Chemical composition, antioxidant activity and development of a facial serum formulation from the extract of Hancornia speciosa.

The goal of this work was to chemically characterise Hancornia speciosa extracts to develop an antioxidant serum formulation. Stem and bark extracts were prepared using 70% hydroethanol solution by Sohxlet and ultrasound assisted extraction. The content of total phenols, flavonoids, and antioxidant activity were evaluated, and chemical characterization was performed by HPLC -detector UV-VIS (SPD - 10 A). The formulation was developed with stem extract (0.250 mg/g) in hydroxyethylcellulose fluid gel. Stem extracts had higher total phenols and flavonoids, and higher antioxidant activity than bark extracts. The formulation presented low viscosity, a yellowish colour, 81.28% ± 0.14 of antioxidant activity. In the stability test, the physicochemical characteristics showed small variations, remaining more stable at a temperature of 5 °C, with an antioxidant activity of 64.81% ± 0.75. Therefore, the stem of H. speciosa has the potential to be used in antioxidant formulations.

Production of mycosporine-like amino acid (MAA)-loaded emulsions as chemical barriers to control sunscald in fruits and vegetables.

BACKGROUND: Sunscald is a physiological disorder that occurs in many horticultural products when exposed to excessive solar radiation and high temperatures. Traditionally, sunscald is controlled using physical barriers that reflect radiation, however this practice is not always efficient. A possible alternative would be the use of chemical barriers, such as mycosporine-like amino acids (MAAs), which protect aquatic organisms against ultraviolet (UV) radiation. Thus, this study aimed to develop a lipid-based emulsion containing MAAs for using in the preharvest of horticultural products. RESULTS: Emulsions were developed using 10% (w/v) of corn oil (CO) and soybean oil (SO), carnauba wax (CW), and beeswax (BW) as lipid bases (LBs). The emulsion containing CW and ammonium hydroxide was the most stable, resembling commercial wax. Therefore, this formulation was used as the basis for the incorporation of the commercial product Helioguard™ 365, a source of MAA, in concentrations of 0%, 1%, 2%, and 4% (v/v). The MAA incorporation resulted in little modifications in the stability of the emulsion, providing an increase in the absorbance with peaks in the UV-B ranging from 280 to 300 nm. CONCLUSION: The lipid-base emulsion containing MAAs could be used as a chemical barrier to control sunscald in horticultural products. © 2021 Society of Chemical Industry.

In vitro evaluation of the cytotoxicity and eye irritation potential of preservatives widely used in cosmetics

Abstract The consumption of cosmetics has been increasing every year and is expected to reach $675 billion by 2020 at an estimated growth rate of 6.4% per year. Exposure to skin irritants is the major cause of non-immunological inflammation of the skin. Therefore, the safety evaluation of cosmetic preservatives should be increased. Thus, the present work aimed to evaluate the cytotoxicity as the viability endpoint and the eye irritation potential of preservatives used in cosmetics. Cytotoxicity assays were performed using MTT and NRU in human keratinocytes (HaCaT), human dermal fibroblasts, adult (HDFa), and human hepatoma cells (HepG2). The eye irritation potential was evaluated using the Hen's Egg Test-chorioallantoic membrane (HET-CAM). The evaluated preservatives were methylparaben (MP), propylparaben (PP), phenoxyethanol (PE), and a mixture of methylchloroisothiazolinone and methylisothiazolinone (CMI/MI). All preservatives showed cytotoxic potential within the permitted concentrations for use in cosmetic products. In the HET-CAM test, PE and CMI/MI, MP, and PP were classified as severe, moderate, and poor irritants, respectively. Our results indicate that proper safety evaluations are required to ensure the beneficial properties of preservatives on cosmetic products without exceeding exposure levels that would result in adverse health effects for consumers.

New and potential properties, characteristics, and analytical methods of ferulic acid: A review

Abstract Phenolic compounds are widely distributed in the plant kingdom and in the microorganisms. Cinnamic acid and its hydroxylated derivative-ferulic acid, are phenolic compounds. Ferulic acid possesses antioxidant potential, as well as anti-cancer, anti-inflammatory, and antimicrobial properties. It prevents the harmful effects of radiation both as an ultraviolet absorber and as a free radical scavenger; it is not cytotoxic. Although ferulic acid has beneficial properties, it is hardly used in cosmetic preparations and has been rarely studied in the literature. Herein, we review the literature on ferulic acid, to provide information which can contribute to further research on the compound.

