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Systemic arterial hypertension (SAH) is a major health problem around the world and its development has been associated with exceeding salt consumption by the modern society. The mechanisms by which salt consumption increase blood pressure (BP) involve several homeostatic systems but many details have not yet been fully elucidated. Evidences accumulated over the last 60 decades raised the involvement of the immune system in the hypertension development and opened a range of possibilities for new therapeutic targets. Green propolis is a promising natural product with potent anti-inflammatory properties acting on specific targets, most of them participating in the gut-brain axis of the sodium-dependent hypertension. New anti-hypertensive products reinforce the therapeutic arsenal improving the corollary of choices, especially in those cases where patients are resistant or refractory to conventional therapy. This review sought to bring the newest advances in the field articulating evidences that show a cross-talking between inflammation and the central mechanisms involved with the sodium-dependent hypertension as well as the stablished actions of green propolis and some of its biologically active compounds on the immune cells and cytokines that would be involved with its anti-hypertensive properties.

The reuse of agro-industrial residues is vital to minimize their environmental impact and alternatives for their application are needed. In this research, we evaluated the chemical composition as well as antioxidant and antibacterial activities of the extract from hot trub, that is the second solid waste obtained during the brewing process. Total phenolic and flavonoids compounds were determined by colorimetric assays and the compounds were identified by UHPLC-DAD-MS/MS. Antioxidant activity was evaluated by ABTS and DPPH methods. Antibacterial activity against Gram-positive and Gram-negative bacteria was analyzed by agar diffusion and microdilution methods. Cytotoxicity was evaluated against murine fibroblast L929 cell line by MTT assay. The results showed that the content of phenolic and flavonoid compounds ranged according to the fractions from 8.237 to 13.390 mg GAE/g and from 0.019 to 1.643 mg QE/g, respectively. The compounds cohumulone, cohulupone, hulupone/adhulupone, isoxanthohumol, xanthohumol, hydroxytricyclocolupone epimers, hydroxytricyclolupone/hydroxytricicloadlupone epimers and nortricyclocolupone were suggested. Higher antioxidant activity was observed for the crude ethanol extract. The hexane fraction presented the lowest MIC value against Gram-positive bacteria, as well as lower cytotoxicity. These results are promising and indicate a great potential for the reuse of this byproduct as a source of natural antioxidant and for the microbiological applications, which consequently would reduce the environmental impact.

Bladder cancer has a high incidence and recurrence rate among patients worldwide. This study aimed to evaluate the cytotoxic activity of fractions of Sambucus nigra L. flower extracts on bladder carcinoma cells (T24 cells) and human fibroblast cells (MRC-5). The butanolic fraction (F-BuOH) was characterized by UPLC-DAD-MS/MS and nine flavonoids were identified. Rutin was the major compound. The cytotoxic activity of this fraction was observed in the T24 cells but not in MRC-5 cells, indicating selectivity. F-BuOH was incorporated in micellar solutions of Pluronic® F127 and cytotoxic effect for T24 cells was observed again. In vitro assay demonstrated a controlled release of the fraction from the micelles. The results obtained showed that flavonoids are the possible responsible for cytotoxic activity in bladder carcinoma cells. In addition, micellar solutions act together to increase the action of the butanolic fraction.

The physicochemical characteristics of nanostructured suspensions are important prerequisites for the success of new drug development. This work aimed to develop nanometric systems containing Cymbopogon densiflorus leaf essential oil and to evaluate their antimicrobial activity. The essential oil was isolated by hydrodistillation from leaves and analyzed by GC-MS. The main constituents were found to be trans-p-mentha-2,8-dien-1-ol, cis-p-mentha-2,8-dien-1-ol, trans-p-mentha-1(7),8-dien-2-ol, cis-piperitol, and cis-p-mentha-1(7),8-dien-2-ol. In silico prediction analysis suggested that this oil possesses antimicrobial potential and the main mechanism of action might be the peptidoglycan glycosyltransferase inhibition. Nanoemulsions were prepared by the phase inversion method, and liposomes were made by the film hydration method. Qualitative evaluation of the antimicrobial activity was performed by the diffusion disk assay with 24 microorganisms; all of them were found to be sensitive to the essential oil. Subsequently, this property was quantified by the serial microdilution technique, where the nanoformulations demonstrated improved activity in comparison with the free oil. Bactericidal action was tested by the propidium iodide method, which revealed that free essential oil and nanoemulsion increased cytoplasmic membrane permeability, while no difference was observed between negative control and liposome. These results were confirmed by images obtained using transmission electron microscopy. This study has shown an optimization in the antimicrobial activity of C. densiflorus essential oil by a nanoemulsion and a liposomal formulation of the active substances.

