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Piper crassinervium Kunth (Piperaceae) essential oil (EO) was evaluated for its toxicity and repellency against red imported fire ants (RIFA), Solenopsis invicta Buren, and a hybrid (HIFA) of red (S. invicta) and black (S. richteri Forel) imported fire ants. Through bioactivity-guided fractionation, two major components, elemicin and myristicin, were isolated from the EO. Removal of treated sand in a digging bioassay was used as the criterion for repellency. The EO showed significantly higher repellency at concentrations of 7.8 µg/g against RIFA and HIFA workers, as compared to the DEET (N,N-diethyl-meta-toluamide) or ethanol control. Elemicin exhibited repellency at 3.9 and 7.8 µg/g against RIFA and HIFA workers, respectively, whereas myristicin was active at 7.8 µg/g against both species. DEET failed at 31.25 µg/g against RIFA and 15.6 µg/g against HIFA. The EO showed LC50 values of 97.9 and 73.7 µg/g against RIFA and HIFA workers, respectively. Myristicin was more toxic against RIFA and HIFA with LC50 values of 54.3 and 35.3 µg/g, respectively. Elemicin showed 20–40% mortality at the highest screening dose of 125 µg/g. Fipronil exhibited the highest toxicity against RIFA and HIFA, with LC50 of 0.43 and 0.51 µg/g, respectively. Different formulations of these natural products should be evaluated to explore their use potential under natural field conditions.

This research investigates the morpho-anatomical characteristics of seven Baccharis species, namely B. articulata, B. milleflora, B. myriocephala, B. pentaptera, B. riograndensis, B. sagittalis and B. trimera. Commonly called carquejas, these species have aerial photosynthetic winged stems known as cladodes and are widely used traditionally to treat digestive and diuretic disorders. This study aimed to characterize these commonly misidentified species using morphological and microscopic techniques, including light and scanning electron microscopy coupled with energy-dispersive X-ray spectroscopy. Trichomes, the presence or absence of oil bodies, and a subepidermal collenchyma layer at the wing edge were identified as primary anatomical markers that can help differentiate the studied species.

Abstract Monteverdia ilicifolia (Mart. ex Reissek) Biral (basionym: Maytenus ilicifolia Mart. ex Reissek) (Celastraceae) is popularly known as holy thorn or “espinheira-santa” in Brazil. This herb is traditionally used for gastric and digestive problems. However, similar species are often used as adulterants. Considering the pharmacological interest and the existence of adulterants, this study was devoted to characterizing M. ilicifolia samples by Fourier-transform infrared (FTIR) spectroscopy coupled with principal component analysis (PCA) and photoacoustic spectroscopy (PAS) by using Citronella gongonha (Mart.) R. A. Howard as adulterant sample. Six commercial samples were purchased, and seven collected samples were obtained in the Campos Gerais region. The leaves were then dehydrated and converted to powder. The FTIR spectroscopic assay was carried out and consisted of ten different measurements for each sample with a time interval of seven days between them. The PCA was performed from these spectra. The characterization by FTIR demonstrated the presence of tannins and flavonoids in the studied samples. FTIR spectroscopy coupled with PCA was able to discriminate the commercial and the collected samples of M. ilicifolia using three principal components. The photoacoustic spectroscopy resulted in absorption bands centered at ~280, ~380, ~480, and ~630 nm. These bands presented a higher spectral resolution for the collected samples. The commercial samples showed broadening bands, which allowed the differentiation between these two sets of samples. FTIR spectroscopy coupled with PCA, and photoacoustic spectroscopy are alternative tools for the differentiation of M. ilicifolia samples.

Abstract Baccharis articulata (Lam.) Pers., popularly known as carqueja, carquejinha or carqueja-doce, is a plant widely used in traditional medicine as a diuretic, digestive and antidiabetic. Due to its similar morphology with other species of the "carqueja group", especially Baccharis pentaptera (Less.) DC., it can be easily confused even by specialists. Thus, this study aimed to characterize micromorphology of the crystals present in B. articulata to show botanical markers that can help differentiate this species from other carquejas. Eleven crystalline morphotypes, including druses, styloids and various shapes of prismatic and sand crystals, were evidenced by scanning electron microscopy. In addition, the elemental chemical composition and the degree of hydration of the crystals were analyzed by EDS and Raman spectroscopy. The results of this study would aid in the authentication of B. articulata and serve as a basis for future studies of other species of Baccharis.

Abstract Eugenol is a phenolic compound with numerous biological activities. It is widely used in dentistry to treat toothache and pulpitis. In particular, eugenol may be used for tooth whitening procedures to minimize dental sensitivity in patients. However, eugenol has some disadvantages such as its volatility, its photosensitivity, and immediate effect, which can be avoided by using pharmaceutical nanotechnology. The aim of the present study was to obtain, characterize, quantify, and evaluate the physicochemical stability of eugenol-loaded Eudragit RS100 nanocapsules. The nanocapsules (NCs) were prepared by interfacial deposition of the preformed polymer method. The NCs were characterized through morphological and spectroscopic studies. The encapsulation efficiency was achieved by quantifying the non-encapsulated eugenol using a previously developed and validated analytical method. The physicochemical stability of NCs was assessed at predetermined time intervals for 90 days after preparation. The nanocapsules were successfully prepared by the chosen method and had a predominantly spherical shape with a smooth surface. The mean size, the polydispersion index, and the zeta potential were in agreement to literature data. Infrared spectra ensured that the nanoencapsulation process did not result in chemical reactions between the drug and the polymer. The formulations showed encapsulation efficiency higher than 90% and remained stable after 60 days of preparation. Thus, eugenol-loaded Eudragit RS100 nanocapsules may be further considered as an alternative formulation for dental sensitivity in order to provide a controlled release, a decreased toxicity, and a better dental sensitivity relief.

