Employing photoacoustic spectroscopy in the evaluation of the skin permeation profile of emulsion containing antioxidant phenolic-rich extract of Melochia arenosa.

CONTEXT: Oxidative stress is an important factor modulating skin alterations. Melochia arenosa Benth. (Malvaceae) is a Brazilian plant with antimicrobial activity and antioxidant potential. OBJECTIVE: The objective of this study is to develop a topical formulation containing antioxidant phenolic-rich extract of M. arenosa and to evaluate its skin permeation profile. MATERIALS AND METHODS: Response surface methodology was used to maximize the total phenolic (TP) content of the extract and its antioxidant activity was evaluated by 2,2-diphenyl-1-picryl-hydrazyl (DPPH), 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and respiratory burst methods. An emulsion containing 1% optimized extract (OE) was developed and employed photoacoustic spectroscopy (PAS) for the determination of its skin permeation profile. The morphology of the skin was studied in histological sections stained with hematoxylin-eosin. RESULTS AND DISCUSSION: The optimum conditions predicted for the major extractive efficiency of the phenolics with 100% ethanol led extraction time 101 h and plant:solvent proportion 1:13.5 (w/v). OE presented TP = 724.6 ± 8.2 mg GAE/g extract and scavenging capacity of DPPH (IC50 value = 11.43 ± 0.14 µg/mL) and ABTS radicals (IC50 value = 35.42 ± 0.48 µg/mL). The production of ROS by neutrophils after stimulation with phorbol miristate acetate was lower when the OE was present in the reaction medium, endorsing its high antioxidant capacity. The data obtained by PAS indicated that the OE present in the emulsion has permeated and was distributed in the whole skin. No histopathological alterations were observed in the histological analysis. CONCLUSION: The formulation developed is a promising tool for skin care and could prevent the damage caused by oxidative stress.

Inhibitory Effect of Helicteres gardneriana Ethanol Extract on Acute Inflammation.

The anti-inflammatory effect of an ethanol extract of Helicteres gardneriana (Nees) Castiglioni was assayed in experimental models of pleurisy and microcirculation in situ. Treatment of animals with 500 mg/kg body weight reduced the exudate volume (35% reduction) induced by intrapleural injection of carrageenan and the migration of polymorphonuclear cells into the inflamed pleural cavity of rats (40%). Additionally, rolling and adhesion of leukocytes and the number of leukocytes that migrated toward the perivascular space in response to the carrageenan injection were decreased by the extract (500 mg/kg). These data demonstrate the anti-inflammatory effect of the ethanol extract of Helicteres gardneriana and imply that inhibition of leukocyte-endothelial interactions is important in the extract's mechanism of action.

Photodamage attenuating potential of Nectandra hihua against UVB-induced oxidative stress in L929 fibroblasts.

The total phenolic content (TP) and antioxidant activity of the ethanolic extract and fractions that were obtained from the leaves of Nectandra hihua were assessed using different methods. The ethanolic extract (EE) and ethyl acetate fraction (EAF) had the best antioxidant capacity, which was comparable to butylated hydroxytoluene and quercetin (ABTS+ 2.55 ±â€¯0.06, 3.54 ±â€¯0.03 mmol TE/g; DPPH IC50 10.27 ±â€¯0.05, 9.88 ±â€¯0.02 µg/mL; FRAP 2.17 ±â€¯0.08, 2.38 ±â€¯0.04 mmol TE/g; ORAC 5.16 ±â€¯0.08, 5.35 ±â€¯0.07 mmol TE/g; TP 568.05 ±â€¯18.15, 397.20 ±â€¯17.88 mg GAE/g, respectively). The cytoprotective effect, reactive oxygen species (ROS) and lipid peroxidation inhibitions on L929 fibroblasts irradiated with UVB (600 mJ/cm2) in pre- and post-treatments with EE and EAF were determined. These plant materials demonstrated high ROS scavenging activity and lipid peroxidation inhibition on L929 fibroblasts in both treatments, especially with pre-treatment (EE 38.47 ±â€¯1.95% and EAF 40.20 ±â€¯4.5% inhibition of ROS production, and EE 39.03 ±â€¯3.33% and EAF 41.67 ±â€¯7.6% of lipid peroxidation inhibition), indicating the best cytoprotection with pre-treatment (13.52 ±â€¯1.66% and 13.34 ±â€¯2.61% increases in cell viability). The antioxidant flavonoids quercitrin, avicularin, juglalin, afzelin and astragalin were isolated from EAF. The results obtained indicate that EE and EAF present photodamage attenuating potential against UVB-induced oxidative stress and can be useful as a starting point for developing dermatological products to prevent oxidative skin damage.

Antileishmanial and antioxidant potential of fractions and isolated compounds from Nectandra cuspidata.

The effects on the viability of promastigote and amastigote forms of Leishmania (Leishmania) amazonensis and citotoxicity in J774.A1 macrophages of ethanolic extract, fractions and isolated compounds that were obtained from the leaves of Nectandra cuspidata were determined. The total phenolics content (TP) and antioxidant activity were assessed using different assays. The ethyl acetate fraction (EAF) had the best antiproliferative activity (amastigote IC50: 4.42 ± 0.60 µg/mL, promastigote IC50: 33.33 ± 0.78) and presented no cytotoxicity at the highest concentration tested (1000 µg/mL). The EAF also had the greatest antioxidant capacity, which was comparable to butylated hydroxytoluene and quercetin (DPPH IC50 6.54 ± 0.10 µg/mL, ABTS 4.75 ± 0.11 mmol ET/g; FRAP 2.37 ± 0.03 mmol ET/g; ORAC = 33.52 ± 1.99 mmol ET/g; TP 387.11 ± 0.25 mg GAE/g). Vitexin, epicatechin and isovitexin isolated from EAF contribute to both activities.