The research for new treatments of skin and soft tissue infections (SSTIs) is important due to their high prevalence and number of hospitalizations. The purpose of this review is to address the pathophysiology of SSTIs to highlight the advantages of herbal medicines to their treatment, showing examples of species and compounds with multi-targets action. SSTIs have a complex physiopathology involving the microorganism, as well as inflammation and difficult healing. Therefore, antimicrobial, anti-inflammatory, antioxidant and healing activities are an approach possible for their treatment. Herbal medicines have a wide diversity of biological compounds, mainly phenolic compounds that may act on different targets and also have synergism between them. Therefore, a single medicine may have the four key activities that allied allow eliminating the infection, control the inflammation process and accelerating the healing process, preventing complications with chronic infections.

Propolis has demonstrated potential use as food preservative but it presents strong and unpleasant flavor that alters the sensory characteristics foods. A nanoemulsion was proposed to carry the Brazilian propolis extracts for use as natural food preservative. Antimicrobial and antioxidant activities and chemical constituents of the extracts were investigated. The latter were made by sequential extraction using different solvents (hexane, ethyl acetate and ethanol). Antimicrobial activity was evaluated by agar diffusion and microdilution methods and antioxidant activity by DPPH and ABTS assays. Extracts showed antibacterial and antioxidant activity, highlighting the ethanolic which contained artepillin-C, kaempferide, drupanin and p-coumaric acid as main compounds by LC-MS analysis. The nanoemulsion developed by phase inversion method was characterized and stable under thermal-stress and centrifugation conditions. Biological properties evaluated were effectively maintained by the formulation. It was concluded that the nanoemulsion can be used as a food preservative, preventing degradation and masking the propolis off-flavor.

The excessive sun exposure, coupled with lack of sun protection represents one of the biggest risks to the occurrence of skin cancer and photoaging. Recent strategies for photoprotection have included the incorporation of natural antioxidant and anti-inflammatory compounds, into sunscreens, and the oral administration of natural antioxidant extracts. In this work, we use Brazilian red propolis extract because its antioxidant and anti-inflammatory activities. The aim of this work was to evaluate the sun protection factor and antioxidant activity of different hydroalcoholic extracts of red propolis (70% and 75%) prepared from lyophilized red propolis at room and high temperatures. The sun protection factor in vitro was determined by a spectrophotometric method developed by Mansur. The hydroalcoholic extracts of red propolis incorporated with Filter UVA-UVB 5% Gel Permulem TR-1 presented absorption in the UVB region. Also, the in vitro capacity of the hydroalcoholic extracts of red propolis to increase photoprotective activity of Filter UVA-UVB 5% Gel was evaluated. The hydroalcoholic extracts of red propolis incorporated presented higher values of sun protection factor and showed synergism in the photoprotective activity of Filter UVA-UVB 5% Gel Permulem TR-1. The antioxidant activity and sun protection factor are correlated with total phenolics content of the extracts and the hydroalcoholic extract of red propolis 75% at room temperature was choosen. The formulation developed with Filter UVA-UVB 5% Gel Permulem TR-1 with this hydroalcoholic extract of red propolis showed safe to be applied on the skin according HET-CAM test. Suggests indication of hydroalcoholic extract of red propolis (75% – room temperature) associated to photoprotective formulations for use in photoprotective products. Keywords: Sun protection factor, Red propolis, Filter UVA-UVB, Total phenolics, HET-CAM test, Antioxidant activity

Due to the increase of bacterial resistance, the search for new antibiotics is necessary and the medicinal plants represent its most important source. The aim of this study was to evaluate the antibacterial property of extract and fractions from Protium spruceanum leaves, against pathogenic bacteria. By means of diffusion and microdilution assays, the crude extract was active against the nine bacteria tested being the hydromethanolic fraction the most active. During phytochemical procedures, procyanidin (1) and catechin (2) were identified as the main antibacterial constituents of this fraction. In silico results obtained using PASSonline tool indicated 1 and 2 as having good potential to interact with different targets of currently used antibiotics. These results no indicated potential to none DNA effect and indicated the cell wall as mainly target. Electrophoresis result supported that had no DNA damage. Cell wall damage was confirmed by propidium iodide test that showed increased membrane permeability and by cell surface deformations observed in scanning electronic microscopy. The in vitro assays together with the in silico prediction results establish the potential of P. spruceanum as source of antibacterial compounds that acts on important bacterial targets. These results contribute to the development of natural substances against pathogenic bacteria and to discovery of new antibiotics.