Abstract Hydroxytyrosol (HT) is a natural phenolic compound found in leaves of olive trees. It is a photosensitive solid phytochemical constituent and an irritant substance to skin and mucosa as pure drug. HT is a lipophilic chemical constituent and shows low solubility in water, bitter taste, and instability to oxidizing atmosphere. Considering the limitations for its suitable therapeutic use, the aim of the present study was to obtain, to characterize, to quantify, and to evaluate the stability of HT-loaded poly(ԑ-caprolactone) nanocapsules for its further use in pharmaceutical and nutraceutical products. Nanocapsules were prepared by method of interfacial deposition of the preformed polymer. The formulations were characterized by morphological and spectroscopic methods. The UHPLC-PDA analytical method was developed and validated for quantifying the HT encapsulation. Physicochemical stability assay was performed for 120 days. Nanocapsules were successfully obtained by the proposed method. The morphological evaluation demonstrated the drug absence in the nanocapsule surface. Fourier-transform infrared spectroscopy demonstrated the drug nanoencapsulation. The analytical method was validated and confirmed a high HT encapsulation efficiency over 95%. Considering the physicochemical stability testing, the polydispersity index changed after 30 days for NC-2 (HT at 2 mg/mL) and after 90 days for NC-5 (HT at 5 mg/mL). Zeta potential changed after 60 days for both formulations (NC-2 and NC-5). pH values were modified after 60 days for NC-5 and after 90 days for NC-2. HT-loaded PCL nanocapsules demonstrate adequate physicochemical features and high drug encapsulation. The different formulations revealed stability changes from 30 to 90 days. Additional in vitro and in vivo evaluations may be performed in order to use these nanoformulations for treating several diseases based on oxidative-inflammatory environments.

Abstract Silsesquioxane 3-n-propylpyridinium chloride (SiPy+Cl-) is a water-soluble polymer that can be used as a promising material with remarkable biological effects. SiPy+Cl- can form thin films on substrate surfaces and shows suitable adhesiveness. Besides, it has high affinity for metal ions. Considering this effect as exchanger polymer and the well-known antimicrobial and cytotoxic features of copper, the aim of this study was to perform the copper functionalization of silsesquioxane 3-n-propylpyridinium chloride Cu-SiPy+Cl-. The SiPy+Cl- was obtained by the sol-gel processing method and the incorporation of copper (II) chloride was carried out by immobilization. Its characterization was performed by spectroscopic methods of Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance (NMR). The FTIR spectrum of SiPy+Cl- showed symmetric and asymmetric stretching of Si-O-Si group and also exhibited vibrational bands of pyridinium ring. The FTIR spectrum of Cu-SiPy+Cl- assigned typical bands displacements of the metal coordination to nitrogen atoms. Spectroscopic data recorded by 13C and 29S NMR confirmed the chemical structures of SiPy+Cl- and Cu-SiPy+Cl-. Concerning to the in vitro susceptibility assay, the antimicrobial activity against Staphylococcus aureus, Escherichia coli and Streptococus mutans was achieved by the agar-well diffusion method. Cu-SiPy+Cl- showed similar cytotoxicity than SiPy+Cl- against Calu-3 and 3T3 cell lines by the MTT colorimetric assay. Further studies are required to investigate the use of Cu-SiPy+Cl- as a novel dental material.

ABSTRACT Objectives: to analyze the diagnostic criteria for ventilator-associated pneumonia recommended by the Brazilian Health Regulatory Agency and the National Healthcare Safety Network/Centers for Disease Control and Prevention, as well as its risk factors. Methods: retrospective cohort study carried out in an intensive care unit throughout 12 months, in 2017. Analyses included chi-square, simple linear regression, and Kappa statistical tests and were conducted using Stata 12 software. Results: the sample was 543 patients who were in the intensive care unit and under mechanical ventilation, of whom 330 (60.9%) were men and 213 (39.1%) were women. Variables such as gender, age, time under mechanical ventilation, and oral hygiene proved to be significant risk factors for the development of ventilator-associated pneumonia. Conclusions: patients submitted to mechanical ventilation need to be constantly evaluated so the used diagnostic methods can be accurate and applied in an objective and standardized way in Brazilian hospitals.

Abstract Eucalyptus species possess anti-inflammatory, antifungal, antibacterial, and insecticidal properties. In this study, the chemical composition and biological activities of Eucalyptus cinerea essential oil (EO) and the leaf and stem anatomy were investigated. EO was extracted by Clevenger apparatus and the compounds were identified by GC/MS. The antioxidant activity was evaluated by DPPH, ABTS, and reducing phosphomolybdenum complex. Broth microdilution was used to determine antimicrobial activity. Cytotoxicity was verified against HeLa, HRT-18, and Calu-3 cells by MTT assay. The cytotoxic mechanism was studied by cell DNA content, cell cycle, and DNA fragmentation. The microscopic analyzes of the leaves and the stems were performed by light microscopy, field emission scanning electron microscopy, and energy-dispersive X-ray spectroscopy. The main constituent of the EO was 1,8-cineole (55.24%). The EO showed low antioxidant and antimicrobial activities. Calu-3 cells showed a significant reduction in viability with IC50 of 689.79 ± 29.34 μg/mL. EO at 1000 μg/mL decreased the DNA content in Jurkat cells. In general, EO increased cell percentage in sub-G0 and S phases with concomitant reduction of cell percentage in G0/G1 and G2/M phases and provided DNA fragmentation of 29.73%. Anatomical and micromorphological features of the leaves and stems can help in the species identification and its differentiation from other Eucalyptus species.