Integrated approaches to testing and assessment as a tool for the hazard assessment and risk characterization of cosmetic preservatives.

The safety assessment of cosmetic products is based on the safety of the ingredients, which requires information on chemical structures, toxicological profiles, and exposure data. Approximately 6% of the population is sensitized to cosmetic ingredients, especially preservatives and fragrances. In this context, the aim of this study was to perform a hazard assessment and risk characterization of benzalkonium chloride (BAC), benzyl alcohol (BA), caprylyl glycol (CG), ethylhexylglycerin (EG), chlorphenesin (CP), dehydroacetic acid (DHA), sodium dehydroacetate (SDH), iodopropynyl butylcarbamate (IPBC), methylchloroisothiazolinone and methylisothiazolinone (MCI/MIT), methylisothiazolinone (MIT), phenoxyethanol (PE), potassium sorbate (PS), and sodium benzoate (SB). Considering the integrated approaches to testing and assessment (IATA) and weight of evidence (WoE) as a decision tree, based on published safety reports. The hazard assessment was composed of a toxicological matrix correlating the toxicity level, defined as low (L), moderate (M), or high (H) and local or systemic exposure, considering the endpoints of skin sensitization, skin irritation, eye irritation, phototoxicity, acute oral toxicity, carcinogenicity, mutagenicity/genotoxicity, and endocrine activity. In a risk assessment approach, most preservatives had a margin of safety (MoS) above 100, except for DHA, SDH, and EG, considering the worst-case scenario (100% dermal absorption). However, isolated data do not set up a safety assessment. It is necessary to carry out a rational risk characterization considering hazard and exposure assessment to estimate the level of risk of an adverse health outcome, based on the concentration in a product, frequency of use, type of product, route of exposure, body surface location, and target population.

LQFM184: A Novel Wide Ultraviolet Radiation Range Absorber Compound.

The use of sunscreen has become an indispensable daily routine since UV radiation is a critical environmental stress factors for human skin. This study focused on the design, synthesis, thermal/chemical stability and efficacy/safety evaluations of a new heterocyclic derivative, namely LQFM184, as a photoprotective agent. The compound showed stability when submitted under oxidative and high-temperature conditions. It also revealed an absorption at 260-340 nm (UVA/UVB), with a main band at 298 nm and a shoulder close to 334 nm. LQFM184 showed capacity to interact with other existing UV filters, promoting an increase in the sun protection factor. In relation to acute toxicity, its estimated LD50 was >300-2000 mg kg-1 , probably with a low potential of inducing acute oral systemic toxicity hazard. In addition, our data showed that this compound did not have eye irritation, skin sensitization or phototoxicity potentials. Taken together, these findings make LQFM184 a promising ingredient to be used, alone or in association with other UV filters, in cosmetic products such as sunscreens with a broad spectrum of protection.

In vitro methods to determine the antioxidant activity of caffeic acid.

Caffeic acid (CA) is a plant metabolite acting as a carcinogenic inhibitor, and exhibits a high antioxidant effect and some antimicrobial activity. Besides, this compound can be useful in the prevention of heart diseases and atherosclerosis, among others. The present study aims to determine the in vitro antioxidant activity of CA in order to increase the frequency of its use and reliability in the prevention of damage caused by free radicals and other reactive species. The tests performed were as follows: Radical anion superoxide capture; crocin bleaching assay; capturing ability of hypochlorous acid; H2O2 capture; capturing capacity of the ABTS•+/DPPH•; and SOD-like activity. The values of the CA antioxidant activity were very close to the values of standards in all tests. Besides, CA presented an antioxidant activity greater than that of ascorbic acid and trolox, and its advantages include higher stability than ascorbic acid and extraction from natural sources, as opposed to trolox.

Release and permeation profiles of spray-dried chitosan microparticles containing caffeic acid.