The new severe acute respiratory syndrome coronavirus (SARS-CoV-2) recently emerged as a worrying pandemic, with many confirmed cases and deaths globally. Therefore, there is a clear need for identifying effective therapeutic options and a review of secondary metabolites related to Brazilian herbal medicines was performed as a strategy for the discovery of new antiviral agents. To confirm this potential, an in silico screening of the identified compounds identified was also evaluated. The review was performed by the PubMed database and the selected natural compounds were subjected to in silico analysis such as QSAR, molecular docking and ADMET. 497 secondary metabolites were identified from 23 species. The in silico assays indicated 19 potential anti-SARS-CoV-2 compounds, being triterpenes and phenolic compounds. The indicated compounds showed a high affinity with proteins considered as the main molecular targets against SARS-CoV-2 and parameters indicated low toxicity. In addition to Brazilian medicinal plants, these compounds can be found in other species and they can be a base for the synthesis of other anti-COVID-19 drugs. Therefore, this review is important to conduct researches that address the emerging need for drugs in COVID-19 treatment.

Chromone derivatives exhibiting high absorbance values in the UVA/UVB region were synthesized, and their photoprotective properties were evaluated. Chromones were prepared according to known literature procedures and characterized by high resolution mass spectrometry, infrared (IR) and nuclear magnetic resonance (NMR) spectroscopy. The in vitro solar protection factor (SPF) was determined by the Mansur method and cytotoxicity was evaluated using the sulforhodamine B assay. Two of the chromones synthesized demonstrated suitable SPF values and displayed no cytotoxic effect towards MRC-5 human fibroblasts at the tested concentrations, indicating great potential for future in vivo assays and clinical trials. Finally, the lead compound was incorporated into a nanoemulsion. Nanoemulsions showed high droplet size homogeneity and excellent stability. Chromones bearing methoxy substituents were found to be the most promising compounds with ideal photoprotective properties desirable for utilization and incorporation in sunscreen formulations.

Selecting a polymer depends on its characteristics, the properties of the drug and of the remaining ingredients in the formulation. The drug, when incorporated into a polymeric matrix, can show several advantages when compared with its conventional form. In this context, this work describes the preparation and characterization of polyethylene glycol (PEG 4000) and its derivative particles loaded with benznidazole, as well as evaluates their trypanocidal activity. In this work, reactions to modify the PEG 4000 polymer and the subsequent incorporation of the benznidazole were made. The nuclear magnetic resonance (NMR) analysis confirmed the efficiency in modifying the PEG chains. The morphology of polymeric films was observed by atomic force microscopy (AFM) and showed considerable changes on the film organization. The acetylation of PEG favored the stability of the system and an increase in the zeta potential from -14.83 to -25.54 mV was observed. Although encapsulation efficiency values between 30.14 and 39.48% were found, the enhanced benznidazole dissolution profile by microparticles enables the use of lower drug concentrations. This fact can be proven by the increased trypanocidal effect of benznidazole when encapsulated in BP3 microparticles. Finally, the high selectivity of the formulations for trypanocidal action guarantees their safety as an alternative for the treatment of the Chagas disease.

The high prevalence of diabetes and obesity encourages research for the development of α-glucosidase inhibitors from natural sources. This study evaluated the activity of fractions obtained from Protium spruceanum branches. Anti-α-glucosidase activity was investigated in vitro using 4-nitrophenyl-α-D-glucopyranoside as the substrate, while free-radical scavenging activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azinobis-3-ethylbenzotiazoline-6-sulfonic acid (ABTS) assays. Furthermore, a model of oxidative stress promoted by H2O2 in fibroblasts was employed, and cell viability was determined by sulforhodamine B. Fractions inhibited α-glucosidase activity effectively, highlighting the hydromethanolic fraction (HMF). Quercitrin, isolated from the HMF, was identified by spectroscopy and quantified by a validated high performance liquid chromatography with diode array detector (HPLC-DAD) method and exhibited free radical scavenging activity comparable to the HMF. However, this flavonoid showed low anti-α-glucosidase effect, suggesting a synergism effect among several components of the HMF. This proposal is also supported by the docking results obtained by PyRx software. The compounds present in the HMF showed a noncompetitive inhibition at the in silico simulation. Finally, the HMF also protected fibroblasts against cell death induced by oxidative stress. This is the first evidence of the capacity of P. spruceanum branches to inhibit α-glucosidase activity and to counteract oxidative stress. These results encourage the use of this Brazilian plant against hyperglycemia-correlated diseases.

Bladder cancer has a high incidence and recurrence rate among patients worldwide. This study aimed to evaluate the cytotoxic activity of fractions of

A viscous solution of low molecular weight chitosan (CH) at 5% w/v (10.2 kDa, 75 % deacetylated, 1451 cP at 25 °C) was associated with a microemulsion (ME) that undergoes a phase transition after water absorption in situ (≈28 % w/w), forming a more viscous liquid crystal, which was potentially evaluated as a topical vehicle. The ME was selected from a phase diagram, selecting a composition based on Tween® 80 (52 %), myristate isopropyl (28 %), and the aqueous phase (water and polyethylene glycol 400, 60:40 w/w) (20 %), which was after replaced by CH and herbal medicines (HM). HM are alternatives to treat candidiasis, and Stryphnodendron adstringens shell extract, characterized by molecular networking, and Melaleuca alternifolia Chell essential oil (46 % of terpinen-4-ol), showed in vitro activity against Candida albicans. Associating CH in ME improved the mechanical properties of the topical formulation, as adhesiveness, which is an advantageous feature for the topical treatment of vulvovaginal candidiasis.