Resumo. Este estudo teve como objetivo obter uma formulação atrativa à base de óleo de citronela e seus componentes voláteis para captura de Diabrotica speciosa (Germar). Três experimentos sequenciais foram realizados em culturas de abobrinha ou pepino. Os insetos foram coletados por armadilhas de garrafa PET com três aberturas laterais, contendo um volume de 200 ml de cada formulação, suspensas a 10 cm do nível do solo numa área experimental de 30 m2. No primeiro experimento foram testados óleo de citronela em 1, 2 e 4%. No segundo investigou-se também a ação de citronelal, citronelol e geraniol a 1%. E, o citronelol a 0,5, 1 e 2% foi testado no terceiro experimento. Como resultado observou-se que a formulação contendo citronelol a 0,5% foi estatisticamente superior às demais. Outros insetos foram capturados pelas armadilhas como coleópteros Diabrotica viridula (Fabricius)e Astylus variegatus (Germar), e também exemplares de Diptera, Hemiptera e Hymenoptera. Considerando a alta demanda por alimentos orgânicos e da preocupação com o ambiente e a saúde, a emulsão a base de citronelol em 0,5% cumpre adequadamente o seu objetivo, garantindo uma boa capacidade atrativa para D. speciosa. Esta formulação pode ser usada paralelamente com outros métodos alternativos para reduzir a presença desse inseto nas culturas. Citronella (Poaceae) essential oil and its components for the control of brasileirinho (Coleoptera: Chrysomelidae) in vegetable crops Abstract. The present study aimed to get an attractive formulation of oil-based citronella and its volatile components to capture Diabrotica speciosa (Germar). Three sequential experiments were performed in zucchini or cucumber crops. The insects were collected in PET bottle traps with three lateral apertures, containing a volume of 200 ml of each formulation, suspended 10 cm above the ground level in an experimental area of 30 m2. In the first experiment citronella essential oil was tested at 1, 2 and 4%. In the second experiment the action of citronellal, citronellol and geraniol at 1% were investigated. Furthermore, citronellol at 0.5, 1 and 2% has been tested in the third experiment. As a result it was observed that the formulation containing 0.5% citronellol was statistically higher than the other tested formulations. Other insects were captured by the traps as the beetles of Diabrotica viridula (Fabricius)and Astylus variegates (Germar), and also copies of Diptera, Hemiptera and Hymenoptera. Considering the high demand for organic food, and concern for the environment and health, the citronellol emulsion at 0.5% adequately fulfilled its goal, ensuring a good attractive capacity for D. speciosa. This formulation can be used simultaneously with other alternative methods to reduce the presence of such insects in crops.

Antibacterial activity and good mechanical properties are some of the characteristics required for an appropriate film dressing. A novel polymer blend was developed for wound healing application. Twenty-four formulations using the polymers chitosan, poly(vinyl alcohol) and/or ɛ-Polylysine and the plasticizer glycerol were designed using factorial design and then the films were prepared by the casting/solvent evaporation method. Seventeen films were obtained among the twenty-four proposed formulations that were characterized by Field Emission Scanning Electron Microscopy (FE-SEM) and Fourier Transform Infrared Spectroscopy (FTIR). Mechanical properties, such as tensile strength (σ), elongation at break (ɛ) and Young’s modulus (Y) as well as antibacterial properties were determined. The best candidate was then further analyzed with regard to porosity, Water Vapor Transmission Rate (WVTR), swelling and cytotoxicity experiments. The results showed a film with semi-occlusive characteristics, good mechanical properties and no toxic. Incorporation of ɛ-Polylysine increased antibacterial activity against gram-negative (Escherichia coli) and gram-positive (Staphylococcus aureus) bacteria.

The objective of this work was to develop and characterize liposomes loaded with silver nanoparticles (LAgNPs) to show improvement in stability characteristics. AgNPs were prepared by the green synthesis method with Aloe vera gel extract and exposure to sunlight. Liposomes were prepared by the modified reverse phase method. Particle size, polydispersity index, zeta potential, as well as the scanning electron microscopy (SEM) morphological aspects of AgNPs and LAgNPs were evaluated. In addition, was used flame atomic absorption spectroscopy to determine the amount of AgNP that was encapsulated in liposomes. The AgNPs presented as amorphous and polydisperse structures, with a mean diameter of 278.46 nm and zeta potential of -18.3 mV. LAgNPs had a mean diameter between 321 and 373 nm, the polydispersity index close to 0.2 and a zeta potential around -40 mV, which indicates greater stability to the AgNPs. The images obtained by SEM show semicircular structures for AgNPs and well-defined spherical shape for LAgNPs. The percentage of encapsulation was between 51.81 to 58.83%. These results showed that LAgNPs were obtained with adequate physicochemical characteristics as a release system.

ABSTRACT Introduction: Third generation of LED light curing units might be used in short exposure periods for orthodontic brackets bonding. Objective: This study evaluated the effect of the different radiant exposure (RE) values: Manufacturers’ instructions (MI), ½ MI, 1/4 MI and Turbo mode. Two third-generation LED curing units were used: VALO® and Bluephase 20i® . The degree of conversion (DC) and Vickers hardness (VHN) of an orthodontic composite (OC) (Transbond XT) under metallic (MB) or ceramic brackets (CB) were measured. Methods: OC was applied to the bracket base, which was then placed over an attenuated total reflectance (ATR) table coupled to an infrared light spectroscope, or to a glass surface for the VHN analysis. The specimens were light-cured and DC values were calculated. The VHN was obtained in a microhardness tester. The data were analyzed with 2-way ANOVA followed by Tukey’s post-hoc test (pre-set α=0.05). Linear regression analysis evaluated the relationship between RE values and dependent variables. Results: CB allowed higher DC and VHN values than MB (p< 0.001). No significant difference was noted among groups when CB were used. For MB, MI groups showed the highest DC and VHN values. A significant, but weak relationship was found between delivered RE values and dependent variables. Conclusions: The decrease in RE values from third generation LED CU did not jeopardize the DC values when CB were used, but can compromise DC and VHN values when MB are used.

