not well established and it is still an issue in the development of pharmaceutical and cosmetic products. The purpose of this paper was to establish a space design using a simplex-centroid approach to achieve the lowest effective concentration of 3 preservatives (methylparaben, propylparaben, and imidazolidinyl urea) and EDTA for an emulsion cosmetic product. Twenty-two formulae of emulsion differing only by imidazolidinyl urea (A: 0.00 to 0.30% w/w), methylparaben (B: 0.00 to 0.20% w/w), propylparaben (C: 0.00 to 0.10% w/w) and EDTA (D: 0.00 to 0.10% w/w) concentrations were prepared. They were tested alone and in binary, ternary and quaternary combinations. Aliquots of these formulae were inoculated with several microorganisms. An electrochemical method was used to determine microbial burden immediately after inoculation and after 2, 4, 8, 12, 24, 48, and 168 h. An optimization strategy was used to obtain the concentrations of preservatives and EDTA resulting in a most effective preservative system of all microorganisms simultaneously. The use of preservatives and EDTA in combination has the advantage of exhibiting a potential synergistic effect against a wider spectrum of microorganisms. Based on graphic and optimization strategies, we proposed a new formula containing a quaternary combination (A: 55%; B: 30%; C: 5% and D: 10% w/w), which complies with the specification of a conventional challenge test. A design space approach was successfully employed in the optimization of concentrations of preservatives and EDTA in an emulsion cosmetic product.

Physical and material properties of an emulsion-based lipstick produced via a continuous process.

OBJECTIVES: Water-in-oil emulsions in lipsticks could have the potential to improve moisturizing properties and deliver hydrophilic molecules to the lips. The aim of this work was to investigate the effect of a continuous process (scraped surface heat exchanger (SSHE) and pin stirrer (PS)) on the physical and material properties of an emulsion-based lipstick by altering the processing conditions of both the SSHE and PS. METHODS: Emulsion formation was achieved using a SSHE and PS. Emulsions were analysed using nuclear magnetic resonance restricted diffusion (droplet size), texture analysis and rheology (mechanical properties). RESULTS: Results showed that a higher impeller rotational velocity (IRV) (1500 r.p.m.) and a lower exit temperature (52°C) produce the smallest droplets (~ 4 µm), due to greater disruptive forces and a higher viscosity of the continuous phase. The addition of a PS reduces the droplet size (14-6 µm) if the SSHE has a low IRV (500 r.p.m.), due to greater droplet disruption as the emulsion passes through the PS unit. Results also show that if the jacket temperature of a SSHE is 65°C, so that crystallization occurs in both process and post-production, droplets can be integrated into the network resulting in a stiffer wax network (G' - 0.12, in comparison to 0.02 MPa). This is due to small crystals creating a shell around water droplets which can form connections with the continuous network forming a structured network. The addition of a pin stirrer can disrupt a formed network reducing the stiffness of the emulsion (0.3-0.05 MPa). CONCLUSION: This work suggests the potential use of a continuous process in producing an emulsion-based lipstick, particularly when wax crystals are produced in the process. Future work should consider the moisturizing or lubricating properties of wax continuous emulsions and the release of hydrophilic compounds from the aqueous phase.

Characterization, sensorial evaluation and moisturizing efficacy of nanolipidgel formulations.