Recently, there has been a demand for the replacement of chemical sunscreens with natural compounds that could prevent or restore UV-induced skin damage. Here, we investigated the photoprotective influence of the Melaleuca leucadendron ethanolic flower extract (EEMec) on factors involved in cellular and molecular UVB-induced oxidative stress in human skin keratinocytes (HaCaT). The phytochemical constituents, antioxidant potential by DPPH assay, content of total phenolic and flavonoid compounds in EEMec were evaluated. HaCaT cells were treated with EEMec followed by irradiation with UVB. CAT activity; GSH and ROS levels; and SOD1, GPx, CAT and COX-2 expression assays were employed to verify the oxidative stress, as well as EEMec effect on transmembrane transport, and pro-inflammatory and pro-apoptotic protein expression. EEMec reverted the viability loss of HaCaT cells after irradiation with UVB, exhibited significant antioxidant capacity and free radical scavenging activity in vitro, inhibited COX-2 expression and ensure protection of DNA-damage. EEMec shown a great photoprotective property to prevent keratinocytes damage induced by UV radiation and, thus a candidate potential to application as an adjuvant in sunscreen formulations as a strategy to reduce risk of sunburn and prevent skin diseases associated with UV-induced inflammation and cancer.

The emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in China and its spread worldwide has become one of the biggest health problem due to the lack of knowledge about an effective chemotherapy. Based on the current reality of the SARS-CoV-2 pandemic, this study aimed to make a review literature about potential anti-coronavirus natural compounds guided by an in silico study. In the first step, essential oils from native species found in the Brazilian herbal medicine market and Brazilian species that have already shown antiviral potential were used as source for the literature search and compounds selection. Among these compounds, 184 showed high antiviral potential against rhinovirus or picornavirus by quantitative structure–activity relationship analysis. (E)-α-atlantone; 14-hydroxy-α-muurolene; allo-aromadendrene epoxide; amorpha-4,9-dien-2-ol; aristochene; azulenol; germacrene A; guaia-6,9-diene; hedycaryol; humulene epoxide II; α-amorphene; α-cadinene; α-calacorene and α-muurolene showed by a molecular docking study the best result for four target proteins that are essential for SARS-CoV-2 lifecycle. In addition, other parameters obtained for the selected compounds indicated low toxicity and showed good probability to achieve cell permeability and be used as a drug. These results guided the second literature search which included other species in addition to native Brazilian plants. The majority presence of any of these compounds was reported for essential oils from 45 species. In view of the few studies relating essential oils and antiviral activity, this review is important for future assays against the new coronavirus. Supplementary Information The online version contains supplementary material available at 10.1007/s11101-021-09754-4.

The aim of this study was to analyse the antitumor effect of the

Essential oils are potential antimicrobial agents and can be used as active ingredients in the pharmaceutical, food and cosmetics industries. This work intends to evaluate the antibacterial activity and design a strategy for the proposition of the mechanism of action of Melaleuca leucadendra essential oil. Optimum concentration of the bacteria and the phase where they had the highest pathogenic activity were determined. Results show that for each microorganism it is necessary to use a different concentration at the time of adjusting the initial inoculum, and that the time to achieve exponential growth phase varies from one to the other. M. leucadendra essential oil demonstrated in vitro antimicrobial properties. This oil was chemically characterized and the main compounds were evaluated by their mechanism of antibacterial action based on structure-activity analysis. The mechanism is related to the increase of bacteria cell membrane permeability. This indication was confirmed by flow cytometry and transmission electronic microscopy. Thus, in silico analysis is an important tool in the search for new antimicrobial agents and these results showed that M. leucadendra essential oil may be useful on the development of new chemotherapies or food preservation systems.

Despite many attempts involving TB prevention, diagnosis, and treatment, conventional treatments are often unsuccessful due to two main reasons: poor patient compliance during the long treatment regimen and the emergence of multidrug resistance. Lipid-based nanocarriers are composed of physiological or biocompatible lipids, making them well-tolerated, with the original molecule and their metabolites usually nontoxic. In this chapter, we explore two kinds of lipid-based nanocarriers: solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs). Both of them are produced with solid biocompatible lipids and can be used for delivery anti-TB drugs. High-pressure homogenization, microemulsion technique, emulsification-ultrasonication, film ultrasonication, and solvent emulsification are some of the commonly used methods for the preparation of SLNs and NLCs. Moreover, some anti-TB antibiotics have already been formulated as SLN and/or NLC, including the possibility of specific targeting ligands. Formulations based on SLN and NLC have promising and innovative potential in improving TB treatment.