Abstract Curcumin (CUR) shows potential use for treating cancer. However, CUR has low solubility and reduced bioavailability, which limit its clinical effect. Therefore, the development of nanocarriers can overcome these problems and can ensure the desired pharmacological effect. In addition, it is mandatory to prove the quality, the efficacy, and the safety for a novel nanomedicine to be approved. In that sense, this paper aimed (a) to prepare CUR-loaded polyethylene glycol-poly(ε-caprolactone) nanocapsules; (b) to validate an analytical method by high performance liquid chromatography (HPLC) for quantifying CUR in these nanoformulations; (c) to evaluate the physicochemical stability of these formulations; and to investigate their cytotoxicity on NIH-3T3 mouse fibroblast cells. The HPLC method was specific to CUR in the loaded nanocapsules, linear (r = 0.9994) in a range of 10.0 to 90.0 µg.mL-1 with limits of detection and quantification of 0.160 and 0.480 µg.mL-1, respectively. Precision was demonstrated by a relative standard deviation lower than 5%. Suitable accuracy (102.37 ± 0.92%) was obtained. Values of pH, particle size, polydispersity index, and zeta potential presented no statistical difference (p > 0.05) for CUR-loaded nanoparticles. No cytotoxicity was observed against NIH-3T3 mouse embryo fibroblast cell line using both the tetrazolium salt and sulforhodamine B assays. In conclusion, a simple and inexpensive HPLC method was validated for the CUR quantification in the suspensions of nanocapsules. The obtained polymeric nanocapsules containing CUR showed suitable results for all the performed assays and can be further investigated as a feasible novel approach for cancer treatment.

Abstract Cilostazol (CLZ) is a phosphodiesterase III inhibitor with antiplatelet and vasodilator properties. It has been recently verified that CLZ plays a significant role in the arteries by inhibiting the proliferation and growth of muscle cells, increasing the release of nitric oxide by the endothelium and promoting angiogenesis. Considering these promising effects, the use of nanocapsules may be an interesting strategy to optimize its pharmacokinetics and pharmacodynamics at the vascular level for preventing atherosclerosis. The aim of this study was to evaluate the effect of cilostazol-loaded nanocapsules in the abdominal aortic tunics and on the lipid profile of Wistar rats in order to investigate its potential role in the prevention of atherosclerosis. Thirty-two animals were divided into four groups of eight animals, with 30-day treatment. Group 1 received nanoencapsulated CLZ; Group 2, control nanocapsules with no drug; Group 3, propylene glycol and water; and Group 4, a solution of CLZ in propylene glycol and water. After 30 days, there was no statistically significant difference between the groups regarding the cellularity and thickness of the arterial tunics of the abdominal aorta. However, the group that received nanoencapsulated CLZ (Group 1) had an improvement in HDL-c and triglyceride values compared to unloaded nanocapsules (Group 2).

Abstract Ocotea porosa (Nees & Mart.) Barroso, commonly known as “imbuia”, “canela-imbuia” or “imbuia-amarela” in Brazil, is a tree of the Southern Atlantic Forest. The present study investigates the anatomy of leaf and stem, volatile oil chemistry, as well as cytotoxicity and insecticidal activities of the essential oil of O. porosa. Species identification was achieved by anatomy features, mainly due to paracytic and anomocytic stomata; non-glandular trichomes; biconvex midrib and petiole with a collateral open arc vascular bundle; presence of a sclerenchymatous layer, starch grains and crystal sand in the stem; and the presence of phenolic compounds in the epidermis, phloem and xylem of the midrib, petiole and stem. The main volatile components of the essential oil were α-pinene (19.71%), β-pinene (13.86%) and bicyclogermacrene (24.62%). Cytotoxicity against human cancer cell (MCF-7), mouse cancer cell (B16F10) and mouse non-tumoral cell (McCoy) was observed as well as insecticidal activity of the essential oil against susceptible ‘Ft. Dix’ bed bugs (Cimex lectularius L.) by topical application.

Background and Objectives: A sepsis is a challenge for public health, and the protocols are fundamental for management. The aim of this study was to evaluate the implementation of a care protocol for the management of sepsis and to characterize the patients submitted to clinical evaluation. Method: Descriptive cross-sectional study performed at the Emergency Service (EC) of the Campos Gerais Regional University Hospital. The protocol was elaborated from the literature, focusing on adult patients with criteria of systemic inflammatory response syndrome (SIRS), sepsis, severe sepsis and septic shock, being described by flowchart. They were part of the study of the patients attended in the EC between july and september of 2016 submitted to the protocol (n=50), being collected by electronic medical records and analyzed descriptively. Results: For the implementation of the protocol, the training was carried out by the EC staff, for acceptance and alignment of knowledge regarding the conceptual, technical and logistical aspects. The protocol consists of 3 steps: initial approach to the patient with sepsis; package 3/6 hours - hemodynamic optimization and optional package - optimization of central venous oxygen saturation/ central venous pressure. Patients submitted to the protocol were mean of 66 years (SD=±13.71), most of them were 56% women, presented hypotension (96%), creatinine elevation (76%) and leukocytosis (70%) among SIRS, achievement immediate exams (100%), initiation antibiotic therapy (74%) and death (72%). Conclusion: an implementation of the protocol subsidized the precocious identification of patients, qualification of care, operational experience and as characteristics of patients consistent with severe sepsis.

Background: Tacrolimus (TAC) is a drug of natural origin used in conventional topical dosage forms to control atopic dermatitis. However, direct application of the drug often causes adverse side effects in some patients. Hence, drug nanoencapsulation could be used as an improved novel therapy to mitigate the adverse effects and enhance bioavailability of the drug. Methods: Physicochemical properties, in vitro drug release experiments, and in vivo anti-inflammatory activity studies were performed. Results: TAC-loaded nanocapsules were successfully prepared by the interfacial deposition of preformed polymer using poly(ε-caprolactone) (PCL). The nanoparticulate systems presented a spherical shape with a smooth and regular surface, adequate diameter (226 to 250 nm), polydispersity index below 0.3, and suitable electrical stability (−38 to −42 mV). X-ray diffraction confirmed that the encapsulation method provided mainly the drug molecular dispersion in the nanocapsule oily core. Fourier-transform infrared spectra suggested that nanoencapsulation did not result in chemical bonds between drug and polymer. In vitro drug dissolution experiments showed a controlled release with a slight initial burst. The release kinetics showed zero-order kinetics. As per the Korsmeyer–Peppas model, anomalous transport features were observed. TAC-loaded PCL nanocapsules exhibited excellent anti-inflammatory activity when compared to the free drug. Conclusions: TAC-loaded PCL nanocapsules can be suitably used as a novel nano-based dosage form to control atopic dermatitis.