Caffeic acid (CA), a phenolic compound found in plants with antioxidant and antimicrobial activity, induces collagen production and prevents premature aging of the skin. The objective of this study was to develop two types of chitosan microparticles (MP) containing CA and to relate the morphology with the release and permeation profiles. One type of MP was prepared from a hydroalcoholic solution (MPI) and the other from an aqueous solution (MPII). Their morphology and size was evaluated by high-resolution scanning electron microscopy. The release profile of CA was evaluated using the cellulose membrane from the two MPs in Franz diffusion cells and the permeation profile was evaluated using human abdominal skin samples; the epidermal membranes were prepared by the heat-separation technique. MPII was spherical with a smooth surface, suitable for the controlled release of substances, whereas MPI was porous with non-internalized residual material. This result was consistent with their release and permeation profiles because MPII exhibited a slower and more controlled release than MPI. Thus, the method of preparation of MP and their composition influence the release profile of CA. Therefore, the production conditions must be closely controlled.

Bacterial cellulose skin masks-Properties and sensory tests.

BACKGROUND: Bacterial cellulose (BC) is a versatile material produced by microorganisms in the form of a membranous hydrogel, totally biocompatible, and endowed with high mechanical strength. Its high water-holding capacity based on its highly porous nanofibrillar structure allows BC to incorporate and to release substances very fast, thus being suitable for the preparation of skincare masks. AIMS: The preparation and characterization of cosmetic masks based on BC membranes and active cosmetics. METHODS: The masks were prepared by the simple incorporation of the cosmetic actives into BC membranes, used as a swelling matrix. The masks were characterized by Fourier transform infrared (FTIR), scanning electron microscopy (SEM), sensory tests, and skin moisture tests on volunteers. RESULTS: The results of sensory tests revealed the good performance of BC, being considered effective by the panel of volunteers, specially for adhesion to the skin (7.7 at the score scale), and improvement of the skin moisture (the hydration effect increased 76% in 75% of the volunteers that used vegetable extract mask formulation [VEM]), or a decrease in skin hydration (80% of the volunteers showed 32.6% decrease on skin hydration using propolis extract formulation [PEM] treatment), indicating the BC nanofiber membranes can be used to skincare applications. CONCLUSION: The results demonstrate the BC can be used as an alternative support for cosmetic actives for skin treatment.

Caffeic Acid in Dermatological Formulations: In Vitro Release Profile and Skin Absorption.

AIM AND OBJECTIVE: Caffeic acid (CA) is a cinnamic acid derivative, found in many vegetable products, with powerful antioxidant activity, the ability to increase collagen production and capacity to prevent premature aging of the skin. The classic emulsions of CA are widely used by the consumer to provide a pleasant, refreshing sensorial experience; however, preparations developed in the form of dry film are presented as a technological alternative due to its facile and safe transportation. The aim of this study was to evaluate the release, permeation, and retention of CA in a film and emulsion through in vitro experiments. MATERIAL AND METHODS: The release evaluation of CA from the emulsion and the film was performed using modified Franz diffusion cells, with an area of 1.77 cm², using Microette equipment (Hanson Research) with a cellulose membrane. The evaluation of the permeation of CA from the formulations was conducted using a similar technique of release, except that a biological membrane was used. RESULTS: High release of active compound and reduced permeation was observed, indicating that CA was able to be retained in the epidermis/dermis, where it should have the desired action. The concentration of caffeic acid in the skin was higher for the film formulation than for the emulsion. This demonstrates a greater efficiency of this type of innovative release system, besides its facile and safe transportation. CONCLUSION: The formulations tested in this paper can release caffeic acid with a Higuchi kinetic profile, in which release of active ingredient occurs by a diffusion process. The film formulations exhibited a lower permeation rate and higher retention in the skin, which is essential for a cosmetic product. The concentration of CA in the skin was also higher for the film formulation when compared to the emulsion. This demonstrates a greater efficiency of this type of innovative release system, in addition to its easy and safe transportation. Therefore, it is possible to suggest CA as a promising substance for dermal use due to its antioxidant, anti-inflammatory, antimicrobial, and collagen production stimulating activity.