The aim of this study was to analyse the antitumor effect of the Cymbopogon densiflorus essential oil in silico and in vitro on bladder cancer cells RT4 and T24, with different TP53 status. The oil was extracted by hydrodistillation and the gas chromatography coupled to the mass spectrometry was used for characterisation. In silico analysis was carried out by Pass online software. Cytotoxicity, cell proliferation, cell cycle progression, apoptosis and wound healing assays were performed. Five major compounds were identified. In silico analysis showed that major compounds present high potential for antitumor activities. The treatment with C. densiflorus essential oil reduced cell viability of bladder cancer cells. Only in wild-type cells, the increase of apoptosis rates and the decrease of cell migration were observed. In conclusion, the C. densiflorus essential oil presents antitumor effects on TP53 wild-type and mutated bladder cancer cells, however, the mechanism of action is TP53 status-dependent.

Propolis is a natural, non-toxic resin produced by honey bees that has been used for hundreds of years for its biological activities, such as antimicrobial, anti-inflammatory, anesthetic, cytostatic, and cariostatic properties. Currently, it is used in food, pharmaceutical, and cosmetic industries. The aim of this work was to evaluate the antioxidant activity, sun protection factor, and photostability of different hydroalcoholic extracts of green propolis. All extracts prepared presented high absorption in the UVB region. The extract of 70% green propolis (high temperature) was incorporated into Gel Permulen TR-1. This new formulation presented a higher value of sun protection factor. Besides that, the formulation developed with Gel Permulen TR-1 and the hydroalcoholic extract of 70% green propolis (high temperature) showed good photostability and it was safe to be applied on the skin according the HET-CAM test. These results indicated the potential of hydroalcoholic extracts of 70% green propolis (high temperature) for use in sunscreen.

Although Quercetin absorbs in the UVA/UVB electromagnetic region, it is limited for applications as a UV filter due to its low lipophilicity and capacity to penetrate the epidermis. In order to overcome this limitation, we synthetized and evaluated the photo protective properties of a derivative obtained from Quercetin. The derivative was prepared by alkylation of Quercetin with iodoethane and characterized by IR and NMR spectroscopy. The in vitro Solar Protection Factor was determined by the Mansur method and the cytotoxicity was evaluated using hepatocellular cell (Hep G2) cells. Finally, Quercetin and the corresponding derivative were incorporated in nanoemulsions. Nanoemulsions with particles sizes between 53 and 73 nm were obtained, and polydispersity indexes were around 0.1, indicating good homogeneity of the nanoemulsion particles. The cell viability study for the Quercetin derivative indicated a very low cytotoxicity profile. The chemical modification of Quercetin resulted in a promising compound with improved properties desirable for skin penetration and incorporation into sunscreen formulations.

Tuberculosis is an infectious bacterial disease that causes millions of deaths worldwide. Current treatment recommended by WHO is effective, however it is an extensive and arduous process associated to severe adverse effects, which induces a low patient compliance and the emerging of multidrug resistant tuberculosis. Thus, as a main goal of this study, rifampicin nanoparticles were surface functionalized with a tuftsin-modifed peptide to selectively recognize receptors located on infected alveolar macrophages, enhancing nanoparticles uptake by these cells and improving antimycobacterial activity. A tuftsin-based modified peptide was synthesized and successfully attached to nanoparticles interface (NP-pRIF). In parallel, nanoparticles without peptide were also developed for comparison (NP-RIF). Physicochemical characterization demonstrated that stable and monodisperse nanodelivery systems were obtained, with a controlled drug release profile and non-cytotoxic potential. Moreover, nanoparticles containing peptide were significantly more internalized by macrophages than nanoparticles without peptide over a wide range of time. Both nanoparticles were 2-fold more effective against M. tuberculosis than free rifampicin, suggesting NP-pRIF as a promising strategy for the management of tuberculosis treatment.

The triterpenes α- and β-amyrins display important pharmacological activities. As a result of their high hydrophobia, they present low water solubility and reflect poor oral bioavailability. Different techniques can be used for the improvement of amyrins solubility, one of them is the use of nanoemulsions. Therefore, the method of direct emulsification was used to develop a nanoemulsion of these triterpenes and the resulting drug delivery system was characterized by an in vitro release assay. Encapsulation efficiency higher than 99% was achieved with total release around 30% in 24 h, which suggests that this system could be useful for the administration of α- and β-amyrins by different routes in an efficient way.