Abstract Metallic nanoparticles have great potential as a chemotherapeutic agent. The aim of this study was to develop and characterize silver and gold nanoparticles using a simple method, as well as evaluating the potential cytotoxic activity in relation to the K-562 cell line. For the synthesis, a solution containing the metallic ions was subjected to magnetic stirring with the aqueous extract of Lavandula dentata L. and a change of colour was observed. With the data obtained from the analyses we concluded that the nanoparticles were successfully obtained by a simple and green method using the aqueous extract of L. dentata. The obtained nanoparticles presented a reduced size, a low level of polydispersion, and a homogenous spherical shape. The nanoparticles presented intense and characteristic diffraction peaks, which could be correlated to the planes of the centred cubic structure of the silver and gold. The two formulations presented predominantly crystalline characteristics. The infrared analysis suggested that the amides and alcohols present in the samples may have been responsible for the reduction and limitation of the size and dispersion of the silver and gold nanoparticles. The cytotoxic assay showed that the nanoparticles demonstrated great potential to reduce the cell viability of the K-562 cell line, especially the gold nanoparticles.

Adapalene (ADAP) is an important drug widely used in the topical treatment of acne. It is a third-generation retinoid and provides keratolytic, anti-inflammatory, and antiseborrhoic action. However, some topical adverse effects such as erythema, dryness, and scaling have been reported with its commercial formula. In this sense, the microencapsulation of this drug using polyesters can circumvent its topical side effects and can lead to the enhancement of drug delivery into sebaceous glands. The goal of this work was to obtain ADAP-loaded poly(ε-caprolactone) (PCL) microparticles prepared by a simple emulsion/solvent evaporation method. Formulations containing 10 and 20% of ADAP were successfully obtained and characterized by morphological, spectroscopic, and thermal studies. Microparticles presented encapsulation efficiency of ADAP above 98% and showed a smooth surface and spherical shape. Fourier transform infrared spectroscopy (FTIR) results presented no drug-polymer chemical bond, and a differential scanning calorimetry (DSC) technique showed a partial amorphization of the drug. ADAP permeation in the Strat-M membrane for transdermal diffusion testing was evaluated by photoacoustic spectroscopy (PAS) in the spectral region between 225 and 400 nm after 15 min and 3 h from the application of ADAP-loaded PCL formulations. PAS was successfully used for investigating the penetration of polymeric microparticles. In addition, microencapsulation decreased the in vitro transmembrane diffusion of ADAP.

Background: As part of the efforts to find natural alternatives for cancer treatment and to overcome the barriers of cellular resistance to chemotherapeutic agents, polymeric nanocapsules containing curcumin and/or methotrexate were prepared by an interfacial deposition of preformed polymer method. Methods: Physicochemical properties, drug release experiments and in vitro cytotoxicity of these nanocapsules were performed against the Calu-3 lung cancer cell line. Results: The colloidal suspensions of nanocapsules showed suitable size (287 to 325 nm), negative charge (−33 to −41 mV) and high encapsulation efficiency (82.4 to 99.4%). Spherical particles at nanoscale dimensions were observed by scanning electron microscopy. X-ray diffraction analysis indicated that nanocapsules exhibited a non-crystalline pattern with a remarkable decrease of crystalline peaks of the raw materials. Fourier-transform infrared spectra demonstrated no chemical bond between the drug(s) and polymers. Drug release experiments evidenced a controlled release pattern with no burst effect for nanocapsules containing curcumin and/or methotrexate. The nanoformulation containing curcumin and methotrexate (NCUR/MTX-2) statistically decreased the cell viability of Calu-3. The fluorescence and morphological analyses presented a predominance of early apoptosis and late apoptosis as the main death mechanisms for Calu-3. Conclusions: Curcumin and methotrexate co-loaded nanocapsules can be further used as a novel therapeutic strategy for treating non-small-cell lung cancer.

ABSTRACT Lavandula dentata, popularly known as lavender, is commonly used in traditional medicine for the treatment of digestive and inflammatory disorders. The objective of this study was to analyzed the chemical oil composition, antioxidant and antimicrobial activities of the essential oil and anatomical markers of the leaf and stem of L. dentata cultivated in South Brazil. Essential oil showed an antioxidant activity similar to rutin and gallic acid when analyzed by phosphomolybdenum method. However, by the free radical DPPH and ABTS methods, it showed a slight potential antioxidant. Essential oil presented 1,8-cineol (63%) as major component, antimicrobial activity against Gram-positive, Gram-negative bacteria strains and Candida albicans, by broth microdilution. The anatomical profile provided the following main microscopic markers: hypostomatic leaves; diacytic stomata, thin and striate cuticle; multicellular and branched non-glandular trichomes; capitate glandular trichomes; peltate glandular trichomes; dorsiventral mesophyll; flat-convex shape midrib, truncated on the abaxial side; one collateral vascular bundle in the midrib; square stem shape, angular collenchyma alternated with cortical parenchyma; sclerenchymatic fibers well-developed on the four edges.

