Ascorbic acid and ascorbyl palmitate-loaded liposomes: Development, characterization, stability evaluation, in vitro security profile, antimicrobial and antioxidant activities.

The objective of this work was to prepare and characterize liposomes containing co-encapsulated ascorbic acid (AA) and ascorbyl palmitate (AP), as well as to evaluate their stability, cytotoxicity, antioxidant, and antimicrobial activity. Through the pre-formulation studies, it was possible to improve the formulation, as leaving it more stable and with a greater antioxidant activity, resulting in a formulation designated LIP-AAP, with 161 nm vesicle size, 0.215 polydispersity index, -31.7 mV zeta potential, and pH of 3.34. Encapsulation efficiencies were 37% for AA and 79% for AP, and the content was 1 mg/mL for each compound. The optimized liposomes demonstrated stability under refrigeration for 60 days, significant antioxidant activity (31.4 µMol of TE/mL), and non-toxicity, but no antimicrobial effects against bacteria and fungi were observed. These findings confirm that the co-encapsulated liposomes are potent, stable antioxidants that maintain their physical and chemical properties under optimal storage conditions.

Phytochemical analysis of carotenoid profile in Mentha piperita and Artemisia vulgaris: cytotoxicity in tumoral cells and evaluation of plasmid DNA cleavage.

Several medicinal plants have been administered to cancer patients attributed to their anticarcinogenic and chemoprotective properties, in addition to lower toxicity compared to traditional therapies. The aim was to investigate the antioxidant properties and carotenoid composition of aqueous extracts of Mentha piperita or Artemisia vulgaris which were previously found to exert beneficial effects on human health through diet. aqueous extracts exhibited potent antioxidant activity. A diversity of carotenoids was identified in these extracts using HPLC-PDA-MS/MS. Both extracts contained predominantly all-trans-lutein as the main component within this class. In order to investigate antioxidant properties, the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) techniques were used. The (3-4,5 dimethylthiazol-2, 5 diphenyl tetrazolium bromide) (MTT) and Crystal Violet assays assessed cellular cytotoxicity. Assessments of presence of reactive species were carried out following exposure of oral squamous cell carcinoma cell line (SCC-4) to various aqueous extracts of M piperita or A vulgaris utilizing dichlorofluorescein diacetate (DCFH-DA) and nitric oxide (NO) assays. Exposure to these extracts induced severe cytotoxic effects, which led to investigation of the biochemical and molecular mechanisms underlying this observed effect. Data demonstrated that both solutions induced oxidative stress and DNA damage, especially at higher concentrations using agarose gel subjected to electrophoresis. It is known that exposure to excess amounts of antioxidants results in a prooxidant effect which is beneficial in cancer therapy. Further, the extracts were found to reduce viability of SCC-4 in culture, indicating that this antitumoral activity may be of therapeutic importance and requires further study.

Phytochemical characterization and toxicological activity attributed to the acetonic extract of South American Vassobia breviflora.

The particular plant species found in southern Brazil, Vassobia breviflora (Solanaceae) has only a few apparent studies examining its biological effect. Thus, the aim of the present study was to determine the activity of the acetone extract fraction derived from V. breviflora. Four compounds were identified by ESI-qTOF-MS: eucalrobusone R, aplanoic acid B, pheophorbide A, and pheophytin A. In addition, 5 compounds were identified by HPLC-PDA-MS/MS: all-trans-lutein, 15-cis-lutein, all-trans-ß-carotene, 5,8-epoxy-ß-carotene, and cis-ß-carotene. Cell lines A549 (lung cancer), A375 (melanoma cancer) and HeLa (cervical cancer) were incubated with different concentrations of each studied extract using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), lactate dehydrogenase (LDH), and 2'-7'dichlorofluorescin diacetate (DCFH-DA) assays. The acetonic extract exhibited cytotoxic activity at a concentration of 0.03 mg/ml in the HeLa strain and 0.1 mg/ml in the others. In addition to increased production of reactive oxygen species (ROS). Antibacterial activity was assessed utilizing minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) in 9 ATCCs strains and 7 clinical isolates, as well as determination of biofilm production. Data demonstrated that MIC and MBC were approximately 256 mg/ml in most of the strains tested and antibiofilm effect at S. aureus, S. epidermidis, A. baumannii, and E. faecalis, concentrations below the MIC. Genotoxic activity on plasmid DNA did not produce significant elevated levels in breaks in the isolated genetic material.

Hydrogel Containing Silibinin-Loaded Pomegranate Oil-Based Nanocapsules for Cutaneous Application: In Vitro Safety Investigation and Human Skin Biometry and Permeation Studies.