Ethnopharmacological relevance Protium spruceanum (Burseraceae) is used in Brazilian traditional medicine as anti-inflammatory, but the factors involved in this activity were not yet characterized. Aims of the study: analyze the aspects involved in the anti-inflammatory activity of polar fractions obtained from extracts of leaves and branches. Materials and methods: Hydromethanolic fraction was obtained by liquid-liquid partition from crude ethanolic extract and its compounds were identified by LC-DAD-MS. Activity tests were performed using LPS + IFN-γ stimulated J774A.1 macrophages. Cytokines were evaluated by CBA kit, NO by Griess method, ROS by DCFH-DA, N-acetylglucosaminidase (NAG) activity by spectrophotometric method, matrix-metalloproteinase (MMP-9) activity by zymography, inducible nitric oxide synthase (iNOS) expression by immunofluorescence and cyclooxygenase (COX-2) expression by Western blot. Results: Fractions induced an increase of IL-6 and IL-10 which leads to the control of pro-inflammatory cytokines levels. The treatment with the fractions also reduced NO production at all concentrations tested in all evaluated periods. ROS production by the macrophages was inhibited by the treatment and the leaves fraction showed the best results with a lower concentration than that observed for the branches. The enzymes assays showed that leaves fraction inhibited NAG and MMP-9 activities, as well as, iNOS and COX-2 expression. These activities can be associated with the presence of procyanidin, catechin, rutin, quercitrin, isoquercitrin and kaempferol-3-O-rhamnoside, major compounds that were identified in the fraction. Conclusions: Anti-inflammatory activity of P. spruceanum is associated to an immunomodulatory effect that leads to inhibition of ROS, NO, NAG, MMP-9, COX-2 and iNOS.

The aim of this study was to evaluate the influence of hydrocolloids (low methoxyl pectin [LMP], guar gum, and carrageenan) on the characteristics of low caloric orange jellies. A mixture design with to 12 tests to determine properties of the jellies. Physical, physicochemical, and sensory analyses were performed. The results were analyzed by response surface methodology and a Tukey mean test at a significance level of 5% (p ≤ 0.05). The formulations with high LMP concentration resulted in low caloric orange jellies that have a rigid structure, light color, more acidic nature and exhibited optimal sensory acceptability. The jelly formulations with carrageenan concentration of 0.25% had lower total sugar values. Therefore, for the preparation of low caloric orange jellies, it is necessary to use LMP concentration between 0.75% and 1% and carrageenan concentration of 0%–0.25% as well as to exclude guar gum.

Polymeric nanoparticles constitute an important drug delivery system with controlled release profile. This article describes a new way to produce polymeric nanocapsules using a vegetable oil nanoemulsion as template. The process occurs in two steps: First, a nanoemulsion was obtained with a low-energy method based on phase inversion emulsification, using 2-ethylhexyl acrylate as lipophilic monomer. The in situ polymerization of the nanoemulsion droplets is induced by the addition of polymerization catalyzers. The mean size of the polymeric nanoparticles was evaluated by photon correlation spectroscopy and atomic force microscopy. Both techniques showed the formation of polymeric nanocapsules with a mean particle size less than 300 nm.

Infections arising from contaminated medical devices are a serious global issue, contributing to antibiotic resistance and imposing significant strain on healthcare systems. Since the majority of medical device-associated infections are biofilm related, efforts are being made to generate either bacteria-repellent or antibacterial coatings aimed at preventing bacterial colonisation. Here, we utilise a nanocapsule mediated slow release of a natural antimicrobial to improve the performance of a bacteria repellent polymer coating. Poly(lauryl acrylate) nanocapsules containing eugenol (4-allyl-2-methoxyphenol) were prepared and entrapped within a interpenetrating network designed to repel bacteria. When coated on a catheter and an endotracheal tube, this hemocompatible system allowed slow-release of eugenol, resulting in notable reduction in surface-bound Klebsiella pneumoniae and methicillin resistant Staphylococcus aureus.

Emulsions containing vegetable oils and anisotropic phases have especially attractive properties in pharmaceutical technology. They are use as vehicle for different kind of drugs, especially those of topical application. Apart from that, many vegetable oil have pharmacological activity, increasing the necessity for the development of new delivery systems for them. We developed emulsions with vegetable oils at a fixed surfactant ratio and observed the formation of liquid crystalline phases. Nine vegetable oils: Andiroba, Apricot, Avocado, Brazil Nut, Buriti, Cupuassu, Marigold, Passion Fruit and Pequi and mineral oil were tested. Surfactant system was consisted by Steareth-2 and Ceteareth-5. Emulsions were prepared by the emulsion phase inversion (EPI) method, presenting high stability independent on the HLB value. Results indicate that this method could be employed to attain stable emulsions, even if the required HLB value is not known.

The recently introduced one-step process to form double emulsions is analyzed using generalized phase diagrams of water, ethylene oxide adduct surfactants, and hydrocarbons. With the process used, we found three factors to be involved in the successful formation of double emulsions. Temporary ultra-low interfacial tension allowed drops of irregular shape to exist, a large part of the emulsion formed a bicontinuous microemulsion at intermediate times, and the interfacial tension was temporarily reduced extremely by significant amounts of all three compounds transferred over the interfaces in different directions depending on the stage of the process.