Trypanocidal Activity of Flavokawin B, a Component of Polygonum ferrugineum Wedd.

The trypanocidal potential of the natural chalcone flavokawin B, which was isolated from the hexanic extract of Polygonum ferrugineum Wedd., is reported here. Although flavokawin B is widespread, this is the first report about its trypanocidal properties on both Trypanosoma cruzi (IC50 = 9.5 µM, IC50 = 34.7 µM benznidazol, Y strain) epimastigotes and Trypanosoma brucei (IC50 = 4.8 µM, IC50 = 6.4 µM pentamidine, 29-13 strain) procyclic forms, which was also corroborated on T. brucei strain 427 (IC50 = 6.2 µM). In order to learn more about its properties, unspecific cytotoxicity on Hep G2 cells was investigated as well as the trans-splicing inhibitory potential on T. brucei cells. The results shown here point to flavokawin B as a candidate in the search for new agents. It is also cheaper and less toxic than the available drugs to treat trypanosomiasis with a special focus on sleeping sickness disease.

Guava: phytochemical composition of a potential source of antioxidants for cosmetic and/or dermatological applications

ABSTRACT Guava (Psidium guajava L.) is a native fruit of the American tropics with commercial applications for its taste, flavor and aroma. Numerous pharmacological uses have been described for it, such as the antiseptic effect of its leaves, the use of the fresh fruit and tea from its leaves for the treatment of diarrhea, dysentery, diabetes mellitus, and others. However, considering its rich composition, the guava also is a potential source of antioxidants to be used in the development of new formulations for cosmetic and/or dermatological applications, the main focus of this research. Herein, we describe the study of the phytochemical composition and the antioxidant activity of a guava extract prepared with non-toxic solvents aiming its use at biological applications. High performance liquid chromatography and mass spectrometry were employed to identify the major components, while thermoanalytical measurements and hot stage microscopy were used to assess the chemical stability of guava fruit extract. The antioxidant activity was also evaluated assessing the SOD-like activity and ABTS free radical scavenger. The results show that the extract is a rich source of phenolic compounds, such as quercetin, kaempferol, schottenol, among many others. All of the components found in guava extract exhibit biological effects according to the literature data, mainly antioxidant properties.

Photoprotective effect and acute oral systemic toxicity evaluation of the novel heterocyclic compound LQFM048.

The new heterocyclic derivative LQFM048 (3) (2,4,6-tris ((E)-ethyl 2-cyano-3-(4-hydroxy-3-methoxyphenyl)acrylate)-1,3,5-triazine) was originally designed through the molecular hybridization strategy from Uvinul® T 150 (1) and (E)-ethyl 2-cyano-3-(4hydroxy-3-methoxyphenyl)acrylate (2) sunscreens, using green chemistry approach. This compound was obtained in global yields (80%) and showed an interesting redox potential. In addition, it is thermally stable up to temperatures around 250°C. It was observed that LQFM048 (3) showed a low degradation after 150min of sunlight exposure at 39°C, whereas the extreme radiation conditions induced a considerable photodegradation of the LQFM048 (3), especially when irradiated by VIS and VIS+UVA. During the determination of sun protection factor, LQFM048 (3) showed interesting results, specially as in association with other photoprotective compounds and commercial sunscreen. Additionally, the compound (3) did not promote cytotoxicity for 3T3 fibroblasts. Moreover, it was not able to trigger acute oral systemic toxicity in mice, being classified as a compound with low acute toxicity hazard (2.000mg/kg>LD50<5.000mg/kg). Therefore, this compound synthesized using green chemistry approach is promising showing potential to development of a new sunscreen product with advantage of presenting redox potential, indicating antioxidant properties.

Validation of HPLC-UV Assay of Caffeic Acid in Emulsions.

