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The effect of nanoencapsulation on the in vitro photoprotection and antioxidant properties of blueberry (Vaccinium myrtillus) extract, before and after their dispersion into an oil-in-water emulsion and its final stability under stress conditions. Besides its skin healing activity, chitosan was chosen as wall material due to its natural origin, and possibility of obtention from shrimp residues. Chitosan/tripolyphosphate (TPP) nanoparticles loaded with blueberry extract were produced and characterized. Three different semi-solid oil-in-water emulsions, using Ecocert certified materials, were developed containing, respectively, (i) 5% (wt/wt) of extract-free nanoparticles, (ii) 5% (wt/wt) of extract-loaded nanoparticles, (iii) 2% (wt/wt) of free extract. Sun protection factor (SPF), antioxidant activity and stability under stress conditions were evaluated. The concentration of rutin was determined by High Performance Liquid Chromatography (HPLC). The loading of blueberry extract into nanoparticles kept their physicochemical properties, as well as SPF and antioxidant activity, over the course of the stability study. Extract-loaded nanoparticles were dispersed in a semi-solid oil-in-water emulsion and were shown to protect the extract from oxidation, suggesting that formulation containing 5% (wt/wt) of extract-free nanoparticles could presented lower difference between initial and final SPF and antioxidant activity values after 90 days of analysis. The developed formulation is proposed as a greener potential formulation to be used as photoprotector, especially if associated with physical sun filters. The role of blueberry flavonoids and the synergistic effect of nanoparticles against skin aging are here discussed., This research was funded by FAPESP (grant number 2015/25533–7, 2017/14757–7, 2017/05275–9) and in part by CAPES (Finance Code 001). This study was financed by CNPq (301436/2017–7) granted to PGM, and by the Portuguese Science and Technology Foundation (FCT / MCT) and from European Funds (PRODER/COMPETE) under the project reference UIDB/04469/2020 (strategic fund), co-financed by FEDER, under the Partnership Agreement PT2020, granted to EBS., info:eu-repo/semantics/publishedVersion

The cashew nut is an important product in Brazil, both for consumption and export, with the pulp of the cashew fruit being considered a by-product despite its high flavonoid content. In this study, the use of cashew pulp extract as a treatment for acne and in the prevention of early skin damage was investigated. Its flavonoid content was determined using spectrophotometric identification, and its effects on cell and bacterial viability, the migration of keratinocytes, and antioxidant activity in vitro were evaluated. Furthermore, it was incorporated into an emulsion for topical administration, and the physical-chemical stability parameters of the formulation were determined. The cashew pulp contained flavonoids with healing and antioxidant activity, and was not toxic to keratinocyte cells in a viability test. The flavonoid-rich formulation was stable, indicating that this is a promising formulation for use in the treatment of acne and protection of skin against premature damage.

O alecrim, uma planta usada popularmente, contem compostos bioativos com notada capacidade antioxidante, como o acido carnosico e o acido rosmarinico. Quatro metodos de extracao foram avaliados quanto a eficiencia na extracao dos compostos antioxidantes e sua acao no ensaio de cicatrizacao scratch. Dentre os metodos utilizados, a maceracao se mostrou a mais eficiente na extracao dos compostos antioxidantes. Os extratos apresentaram atividade antioxidante e nao apresentaram citotoxicidade significativa, porem o extrato obtido pelo metodo maceracao, testado no cicatrizacao in vitro, nao acelerou o processo de cicatrizacao nas condicoes testadas.

Bromelain, a set of proteolytic enzymes potential pharmaceutical applications, was encapsulated in chitosan nanoparticles to enhance enzyme stability, and the effect of different chitosan sources was evaluated. Chitosan types (i.e., low molecular weight chitosan, chitosan oligosaccharide lactate, and chitosan from shrimp shells) produced nanoparticles with different physicochemical properties, however in all cases, particle size and zeta potential decreased, and polydispersity index increased after bromelain addition. Bromelain encapsulation was higher than 84% and 79% for protein content and enzymatic activity, respectively, with low molecular weight chitosan presenting the highest encapsulation efficiency. Nanoparticle suspension was also tested for accelerated stability and rheological behavior. For the chitosan–bromelain nanoparticles, an instability index below 0.3 was recorded and, in general, the loading of bromelain in chitosan nanoparticles decreased the cohesiveness of the final suspension., This research was granted by FAPESP (2016/03444-5,2017/05275-9,and2017/05333-9), CNPq and FAEPEX, and by the Portuguese Science and Technology Foundation, Ministry of Science and Education (FCT/MEC) through national funds, and co-financed by FEDER, under the project reference M-ERA-NET/0004/2015 (PAIRED) Partnership Agreement PT2020., info:eu-repo/semantics/publishedVersion