The essential oil from leaves of Eremanthus erythropappus (DC.) MacLeish (Asteraceae) collected in South-eastern Brazil was extracted using a combination of water and steam distillation and investigated by chromatography/mass spectrometry (GC-MS). The sesquiterpene hydrocarbons were predominant (46.6%), followed by oxygenated sesquiterpenes (29.3%) and monoterpene hydrocarbons (18.8%). The major compounds were (β)-caryophyllene (29.3%), caryophyllene oxide (22.1%) and β-pinene (12.8%). The allelopathic activity of E. erythropappus essential oil on the seed germination and radicle length of seedlings was evaluated in lettuce (Lactuca sativa L.), tomato (Lycopersicum esculentum Mill.) and in two field weeds (field mustard – Brassica rapa L. and hairy beggarticks – Bidens pilosa L.). Among the weed species tested, the most significant inhibition of seed germination was observed in field mustard, as measured by the half–minimal inhibitory concentration, IC50 (IC50=26.5μL mL–1), and the most significant inhibitory effect on radicle length of seedlings was observed in seedlings of hairy beggarticks (IC50=16.3μL mL–1). In contrast, the lowest allelopathic effects of E. erythropappus essential oil on seed germination and radicle length of seedlings were observed in tomato (IC50=>200μL mL–1 and 130.1μL mL–1 respectively) and lettuce (IC50=97.1μL mL–1 and 35.1μL mL–1 respectively). These results revealed significant allelopathic potential of E. erythropappus essential oil against weeds, but minimal effect on lettuce and tomato germination, and thus suggests it is feasible to use E. erythropappus sustainability as an eco-friendly bioherbicide in cropping settings.

Optical microscope and centrifugation were used to observe the structure change during evaporation of three different commercial emulsions of unknown composition. The degree of evaporation under an infrared lamp at 70°C was determined from the changed weight of a microscope slide with the emulsion on a defined area and thickness. The results revealed information as to which kind of structure would appear after evaporation.

Emulsions surfer alterations in their microstructure after applied on the skin, because of the interaction with skin constituents and mainly by the evaporation of volatile components. These alterations are not even considered by cosmetic formulators, but they are extremely important because they can act on formulation stability, on delivery and on permeation of actives and also on the ability to build the occlusive film, responsible for skin's moisturization. This research studied the phase changing during evaporation of emulsions made with three different oil phase: mineral oil, avocado oil, and isocethyl/stearoil stearate, as a function of the decrease on water ratio, using phase diagrams and evaporation test. It was observed the formation of liquid crystalline phases and their transition along the evaporation path for emulsions with the three different oil phases. It was also observed that these transitions occurred in different water ratios.

Emulsions containing liquid crystals present interesting properties and advantages such as the skin moisturize increase, active release modulation, and emulsion stabilization. In this work, emulsions containing annatto, coffee and tea tree oils, and nonionic surfactants were developed. The HLB method was used for selection of surfactants. The required HLB value was established (9.0). Liquid crystals were attained when used the surfactant mixture Ceteareth‐5 and Steareth‐2 and identified as lamellar. The emulsions showed pseudoplastic behavior and tixotropy. The ternary diagram was useful in the selection of the proportion of surfactant and oily phase considering skin compatibility and liquid crystal presence.

The effects of some composition variables on the development of multiple emulsions by one‐step method were evaluated and their morphology characterized. The formulations that remained stable during the period of the test were submitted to centrifugation and thermal stress tests. The stability and the morphology of multiple droplets were affected not only by the type and concentration of the surfactants employed, but also by the water/oil ratios used. The results suggest that the formation of multiple droplets could involve a combination of transitional and catastrophic phase inversions. The results provide improved knowledge about the one‐step emulsification method, a simplified process to prepare multiple emulsions when compared to the two‐steps method.

Oil/water emulsions, containing liquid crystals, were developed employing Andiroba oil, PEG-12 Dimethicone and Crodafos CES. It was evaluated the influence of silicone surfactants on the emulsions stability and on the formation of liquid crystalline phases and therefore, physicochemical characteristics, such as rheology and zeta potential, were evaluated. Emulsions were prepared by the emulsions phase inversion method. All the formulations presented lamellar liquid crystalline phases. The PEG-12 Dimethicone addition did not change microscopically the liquid crystalline phases. The emulsions containing silicone demonstrated lower viscosity than those without the additive. This is an important feature, as the silicone did not change the rheological profile; however, the addition of silicone still can be used as a viscosity controller. The formulations had their viscosity increased 15 and 150 days after their preparation. This characteristic shows that the emulsions have their organization increased along the storing time. In the analysis of zeta potential, we could verify that all formulations presented negative values between -39.7 and -70.0 mV. Within this range of values, the emulsion physical stability is high (Fig. 10). It was concluded that the addition of PEG-12 Dimethicone kept the liquid crystalline phase of the emulsion obtained with Crodafos CES, influencing in a positive way in the system stability.