BACKGROUND: Nanostructured lipid carriers (NLC) have been widely studied for cosmetic and dermatological applications due to their favourable properties that include the formation of an occlusive film on the skin surface that reduces the transepidermal water loss (TEWL) and increase in water content in the skin which improves the appearance on healthy human skin and reduces symptoms of some skin disorders like eczema. OBJECTIVE: The main objective of this study was the development of semisolid formulations based NLC with argan oil or jojoba oil as liquid lipids, by addition of Carbopol®934 or Carbopol®980 as gelling agents, followed by comparison between instrumental analysis and sensorial evaluation and in vivo efficacy evaluation. METHODS: Nanostructured lipid carriers dispersions were produced by the ultrasound technique, and to obtain a semisolid formulation, gelling agents were dispersed in the aqueous dispersion. Particle size, polydispersity index and zeta potential were determined. Instrumental characterization was performed by rheological and textural analysis; the sensorial evaluation was also performed. Finally, skin hydration and TEWL were studied by capacitance and evaporimetry evaluation, respectively. RESULTS: Particles showed a nanometric size in all the analysed formulations. All the gels present pseudoplastic behaviour. There is a correspondence between the properties firmness and adhesiveness as determined by textural analysis and the sensory evaluation. The formulations that showed a greater increase in skin hydration also presented appropriate technological and sensorial attributes for skin application. CONCLUSIONS: Nanolipidgel formulations with the addition of humectants are promising systems for cosmetic application with good sensory and instrumental attributes and moisturizing efficacy.

Influence of pH, concentration of sodium lactate as an additive and ultrasonic treatment on synthesis of zinc phosphate white pigments.

Zinc oxide that has the photocatalytic activity is used as a white pigment for cosmetics. A certain degree of sebum on the skin is decomposed by the ultraviolet radiation in sunlight. In this work, zinc phosphates were prepared from zinc nitrate and phosphoric acid at pH 5 and 7 with and without the addition of sodium lactate and ultrasonic treatment as a novel white pigment for use in cosmetics. The chemical composition, powder properties, photocatalytic activity, colour phase, moisture retention and smoothness of the zinc phosphates were studied. The obtained materials had a Zn/P ratio of about 1.5, which corresponds to zinc orthophosphate Zn3 (PO4 )2 . Samples prepared with ultrasonic treatment indicated the high ratios of large particles in scanning electron microscopy images and particle-size distributions. The photocatalytic activity of these zinc phosphate particles was too less to protect the sebum on the skin. The materials obtained and their thermal products at 100°C showed a high reflectance within the range of visible light. The slipping resistance and roughness of the powder were enough low for use in cosmetics.

Aqueous dispersions of organogel nanoparticles - potential systems for cosmetic and dermo-cosmetic applications.

OBJECTIVE: The preparation and physicochemical characterization of organogel nanoparticles dispersed in water have been developed. These systems could be employed as nanocarrier for cosmetic applications or as hydrophobic reservoirs for drug delivery. METHODS: Gelled particles of organic liquid and 12-hydroxystearic acid (organogelator) were obtained by hot emulsification (T>Tgel), with a surfactant (acetylated glycol stearate) and polymers (sodium hyaluronate and polyvinyl alcohol) as stabilizing agents, and cooling at room temperature (T

Industrial applications of the Diels-Alder reaction.

The Diels-Alder reaction is one of the most popular transformations for organic chemists to generate molecular complexity efficiently. Surprisingly, little is known about its industrial application for the synthesis of pharmacologically active ingredients, agrochemicals, and flavors and fragrances. This Review highlights selected examples, with a focus on large-scale applications (>1 kg) from a process research and development perspective.

Synthesis, antioxidant and antimicrobial activity of a new phloridzin derivative for dermo-cosmetic applications.

The phenolic compound phloridzin (phloretin 2′-O-glucoside, variously named phlorizin, phlorrhizin, phlorhizin or phlorizoside) is a prominent member of the chemical class of dihydrochalcones, which are phenylpropanoids. Phloridzin is specifically found in apple and apple juice and known for its biological properties. In particular we were attracted by potential dermo-cosmetic applications. Here we report the synthesis, stability studies and antimicrobial activity of compound F2, a new semi-synthetic derivative of phloridzin. The new derivative was also included in finished formulations to evaluate its stability with a view to a potential topical use. Stability studies were performed by HPLC; PCL assay and ORAC tests were used to determine the antioxidant activity. F2 presented an antioxidant activity very close to that of the parent phloridzin, but, unlike the latter, was more stable in formulations. To further explore potential health claims, antifungal activity of phloridzin and its derivative F2 were determined; the results, however, were rather low; the highest value was 31,6% of inhibition reached by F2 on Microsporum canis at the highest dose.