In previous studies, we developed a hydrogel formulation containing silibinin-loaded pomegranate oil nanocapsules (HG-NCSB) that had improved in vivo anti-inflammatory action in comparison to non-encapsulated silibinin. To determine skin safety and whether the nanoencapsulation influences silibinin skin permeation, NCSB skin cytotoxicity, HG-NCSB permeation in human skin, and a biometric study with healthy volunteers were conducted. The formulation of nanocapsules was prepared by the preformed polymer method while the HG-NCSB was obtained by thickening the suspension of nanocarriers with gellan gum. The cytotoxicity and phototoxicity of nanocapsules were assessed in Keratinocytes (HaCaT) and fibroblast (HFF-1) using the MTT assay. The hydrogels were characterized regarding the rheological, occlusive, and bioadhesive properties, and silibinin permeation profile in human skin. The clinical safety of HG-NCSB was determined by cutaneous biometry in healthy human volunteers. NCSB yielded better cytotoxicity results than the blank nanocapsules (NCPO). NCSB did not cause photocytotoxicity, while NCPO and the non-encapsulated substances (SB and pomegranate oil) were phototoxic. The semisolids presented non-Newtonian pseudoplastic flow, adequate bioadhesiveness, and low occlusive potential. The skin permeation demonstrated that HG-NCSB retained a higher SB amount in the outermost layers than HG-SB. In addition, HG-SB reached the receptor medium and had a superior concentration of SB in the dermis layer. In the biometry assay, there was no significant cutaneous alteration after the administration of any of the HGs. Nanoencapsulation promoted greater SB retention in the skin, averted percutaneous absorption, and made the topical use of SB and pomegranate oil safer.

Photocatalytic degradation of Rhodamine B dye by nanostructured powder systems containing nanoencapsulated curcumin or ascorbic acid and ascorbyl palmitate liposomal.

Due to inadequate treatment and incorrect management, wastewater with dyes has a great toxic potential as an environmental liability, representing a major concern. In this context, this work aims to investigate the potential application of nanostructured powdery systems (nanocapsules and liposomes) in the photodegradation of Rhodamine B (RhB) dye, under UV and visible irradiation. Curcumin nanocapsules and liposomes containing ascorbic acid and ascorbyl palmitate were prepared, characterized, and dried using the spray drying technique. The drying processes of the nanocapsule and the liposome showed yields of 88% and 62%, respectively, and, after aqueous resuspension of the dry powders, it was possible to recover the nanocapsule size (140 nm) and liposome size (160 nm). The dry powders were characterized by Fourier transform infrared spectroscopy (FTIR), N2 physisorption at 77 K, X-ray diffraction (XRD), and diffuse reflectance spectroscopy (DRS-UV). Under UV irradiation, 64.8% and 58.48% of RhB were removed with nanocapsules and liposomes, respectively. While under visible radiation, nanocapsules and liposomes were able to degrade 59.54% and 48.79% of RhB, respectively. Under the same conditions, commercial TiO2 showed degradation of 50.02% (UV) and 42.14% (visible). After 5 cycles of reuse, there was a decrease of about 5% for dry powders under UV irradiation and 7.5% under visible irradiation. Therefore, the nanostructured systems developed have potential application in heterogeneous photocatalysis for the degradation of organic pollutants, such as RhB, as they demonstrated superior photocatalytic performance to commercial catalysts (nanoencapsulated curcumin > ascorbic acid and ascorbyl palmitate liposomal > TiO2).

Trypanosoma cruzi: Does the intake of nanoencapsulated benznidazole control acute infections?

Chagas Disease (CD) affects around eight million people worldwide. It is considered a neglected disease that presents few treatment options with efficacy only in the acute phase. Nanoparticles have many positive qualities for treating parasite infections and may be effectively and widely employed in clinical medicine. This research aimed to evaluate the nanoencapsulated benznidazole treatment in animals experimentally infected with Trypanosoma cruzi. To analyze the treatment efficacy, we evaluated survival during thirty days, parasitemia, genotoxicity, and heart and liver histopathology. Thirty-five female Swiss mice were organized into seven groups characterizing a dose curve: A - Negative control (uninfected animals), B - Positive control (infected animals), C - Benznidazole (BNZ) 100 mg/kg (infected animals), D - 5 mg/kg Benznidazole nanocapsules (NBNZ) (infected animals), E - 10 mg/kg Benznidazole nanocapsules (infected animals), F - 15 mg/kg Benznidazole nanocapsules (infected animals), G - 20 mg/kg Benznidazole nanocapsules (infected animals). The animals were infected with the Y strain of T. cruzi intraperitoneally. The treatment was administered for eight days by oral gavage. It was possible to observe that the treatment with the highest NBNZ dose presented efficacy similar to the standard benznidazole drug. The 20 mg/kg NBNZ dose was able to reduce parasitemia, increase survival, and drastically reduce heart and liver tissue damage compared to the 100 mg/kg BNZ dose. Moreover, it showed a lower DNA damage index than the BNZ treatment. In conclusion, the nanoencapsulation of BNZ promotes an improvement in parasite proliferation control with a five times smaller dose relative to the standard dose of free BNZ, thus demonstrating to be a potential innovative therapy for CD.