ABSTRACT Ferulic acid (FA) is a phenolic compound with well-known antioxidant potential that can be used as a promising anti-inflammatory and anti-cancer molecule. Furthermore, it has been reported to have neuroprotective activity. One of the main problems, which limit its clinical use, is its low bioavailability when administered orally. This limitation can be circumvented by changes in their structure and/or for preparing lipid-based formulations. The aim of this study was to synthesize a derivative of FA, the hexadecyl ferulate (HF). This compound would be more susceptible to pass through blood-brain barrier (BBB) due to its lipophilic character. The HF was obtained by Steglich esterification and yielded 76.77 ± 1.35%. Its structural characterization was performed by spectroscopic methods of Fourier-transformed infrared spectroscopy (FTIR) and nuclear magnetic resonance (NMR). FTIR spectrum of HF presented two typical bands of ester group, a C=O ester stretching band at 1725 cm-1 and a C-O stretching band at 1159 cm-1. The 1H and 13C spectral data confirmed the chemical structure of HF. Regarding the 13C NMR spectrum, HF showed a chemical shift at δ 167.39 ppm which corresponded to the carbonyl carbon of the ester group. Concerning the in vitro antioxidant potential, HF had equivalent or improved scavenger activity than FA leading to IC50 values of 0.083 ± 0.009 nmol.mL-1 and 0.027 ± 0.002 nmol.mL-1 in DPPH radical scavenging and ABTS radical cation decolorization assays, respectively. Further studies are required in order to investigate the antioxidant effect of HF in biological media.

ABSTRACT Halcinonide is a high-potency topical glucocorticoid used for skin inflammation treatments that presents toxic systemic effects. A simple and quick analytical method to quantify the amount of halcinonide encapsulated into lipid nanoparticles, such as polymeric lipid-core nanoparticles and solid lipid nanoparticles, was developed and validated regarding the drug's encapsulation efficiency and in vitro permeation. The development and validation of the analytical method were carried out using the high performance liquid chromatography with the UV detection at 239 nm. The validation parameters were specificity, linearity, precision and accuracy, limits of detection and quantitation, and robustness. The method presented an isocratic flow rate of 1.0 mL.min-1, a mobile phase methanol:water (85:15 v/v), and a retention time of 4.21 min. The method was validated according to international and national regulations. The halcinonide encapsulation efficiency in nanoparticles was greater than 99% and the in vitro drug permeation study showed that less than 9% of the drug permeated through the membrane, indicating a nanoparticle reservoir effect, which can reduce the halcinonide's toxic systemic effects. These studies demonstrated the applicability of the developed and validated analytical method to quantify halcinonide in lipid nanoparticles.

The genus Calea belongs to the tribe Heliantheae and presents about 125 species. Calea serrata, popularly known as erva-de-cobra, chá-amargo and quebra-tudo, is an endemic species found in southern Brazil and is used in traditional medicine to treat ulcers and livers problems. The present work aimed to study the pharmacobotanical characters of leaves and stems of C. serrata for quality control purposes. The plant material was processed according to standard methods of light and scanning electron microscopy. Glandular capitate-stalked and capitate-sessile, uniseriate multicellular non-glandular trichome with tapered apical cell, conical non-glandular trichome, isobilateral mesophyll, secretory ducts near the endoderm and circular shape with six ribs in the stem were important characters, which contributed to the identification of the species.

This in vitro study evaluated the physical-chemical characteristics of whitening toothpastes and their effect on bovine enamel after application of a bleaching agent (16% carbamide peroxide). Physical-chemical analysis was made considering mass loss by desiccation, ash content and pH of the toothpastes. Thirty bovine dental enamel fragments were prepared for roughness measurements. The samples were subjected to bleaching treatments and simulated brushing: G1. Sorriso Dentes Brancos (Conventional toothpaste), G2. Close-UP Whitening (Whitening toothpaste), and G3. Sensodyne Branqueador (Whitening toothpaste). The average roughness (Ra) was evaluated prior to the bleaching treatment and after brushing. The results revealed differences in the physical-chemical characteristics of the toothpastes (p < 0.0001). The final Ra had higher values (p < 0.05) following the procedures. The mean of the Ra did not show significant differences, considering toothpaste groups and bleaching treatment. Interaction (toothpaste and bleaching treatment) showed significant difference (p < 0.0001). The whitening toothpastes showed differences in their physical-chemical properties. All toothpastes promoted changes to the enamel surface, probably by the use of a bleaching agent.

O presente trabalho teve o objetivo de analisar os efeitos do enxofre e da chuva ácida simulada sobre a estrutura foliar do feijoeiro (Phaseolus vulgaris L), nos aspectos morfoanatômicos, teores de clorofila a, b, total e feofitina. As plantas-controle sofreram simulações de chuva com pH 6,0 e as plantas-teste sofreram simulação de chuva ácida com pH 3,0. As concentrações de clorofila a, b e total diminuíram no estádio de floração (R6). Já, no estádio R7, onde surgem as primeiras vagens, os teores aumentaram, indicando possível resistência e/ou adaptação dos espécimes às simulações ácidas. O tratamento ácido afetou a concentração de clorofila que foi degradada por processos oxidativos sem a sua conversão em feofitina. Também se observou diminuição na frequência de tricomas tectores e glandulares, assim como de estômatos. As injúrias visualizadas foram classificadas como de caráter leve, provavelmente pela existência de anexos epidérmicos para proteção foliar e peciolar.The goal of this work was to evaluate the effects of sulfur and simulated acid rain on the leaf of Phaseolus vulgaris. Acid rain (pH 3.0) and an aqueous solution (Ph 6.0) were performed on test and control plants, respectively. A decrease in chlorophyll a, chlorophyll b and total chlorophyll concentrations was observed in theflowering stage (R6). However, increased rates were determined in the maturation stage (R7), which can suggest a resistance and/or adjustment of the plants to the acid simulation conditions. The acid treatment achieved chlorophyll degradation by oxidative processes without conversion to pheophytin. A reduction was also seen in the number of glandular and non-glandular trichomes and stomata on the test plants. Moreover, only small injuries were verified on the blade and peciolar areas of the tested individuals of P. vulgaris, probablydue to the presence of the reported epidermal structures.