An accurate, sensitive, precise and rapid reversed-phase high-performance liquid chromatographic method was successfully developed and validated for the determination of caffeic acid (CA) in emulsions. The best separation was achieved on a 250 × 4.6 mm, 5.0 µm particle size RP18 XDB Waters column using ethanol and purified water (40:60 v/v) adjusted to pH 2.5 with acetic acid as the mobile phase at a flow rate of 0.7 mL/min. Ultraviolet detection was performed at 325 nm at ambient column temperature (25°C). The method was linear over the concentration range of 10-60 µg/mL (r(2) = 0.9999) with limits of detection and quantification of 1.44 and 4.38 µg/mL, respectively. CA was subjected to oxidation, acid, base and neutral degradation, as well as photolysis and heat as stress conditions. There were no interfering peaks at or near the retention time of CA. The method was applied to the determination of CA in standard and pharmaceutical products with excellent recoveries. The method is applicable in the quality control of CA.

Antioxidant Activity and Validation of Quantification Method for Lycopene Extracted from Tomato.

Lycopene is a carotenoid found in tomatoes with potent antioxidant activity. The aim of the study was to obtain an extract containing lycopene from four types of tomatoes, validate a quantification method for the extracts by HPLC, and assess its antioxidant activity. Results revealed that the tomatoes analyzed contained lycopene and antioxidant activity. Salad tomato presented the highest concentration of this carotenoid and antioxidant activity. The quantification method exhibited linearity with a correlation coefficient of 0.9992. Tests for the assessment of precision, accuracy, and robustness achieved coefficients with variation of less than 5%. The LOD and LOQ were 0.0012 and 0.0039 µg/mL, respectively. Salad tomato can be used as a source of lycopene for the development of topical formulations, and based on performed tests, the chosen method for the identification and quantification of lycopene was considered to be linear, precise, exact, selective, and robust.

Rheology as a Tool to Predict the Release of Alpha-Lipoic Acid from Emulsions Used for the Prevention of Skin Aging.

The availability of an active substance through the skin depends basically on two consecutive steps: the release of this substance from the vehicle and its subsequent permeation through the skin. Hence, studies on the specific properties of vehicles, such as their rheological behavior, are of great interest in the field of dermatological products. Recent studies have shown the influence of the rheological features of a vehicle on the release of drugs and active compounds from the formulation. In this context, the aim of this study was to evaluate the influence of the rheological features of two different emulsion formulations on the release of alpha-lipoic acid. Alpha-lipoic acid (ALA) was chosen for this study because of its antioxidant characteristics, which could be useful for the prevention of skin diseases and aging. The rheological and mechanical behavior and the in vitro release profile were assayed. The results showed that rheological features, such as viscosity, thixotropy, and compliance, strongly influenced the release of ALA from the emulsion and that the presence of a hydrophilic polymer in one of the emulsions was an important factor affecting the rheology and, therefore, the release of ALA.

Development and evaluation of an emulsion containing lycopene for combating acceleration of skin aging

Lycopene, a carotenoid and potent antioxidant is found in large quantities in tomatoes. Lycopene combats diseases, such as cardiovascular disease and different types of cancer, including prostate cancer. However, its topical use in emulsion form for the combat of skin aging is under-explored. The aim of the present study was to develop an emulsion containing lycopene extracted from salad tomatoes and evaluate its cytotoxicity, stability, rheological behavior, antioxidant activity and phytocosmetic permeation. The developed cosmetic comprised an oil phase made up of shea derivatives and was evaluated in terms of its physiochemical stability, spreadability, thermal analysis, rheological behavior, microbiological quality, cytotoxicity, antioxidant activity, cutaneous permeation and retention. The results demonstrate that this phytocosmetic is stable, exhibits satisfactory rheological behavior for a topical formula and is a promising product for combating skin aging.

Licopeno é um carotenóide com potente atividade antioxidante encontrado em grande quantidade no tomate e usado no combate a diversas doenças como doenças cardiovasculares e diferentes tipos de cânceres, incluindo o câncer de próstata. O objetivo desse trabalho foi desenvolver uma emulsão contendo extrato de licopeno obtido do tomate salada e avaliar a citotoxicidade do extrato, a estabilidade, o comportamento reológico, atividade antioxidante e permeação do fitocosmético. O cosmético foi desenvolvido utilizando fase oleosa contendo derivados de Karité e submetido à avaliação da estabilidade físico-química, espalhabilidade, análise térmica, comportamento reológico, qualidade microbiológica, citotoxicidade, atividade antioxidante e testes de permeação e retenção cutânea. Os resultados demonstraram que o fitocosmético é estável, apresenta comportamento reológico desejável para uma formulação tópica e é um produto promissor para ser utilizado no combate à aceleração do envelhecimento cutâneo.