Development and evaluation of topical formulations that contain hydroethanolic extract from Schinus terebinthifolia against HSV-1 infection

Abstract The therapeutic drugs to treat Herpes simplex virus (HSV) infections have toxic side effects and there has been an emergence of drug-resistant strains. Therefore, the search for new treatments for HSV infections is mounting. In the present study, semi-solid formulations containing a crude hydroethanolic extract (CHE) from Schinus terebinthifolia were developed. Skin irritation, cutaneous permeation, and in vivo therapeutic efficacy of the formulations were investigated. Treatment with the ointment formulations did not result in any signs of skin irritation while the emulsions increased the thickness of the epidermis in Swiss mice. The cutaneous permeation test indicated that the CHE incorporated in the formulations permeated through the skin layers and was present in the epidermis and dermis even 3 h after topical application. In vivo antiviral activity in BALB/c mice treated with the CHE ointments was better than those treated with the CHE emulsions and did not significantly differ from an acyclovir-treated group. Taken together, this suggests that the incorporation of CHE in the ointment may be a potential candidate for the alternative topical treatment of herpetic lesions.

Produtos em filme ? Inovação na tecnologia de cosméticos / Film products - Innovation in cosmetics technology

A indústria cosmética tem investido fortemente na pesquisa e no desenvolvimento de novos produtos, para melhor atender as exigências do consumidor. Como inovação neste segmento têm despontado os cosméticos em filme. A partir de uma fórmula inicial, contendo como formador de película um polissacarídeo constituído de maltotriose e como agente gelificante sodium polyacrylate, foram obtidos géis viscosos que foram espalhados em placas de vidro, de maneira a se obter filmes de 1 mm de espessura. Após secagem à temperatura ambiente, os mesmos foram recortados (1 cm2) e acondicionados. Várias alterações foram realizadas a fim de se obter um filme flexível, com rigidez adequada, ausência de rachaduras e de bolhas, fácil dissolução em água e sensorial agradável. As formulações foram submetidas a diferentes temperaturas para avaliação preliminar da estabilidade. Foram desenvolvidos dois produtos, um contendo extratos hidroglicólicos de Aloe Vera e de Rosa Branca, auxiliares no tratamento da acne, e outro contendo extratos hidroglicólicos de Camomila e de Pera, auxiliares no combate a olheiras. Pequenos, leves e finos, os cosméticos em filme representam inovação que pode ocupar o lugar de produtos tradicionais, por proporcionarem maior praticidade e facilidade de uso e de transporte, mantendo a eficácia e a segurança necessárias a um cosmético.

The cosmetics industry has invested heavily in the research and development of new products, to satisfy consumer demands. As a result of the innovation in this sector, cosmetics have emerged in film format. Starting from an initial formula containing a polysaccharide consisting of maltotriose units as a film former and sodium polyacrylate as gelling agent, viscous gels were obtained and dispersed in glass plate, in order to obtain 1 mm thick films. After drying to room temperature, they were cut out (1 cm2) and conditioned. Various alterations were carried out in order to obtain a film with good flexibility, adequate rigidity, without cracks and bubbles, easy dissolution in water and a pleasant feel. The formulations were submitted to different temperatures, for preliminary evaluation of their stability. Two products were developed: one containing hydroglicolic extracts from aloe vera and white rose, auxiliaries in the treatment of acne, and another containing hydroglicolic extracts from chamomile and of pear, used to combat dark circles under the eyes. Small, light and thin, film cosmetics are an innovation that can take the place of traditional products, as they offer greater practicality and ease of use and transport, maintaining the effectiveness and safety necessary for cosmetics.

In vitro antibacterial activity of a 7-O-beta-D-glucopyranosyl-nutanocoumarin from Chaptalia nutans (Asteraceae)

Ethanolic crude extracts from the roots of Chaptalia nutans, traditionally used in Brazilian folk medicine, were screened against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa by using the disk diffusion test technique. S. aureus with 14 mm inhibition zone was considered susceptible. E. coli and P. aeruginosa without such a zone were considered resistant. As a result of this finding, the ethanolic crude extract was fractionated on silica gel column chromatography into five fractions. The ethyl acetate fraction was active against S. aureus and Bacillus subtilis. Further column chromatography separation of the ethyl acetate fraction afforded 30 fractions, which were assayed against S. aureus. Fractions 16 and 17 showed inhibition zones with S. aureus, indicating the presence of active compounds, and were subjected to purification by repeated preparative thin layer chromatography. The pure compound 7-O-beta-D-glucopyranosyl-nutanocoumarin inhibited B. subtilis and S. aureus at concentrations of 62.5 æg/ml and 125 æg/ml, respectively. The antibacterial property of C. nutans appears to have justified its use for the treatment of wounds, which are contaminated through bacterial infections