The aim of this study was to develop a phytocosmetic sunscreen emulsion with antioxidant effect, containing a blend of flavonoid-enriched plant extracts. In vitro sun protection factor, antioxidant activity, skin irritation, photostability, cutaneous permeation, and retention of flavonoids were evaluated. Thermodynamically stable emulsions were obtained and tested for sensorial analysis after loading the blend of extracts. The selected emulsion was stable when stored at low temperatures (5 C), for which after 120 days the concentration of quercetin and rutin were above their limit of quantification, i.e., 2.8 &plusmn, 0.39 &micro, g/mL and 30.39 &plusmn, g/mL, respectively. Spreadability, low rupture strength and adhesiveness were shown to be similar to a conventional topical product. Higher brittleness, pseudo-plastic, and viscoelastic behaviors were also recorded for the developed phytocosmetic sunscreen. The product presented a critical wavelength of 387.0 nm and ultraviolet rays A and B (UVA/UVB) rate of 0.78, confirming that the developed formulation shows capacity for UVA/UVB protection, protecting skin against damages caused by Ultraviolet (UV) radiation. Rutin was shown to permeate the skin barrier and was also quantified in the stratum corneum (3.27 &plusmn, 1.92 &micro, g/mL) by tape stripping and retention test (114.68 &plusmn, 8.70 &micro, g/mL). The developed flavonoid-enriched phytocosmetic was shown to be non-irritant to skin by an in vitro assay. Our results confirm the antioxidant activity, sun protection, and physical properties of the developed phytocosmetic for topical application.

Os filtros solares são formulações capazes de proteger a pele contra raios ultravioletas, os quais causam diferentes danos à pele. Os filtros solares podem ser divididos em filtros químicos e físicos, em que os filtros químicos apresentam maior suscetibilidade de irritação da pele em relação aos filtros físicos. Os estudos com substâncias naturais visam diminuir a irritação causada por alguns filtros solares, ao passo que algumas substâncias estudadas apresentam um carácter de proteção contra os raios ultravioletas, como os flavonóides. Esse projeto teve como objetivo continuar os estudo de determinação de antocianinas e do fator de proteção solar presente no extrato hidroalcoólico obtido a partir do mirtilo (Vaccinium ashei). Essas características foram determinadas através de uma metodologia in vitro utilizando espectrofotometria na região do ultravioleta. Posteriormente, foi desenvolvida uma formulação cosmética, na qual foi incorporado o extrato previamente microencapsulado. A formulação com e sem a presença do extrato foi analisada quanto ao fator de proteção solar, teor de antocianinas e atividade antioxidante in vitro, além do estudo de sua estabilidade com a verificação dos valores de pH, densidade e viscosidade, após a exposição a condições de estresse. Essas análises tiveram como objetivo a utilização de uma substância natural para o desenvolvimento de um produto alternativo no combate à radiação solar e ao envelhecimento precoce da pele.

The aim of study was to determine the in vitro sun protection factor (SPF) and the photostability profile of a topical formulation composed of nanoparticles loaded with vegetable extracts and to assess its physicochemical properties. Chitosan/tripolyphosphate (TPP) nanoparticles loaded with flavonoids-enriched vegetable extracts (Ginkgo biloba L., Dimorphandra mollis Benth, Ruta graveolens, and Vitis vinifera L.) were produced and characterized for their morphology, mean particle size, zeta potential, and encapsulation efficiency. A final topical formulation was obtained by dispersing chitosan/TPP nanoparticles in an o/w emulsion. Results showed that nanoparticles dispersion exhibited yellowish color, spherical shape, and uniform appearance. Extract-loaded chitosan/TPP nanoparticles showed a mean particle size of 557.11±3.1 nm, polydispersity index of 0.39±0.27, zeta potential of +11.54±2.1 mV, and encapsulation efficiency of 75.89% of rutin. The recorded texture parameters confirm that the developed formulation is appropriate for skin application. The SPF obtained was 2.3±0.4, with a critical wavelength of 387.0 nm and 0.69 UVA/UVB ratio. The developed formulation exhibited photostability, allowing the release of flavonoids from nanoparticles while retaining rutin into the skin in a higher extension., The authors acknowledge FAPESP (grant number 2015/25533-7 and 2017/14757-7), CAPES, and CNPq agencies for the financial support of this study. The authors also acknowledge the financial support received from the Portuguese Science and Technology Foundation (FCT/MCT) and from the European Funds (PRODER/COMPETE) under the project reference M-ERA-NET/0004/2015-PAIRED, co-financed by FEDER, under the Partnership Agreement PT2020., info:eu-repo/semantics/publishedVersion