Ultrasound is widely used in several chemical reactions and other process, including production of nanocapsules by in situ polymerization. In this work, the main objective was to evaluate the impacts and viability of successive ultrasound application in nanoemulsions to obtain nanocapsules. Initiator potassium persulfate (KPS) concentration, number of ultrasound cycles and reaction time influences on polymerization efficiency and droplet size were evaluated. This work revealed the successful in situ production of nanocapsules using successive shorts cycles of ultrasound. Number of cycles was the only parameter that not exerted significant influence in polymerization yield. Particle size decay was observed in all nanoemulsions after the first ultrasound application, the same was not observed in further cycles. Gravimetric assessment showed remarkable increase of monomer conversion, indicating that once started polymerization continued at least until 28 days after ultrasound application. Concluding, ultrasound short cycles can be used with no harm to formulation, if carefully performed and, furthermore is a potential cost-effective route for polymerization reactions.

Emulsion stability is controlled by the physicochemical properties of the adsorbed layers formed on the surface of the droplets. Zeta potential and droplet size measured initially and during storage can estimate O/W emulsion stability. The aim of this study was to characterize and evaluate the effects of different hydrolyzable compounds employed in pharmaceutical and cosmetic preparations on the zeta potential and droplet size of canola O/W nano‐emulsions and, consequently, the emulsion stability. The samples containing additives demonstrated significant change in zeta potential, but in spite of that, no macroscopic instability was observed. Yet the droplet size values did not undergo significant change.

During evaporation, the rate between volatile and nonvolatile components in an emulsion changes. In this study, emulsions of marigold and canola oil were made according to a phase diagram, simulating the decreasing water amount that happens when the water evaporates from an emulsion. In addition, two basic emulsions were submitted to evaporation and then to microscopic analysis to compare the results of both tests. It was observed that when the water rate decreases, the liquid‐crystalline phase changes its organization, reaching a proportion that it is not hydrated anymore, having a solid aspect. Moreover, these emulsions submitted to evaporation remained to show lamellar phase even when there was no water in the formulation. This is interesting to understand the behavior of an emulsion after it is applied under the skin.

O/W emulsions with liquid crystals are complex systems for the delivery of actives into the skin surface since they modulate the release rate in the structure, and they increase the stability and solubility of slightly soluble substances in oil or aqueous phase and support moisturing by decreasing the transepidermal water loss (TEWL). The development of emulsions with vegetable oils is interesting due to their properties; in addition it allows the use of natural raw materials of Brazil's biodiversity, and it has attracted growing attention in the market because of the marketing value of natural products. Following this trend, emulsions were developed containing annatto oil as oily phase. HLB system was used for selection of emulsifying agents because it aids in the correct determination of the ratio of surfactant in a mixture for a better emulsification. In this study, the HLB value of annatto oil was established using nonionic surfactants, such as oleth‐3 and oleth‐20. With the replacement of these by ce...

The aim of this study was to develop O/W emulsions with a self‐emulsifying base (SEB) containing liquid crystals (LC) and evaluate the influence of polyhydroxy alcohols and peach oil addition in liquid crystal formation as well as to analyze the rheological behavior of these systems. Formulations containing SEB were supplemented or not with glycerin, sorbitol, propylene glycol, and/or peach oil. All formulations studied had lamellar crystalline phases. Peach oil addition increased the viscosity of SEB, while humectants had different behavior, glycerin enhanced the viscosity of the studied formulations supplemented or not with peach oil, and propylene glycol decreased the viscosity of all formulations studied. On the other hand, sorbitol enhanced the viscosity of formulations containing peach oil. All emulsions presented pseudoplastic behavior and thixotropy.

Development of new formulations for topical use and cosmetic and pharmaceutical delivery agents has increased the complexity of emulsified systems. Liquid crystals, known since the nineteenth century are the third phase of an emulsion, being responsible for increasing its stability and the solubility of substances poorly soluble in water, or the oily phase, modulating the release of drugs imprisoned in its structure and promoting hydration of the skin surface. In the present work we developed oil/water emulsions, making use of Marigold oil (Calendula officinalis L) and ethoxylated fat alcohols as surfactant. The required HLB value for marigold oil was determined to be 6.0. The surfactants were associated in lipophilic/hydrophilic pairs. The lipophilic surfactants were Ceteth‐2 and Steareth‐2 and the hydrophilic surfactants were Steareth‐20, Ceteareth‐20, Ceteareth‐5, and Ceteth‐10. To identify the liquid crystalline phases, the emulsions were analyzed by polarized light microscopy. The physical stability ...