A simple stability-indicating HPLC-DAD method was validated for the determination of ferulic acid (FA) in polymeric microparticles. Chromatographic conditions consisted of a RP C18 column (250 mm × 4.60 mm, 5 μm, 110 Å) using a mixture of methanol and water pH 3.0 (48 : 52 v/v) as mobile phase at a flow rate of 1.0 mL/min with UV detection at 320 nm. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of quantification, limit of detection, accuracy, precision, and robustness provided suitable results regarding all parameters investigated. The calibration curve was linear in the concentration range of 10.0–70.0 μg/mL with a correlation coefficient >0.999. Precision (intraday and interday) was demonstrated by a relative standard deviation lower than 2.0%. Accuracy was assessed by the recovery test of FA from polymeric microparticles (99.02% to 100.73%). Specificity showed no interference from the components of polymeric microparticles or from the degradation products derived from acidic, basic, and photolytic conditions. In conclusion, the method is suitable to be applied to assay FA as bulk drug and into polymeric microparticles and can be used for studying its stability and degradation kinetics.

Uma das principais causas de mortalidade em bovinos está relacionada à intoxicação por plantas de Senecio spp. (Asteraceae). Assim, alternativas para a redução dessas plantas na região sul do Brasil são necessárias a fim de diminuir as perdas na atividade pecuária. Estudos indicam o crisomelídeo Phaedon confinis Klug como potencial agente de controle biológico de plantas de Senecio brasiliensis Less. O objetivo desse estudo foi avaliar a preferência alimentar de larvas e adultos de P. confinis pelas espécies S. brasiliensis, Senecio madagascariensis Poiret, Senecio oxyphyllus DC e Senecio selloi DC. Os insetos foram alimentados com S. brasiliensis anteriormente ao experimento à temperatura de 22 ± 1ºC, umidade relativa de 60 ± 5% e fotofase de 12 horas. Os resultados obtidos indicam que as categorias de injúria ocasionada por P. confinis foram dependentes da espécie de Senecio oferecida ao inseto, com maior consumo de S. brasiliensis. O estágio de desenvolvimento dos insetos influencia a preferência alimentar, uma vez que larvas neonatas apresentaram maior seletividade ao hospedeiro do que os adultos. Além de S. brasiliensis, os adultos podem colaborar no controle de outras espécies de Senecio, principalmente de S. madagascariensis, uma vez que há oviposição nessas plantas. Feeding Preference of Larvae and Adults of Phaedon confinis Klug (Coleoptera: Chrysomelidae) for Senecio spp. (Asteraceae) Abstract. One of the main causes of death in cattle is related to poisoning by plants of Senecio spp. (Asteraceae). Thus, alternatives for reduction of these plants in the Southern region of Brazil are necessary to diminish losses in livestock. Studies have demonstrated the chrysomelid Phaedon confinis Klug as a potential biological agent of Senecio brasiliensis Less. Our study aimed to evaluate the feeding preference of larvae and adults of P. confinis by the species S. brasiliensis, Senecio madagascariensis Poiret, Senecio oxyphyllus DC and Senecio selloi DC. Previously, the insects were fed on S. brasiliensis to the experiment at 22 ± 1oC temperature, 60 ± 5% relative humidity and 12h photophase. Results obtained indicate that injury caused by P. confinis depended on the species of Senecio offered to the insect, with higher consumption of S. brasiliensis. The developmental stage of the insect influences the feeding preference, since neonate larvae demonstrated higher selectivity to the plant host than adults. In addition to S. brasiliensis, adults can be used to control other species of Senecio, especially S. madagascariensis, since there is oviposition on these plants.

Microparticles of poly(ε-caprolactone) (PCL) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing manidipine dihydrochloride (MAN) were successfully prepared by the simple emulsion/solvent evaporation method. All formulations showed loading efficiency rates greater than 80% and average particle size less than 8 μm. Formulations had spherical shape with smooth and porous surface for PCL and PHBV, respectively. According to Fourier-transform infrared spectroscopy, initial components were not chemically modified during microencapsulation. X-ray diffraction patterns and differential scanning calorimetry demonstrated that this process led to drug amorphization. In vitro dissolution studies showed that all microparticles prolonged MAN release, mainly which one obtained using PCL that contained 5% of drug loaded (PCL-M5). Animal studies demonstrated that formulation PCL-M5 was able to keep the variation of mean arterial pressure after phenylephrine administration up to 24 hours. These data confirmed the sustained antihypertensive effect of the investigated microparticles. Results provided an experimental basis for using formulation PCL-M5 as a feasible carrier for oral controlled release of MAN intended for treating high blood pressure.

Microparticles of poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) and poly(ε-caprolactone) (PCL) containing resveratrol were successfully prepared by simple emulsion/solvent evaporation. All formulations showed suitable encapsulation efficiency values higher than 80%. PHBV microparticles revealed spherical shape with rough surface and presence of pores. PCL microparticles were spherically shaped with smooth surface. Fourier-transformed infrared spectra demonstrated no chemical bond between resveratrol and polymers. X-ray powder diffraction patterns and differential scanning calorimetry analyses indicated that microencapsulation led to drug amorphization. These PHBV/PCL microparticles delayed the dissolution profile of resveratrol. Release profiles were better fitted to biexponential equation. The hypochlorous-acid-scavenging activity and 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation discoloration assay confirmed that the antioxidant activity of PHBV/PCL microparticles was kept, but was dependent on the microparticle morphology and dissolution profile. Resveratrol-loaded PHBV/PCL microparticles showed no cytotoxic effect on red blood cells.

O presente trabalho teve o objetivo de analisar os efeitos do enxofre e da chuva ácida simulada sobre a estrutura foliar do feijoeiro (Phaseolus vulgaris L), nos aspectos morfoanatômicos, teores de clorofila a, b, total e feofitina. As plantas-controle sofreram simulações de chuva com pH 6,0 e as plantas-teste sofreram simulação de chuva ácida com pH 3,0. As concentrações de clorofila a, b e total diminuíram no estádio de floração (R6). Já, no estádio R7, onde surgem as primeiras vagens, os teores aumentaram, indicando possível resistência e/ou adaptação dos espécimes às simulações ácidas. O tratamento ácido afetou a concentração de clorofila que foi degradada por processos oxidativos sem a sua conversão em feofitina. Também se observou diminuição na frequência de tricomas tectores e glandulares, assim como de estômatos. As injúrias visualizadas foram classificadas como de caráter leve, provavelmente pela existência de anexos epidérmicos para proteção foliar e peciolar.