Ethyl ferulate, a component with anti-inflammatory properties for emulsion-based creams.

Ethyl ferulate (FAEE) has been widely studied due to its beneficial heath properties and, when incorporated in creams, shows a high sun protection capacity. Here we aimed to compare FAEE and its precursor, ferulic acid (FA), as free radical scavengers, inhibitors of oxidants produced by leukocytes and the alterations in rheological properties when incorporated in emulsion based creams. The cell-free antiradical capacity of FAEE was decreased compared to FA. However, FAEE was more effective regarding the scavenging of reactive oxygen species produced by activated leukocytes. Stress and frequency sweep tests showed that the formulations are more elastic than viscous. The viscoelastic features of the formulations were confirmed in the creep and recovery assay and showed that the FAEE formulation was less susceptive to deformation. Liberation experiments showed that the rate of FAEE release from the emulsion was slower compared to FA. In conclusion, FAEE is more effective than FA as a potential inhibitor of oxidative damage produced by oxidants generated by leukocytes. The rheological alterations caused by the addition of FAEE are indicative of lower spreadability, which could be useful for formulations used in restricted areas of the skin.

Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi.

Trypanosoma brucei and Trypanosoma cruzi are the etiologic agents of sleeping sickness and Chagas disease, respectively, two of the 17 preventable tropical infectious diseases (NTD) which have been neglected by governments and organizations working in the health sector, as well as pharmaceutical industries. High toxicity and resistance are problems of the conventional drugs employed against trypanosomiasis, hence the need for the development of new drugs with trypanocidal activity. In this work we have evaluated the trypanocidal activity of a series of N1,N2-dibenzylethane-1,2-diamine hydrochlorides (benzyl diamines) and N1-benzyl,N2-methyferrocenylethane-1,2-diamine hydrochlorides (ferrocenyl diamines) against T. brucei and T. cruzi parasite strains. We show that incorporation of the ferrocenyl group into the benzyl diamines increases the trypanocidal activity. The molecules exhibit potential trypanocidal activity in vitro against all parasite strains. Cytotoxicity assay was also carried out to evaluate the toxicity in HepG2 cells.

Estudo da segurança de cosméticos: presente e futuro / Study of the safety of cosmetics: present and future

Cosméticos são usados pelo homem desde a antiguidade e, atualmente, o consumo tem aumentado muito, inclusive no Brasil, o terceiro maior mercado no mundo. Assim sendo, a preocupação com a segurança e eficácia destes produtos deve ser intensificada, mesmo sendo produtos raramente relacionados a reações adversas que causem danos à saúde. Para a avaliação das possíveis reações que podem ser apresentadas pelos produtos (irritação, sensibilização, efeitos sistêmicos), a Legislação Brasileira exige que os fabricantes avaliem a segurança e eficácia de seus produtos. Para este fim, em geral, são utilizados animais como modelo experimental o que está sendo cada vez mais evitado, acarretando a pesquisa por métodos alternativos para estas avaliações, que não necessitem de modelos experimentais in vivo. Desta forma, a presente revisão tem por objetivo apresentar os principais ensaios biológicos utilizados para avaliação da segurança de cosméticos, bem como ensaios in vitro que os substituam.

Cosmetics have been used since ancient times and, recently, their consumption has increased greatly in many countries, including brazil, which is the third largest consumer market in the world. Thus, concern for the safety and efficacy of these products should be heightened, even though these products are rarely related to adverse reactions that damage the health. Brazilian law requires manufacturers to subject their products to safety testing, to assess the possible reactions that could be caused by them (irritation, sensitization, systemic effects). To this end, in general, animals have been used as the experimental model, but this practice is being increasingly controlled, so that the scientific community is looking for alternative tests that do not require experimental in vivo models. Thus, this review aims to describe the main biological assays used to assess the safety of cosmetics, as well as in vitro assays that can replace them.