The aim of this study was to validate a HPLC method for the assay of flavonoids in extracts obtained from natural sources, i.e., from Dirmophandra mollis Benth, Ginkgo biloba L., Ruta graveolens L., and Vitis vin&iacute, fera L. The potential sun protecting effect, antioxidant activity, and cell viability of the extracts were also determined. Individual extracts (obtained from each individual species) and a mixed extract (containing the four extracts) were analyzed by the validated HPLC method for the identification of flavonoids and quantification of rutin and quercetin. An in vitro cell viability study was carried out using the neutral red method. The in vitro sun protection factor was determined by spectral transmittance and in vitro antioxidant efficacy was evaluated against DPPH, ABTS, and AAPH radicals. The HPLC method used for the identification and quantification of flavonoids in extracts exhibited linearity, precision, accuracy, and robustness. Detection and quantification limits were, respectively, 2.881 &plusmn, 0.9 &mu, g&middot, mL&minus, 1 and 0.864 &plusmn, 1 for quercetin, and 30.09 &plusmn, 1 &mu, 1 and 9.027 &plusmn, 1.1 &mu, 1 for rutin. All extracts did not affect cell viability at the evaluated concentration range and exhibited a sun protection effect and antioxidant activity. Among the evaluated extracts, Ginkgo biloba L. and the mixed extract depicted the most expressive antioxidant activity. The mixed extract exhibited sunscreen protection against ultraviolet A (UVA) and ultraviolet B (UVB) and a critical wavelength of 372.7 &plusmn, 0.1. Our results translate the enhanced flavonoids&rsquo, composition of the mixed extract, which may be a potential alternative over sunscreens and antioxidants in pharmaceutic/cosmetic formulations.

A flavonoid enriched extract (FE) was obtained from grape peels, and in vitro SPF, antioxidant activity, and effects on cell viability of this extract were tested with the intent to develop a cosmetic product. A formulation was developed with the FE, and the stability of this mixture was evaluated in terms of pH, density, viscosity, and SPF (90-days). FE showed no cytotoxicity to human keratinocytes and an in vitro SPF of 18.56 (UV-spectrophotometry). Further, FE showed a UVA protection factor of 3.17 ± 0.2, a critical wavelength of 318.0 ± 0.1 and a UVA/UVB of 0.9. Antioxidant activity assays resulted in 92.08% and 86.85% of activity against DPPH and ABTS (IC50 = 296.90 ± 1.2 µg/mL and 643.13 ± 0.9 µg/mL), respectively. Finally, SPF of formulation with FE was 12.45. Results from the in vitro SPF and product stability tests (especially storage under refrigeration), indicate that FE is a promising compound for use as an innovative sunscreen formulation.

Background: The fruits acerola and red plum are known to be good sources of antioxidants, particularly vitamin C. Antioxidants are compounds that protect organisms from biomolecular damage, such as accelerated aging, caused by free radicals. Objective: The objective of this study was to extract vitamin C from acerola and red plum, incorporate these extracts into different topical formulations, and evaluate the physicochemical stabilities of these formulations under stress conditions. Methods: Vitamin C was extracted from acerola and red plum via dynamic maceration for 2 h at 50 ± 2°C and was quantified via HPLC. In vitro antioxidant activities were evaluated using DPPH assays. The extracts were then incorporated into emulsion and gel formulations in two types of packaging, and stability studies were carried out. Results: Red plum and acerola extracts were orange and red and contained vitamin C concentrations of 2732.70 ± 93.01 mg/100 g and 2.60 ± 1.2 mg/100 g, respectively. In vitro antioxidant activity resulted in over 90.0% inhibition of free radicals at 0.01 mL/mL acerola extract and 0.1 mL/mL red plum extract. In the stability study, pH values decreased for both acerola formulations when stored in the oven or in transparent glass containers. Formulations containing red plum extract were stable under all conditions. Acerola extracts contained a higher concentration of vitamin C than red plum extracts. Both extracts possessed antioxidant activity, although the acerola-based formulation was unstable when stored at high temperatures or in transparent glass containers. Highlights: Extracts from red plum and acerola contained vitamin C; antioxidant activity of the extracts resulted in over 90.0% inhibition of free radicals. Formulations containing red plum were stable under all tested conditions, and formulations containing acerola were unstable when stored in the oven or in transparent glass containers.

Made available in DSpace on 2022-04-28T19:01:45Z (GMT). No. of bitstreams: 0 Previous issue date: 2015-01-01 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. University of São Paulo State Faculty of Pharmaceutical Sciences, Araraquara-Jau Highway, Km 1

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. 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.

Appropriate therapeutics for wound treatments can be achieved by studying the pathophysiology of tissue repair. Here we develop formulations of lamellar gel phase (LGP) emulsions containing marigold (Calendula officinalis) oil, evaluating their stability and activity on experimental wound healing in rats. LGP emulsions were developed and evaluated based on a phase ternary diagram to select the best LGP emulsion, having a good amount of anisotropic structure and stability. The selected LGP formulation was analyzed according to the intrinsic and accelerated physical stability at different temperatures. In addition, in vitro and in vivo studies were carried out on wound healing rats as a model. The LGP emulsion (15.0% marigold oil; 10.0% of blend surfactants and 75.0% of purified water [w/w/w]) demonstrated good stability and high viscosity, suggesting longer contact of the formulation with the wound. No cytotoxic activity (50-1000 μg/mL) was observed in marigold oil. In the wound healing rat model, the LGP (15 mg/mL) showed an increase in the leukocyte recruitment to the wound at least on days 2 and 7, but reduced leukocyte recruitment after 14 and 21 days, as compared to the control. Additionally, collagen production was reduced in the LGP emulsion on days 2 and 7 and further accelerated the process of re-epithelialization of the wound itself. The methodology utilized in the present study has produced a potentially useful formulation for a stable LGP emulsion-containing marigold, which was able to improve the wound healing process.