Objetivo Avaliar a liberação e a capacidade de recarga de flúor de diferentes cimentos de ionômero de vidro, durante a simulação de desafio cariogênico. Material e método Foram confeccionados 12 corpos de prova para cada grupo experimental, com cimentos de ionômero de vidro convencionais – Maxxion R (FGM), Ketac Molar EasyMix (3M ESPE); cimento de ionômero de vidro modificado por resina – Vitrebond (3M ESPE), e resina composta, Filtek™ Z350XT (3M ESPE), como controle negativo. Os corpos de prova foram imersos alternadamente em sistema de ciclagem de pH, permanecendo 6 horas na solução de desmineralização e 18 horas na de remineralização, sendo mantidos em estufa a 37°C. Liberação de flúor foi verificada 1, 2, 7 e 14 dias antes e após a recarga com flúor, com eletrodo específico acoplado ao aparelho analisador de pH/fluoretos, calibrado a cada medição com soluções de fluoreto de sódio a 1 e 10 ppm, preparadas com TISAB II. Para leitura, foi adicionado 0,5 mL da amostra a igual volume de TISAB II. Recarga foi realizada com flúor neutro 2% por 4 minutos nas amostras, lavadas e imersas novamente nas soluções do sistema de ciclagem de pH. Os dados foram submetidos à análise de variância e ao teste de Tukey (α=0,05). Resultado A liberação inicial de fluoreto (μgF/cm2) foi de 45,36; 37,49, e 26,35 para Maxxion R, Vitrebond e Ketac Molar EasyMix, respectivamente. Diferenças estatísticas significativas entre os materiais foram verificadas antes e após a recarga (p=0,001). Após a aplicação tópica de flúor, os cimentos de ionômero de vidro apresentaram capacidade de recarga de flúor. Conclusão Cimentos de ionômero de vidro avaliados foram capazes de liberar flúor em soluções de ciclagem de pH e podem recarregar flúor através da aplicação tópica.

ABSTRACT Skin aging causes changes such as wrinkles and flaccidity leading to a large demand for aesthetic procedures, including dermal filling. A key agent in dermal filling is hyaluronic acid (HA), which is a naturally occurring glycosaminoglycan. However, it is a hydrophilic macromolecule that experiences great difficulty in crossing the skin barrier causing most commercial formulations containing it to be injectable, which in turn brings risks since they involve an invasive technique. In that sense, the aim of this study was to develop and characterize nanoparticles obtained from ionic interaction between HA and lysine (Lys) for use as a potential agent of dermal filling for topical application, increasing and improving its applicability and safety. To this end, nanoparticles were obtained by dripping of Lys over HA under magnetic stirring. A nanometric size was confirmed and a suitable surface charge was obtained by zeta potential. Nanoparticles were almost spherical in shape with a smooth surface. Interaction between raw materials for preparing nanoparticles was studied by FTIR and NMR spectroscopy and an ionic interaction was confirmed. These physicochemical features suggest that obtained nanoparticles can be further used as a topical dermal filling.

Abstract Objective To evaluate the surface morphology and in vitro leachability of temporary soft linings modified by the incorporation of antifungals in minimum inhibitory concentrations (MIC) for Candida albicans biofilm. Methodology Specimens of soft lining materials Softone and Trusoft were made without (control) or with the addition of nystatin (Ny), miconazole (Mc), ketoconazole (Ke), chlorhexidine diacetate (Chx), or itraconazole (It) at their MIC for C. albicans biofilm. The surface analyses were performed using Confocal laser scanning microscopy after 24 h, 7 days, or 14 days of immersion in distilled water at 37ºC. In vitro leachability of Chx or Ny from the modified materials was also measured using Ultraviolet visible spectroscopy for up to 14 days of immersion in distilled water at 37ºC. Data (μg/mL) were submitted to ANOVA 1-factor/Bonferroni (α=0.05). Results Softone had a more irregular surface than Trusoft. Morphological changes were noted in both materials with increasing immersion time, particularly, in those containing drugs. Groups containing Chx and It presented extremely porous and irregular surfaces. Both materials had biexponential release kinetics. Softone leached a higher concentration of the antifungals than Trusoft (p=0.004), and chlorhexidine was released at a higher concentration than nystatin (p

Abstract Periodontal therapy usually requires local anesthesia. If effective, a non-invasive, liposomal anesthetic gel could increase the levels of acceptance of patients in relation to periodontal therapy. Objective: This study investigated the efficacy of liposomal anesthetic gel for pain control during periodontal therapy. Methodology: Forty volunteers with moderate to severe chronic periodontitis were recruited, of which at least three sextants required periodontal therapy. At least one of the selected teeth had one site with a probing depth of ≥4 mm. The volunteers received the following three gels: a placebo, lidocaine/prilocaine (Oraqix®), or a liposomal lidocaine/prilocaine, which were applied to different sextants. Pain frequency was registered during treatment and the volunteers received a digital counter to register any painful or uncomfortable experiences. At the end of each session, the volunteers indicated their pain intensity using rating scales (NRS-101 and VRS-4). The volunteers had their hemodynamic parameters measured by a non-invasive digital monitor. Results: Pain frequency/intensity did not show statistical difference between intervention groups. The tested gels did not interfere with the hemodynamic indices. Dental anxiety, suppuration and probing depth could influence pain during periodontal therapy. Conclusion: Our results suggest limited indications for the use of non-invasive anesthesia when used for scaling and root planing. Intra-pocket anesthetic gel could be a good option for anxious patients, or those who have a fear of needles.