Detection of new phytochemical compounds from Vassobia breviflora (Sendtn.) Hunz: antioxidant, cytotoxic, and antibacterial activity of the hexane extract.

Vassobia breviflora (Sendtn.) Hunz is a plant of the Solanaceae family from South America and there are no apparent studies reported on the biological activity of the hexane extract. The aim of this investigation was to conduct phytochemical analyses using ESI-TOF-MS, while antioxidant activities were evaluated by the following methods 1,1-diphenyl-2-picrylhydrazyl (DPPH) 2,2"-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) radical capture (ABTS), ferric reducing antioxidant power (FRAP), total antioxidant capacity (TAC), and total oxidant status (TOS). Antimicrobial activities were performed by determining the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and antibiofilm formed. Cytotoxicity was measured by MTT and dsDNA PicoGreen tests, beyond the production of reactive oxygen species (ROS) determined by Dichlorodihydrofluorescein diacetate (DCFH-DA). The hexane extract showed the presence of 5 (choline, pantothenic acid, calystegine B, lanciphodylactone I, and 15"-cis-zeaxanthin) compounds detected. V. breviflora extract demonstrated reliable results utilizing different antioxidant methods. In antibacterial activity, V. breviflora extract exhibited inhibitory, bactericidal, and antibiofilm action in biofilm-forming bacteria. The hexane extract exhibited cytotoxicity against melanoma, lung cancer, glioblastoma, leukemia, uterine colon, and hepatocarcinoma tumor cells. In addition, all tested strains resulted in increased production of ROS. This plant extract may be considered in future as an alternative for development of new therapeutic options aimed at the treatment of diverse pathologies.

Impact of free curcumin and curcumin nanocapsules on viability and oxidative status of neural cell lines.

Curcumin is an active polyphenol substance found in the highest concentrations in the roots of Curcuma longa. Its health benefits have led to recent increases in the consumption of curcumin. It has anti-inflammatory and antioxidant activities and is a potent neuroprotective against diseases of the brain. Nevertheless, its low bioavailability and its relative difficulty crossing the blood-brain barrier limit curcumin's use for these purposes. Curcumin-loaded nanoparticles may be an effective treatment for several diseases although there is a paucity of studies reporting its safety in the central nervous system (CNS). Therefore, this study aimed to identify non-neurotoxic concentrations of free curcumin and two nanoformulations of curcumin. Cell lines BV-2 and SH-SY5Y, both originating from the CNS, were evaluated after 24, 48, and 72 h of treatment with free curcumin and nanocapsules We measured viability, proliferation, and dsDNA levels. We measured levels of reactive oxygen species and nitric oxide as proxies for oxidative stress in culture supernatants. We found that free curcumin was toxic at 10 and 20 µM, principally at 72 h. Nanoformulations were more neurotoxic than the free form. Safe concentrations of free curcumin are between 1-5 µM, and these concentrations were lower for nanoformulations. We determined the ideal concentrations of free curcumin and nanocapsules serving as a basis for studies of injuries that affect the CNS.

Insights of ethyl acetate fraction from Vassobia breviflora in multidrug-resistant bacteria and cancer cells: from biological to therapeutic.

Cancer and infectious diseases are among the leading causes of death in the world. Despite the diverse array of treatments available, challenges posed by resistance, side effects, high costs, and inaccessibility persist. In the Solanaceae plant family, few studies with Vassobia breviflora species relating to biological activity are known, but promising results have emerged. The phytochemicals present in the ethyl acetate fraction were obtained using ESI-MS-QTOF, and the antioxidants assays 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) radical capture (ABTS), plasma ferric reduction capacity (FRAP), and total antioxidant capacity (TAC). Cytotoxic activity was evaluated by MTT, Neutral Red, and lactate dehydrogenase (LDH) released. The production of reactive oxygen species, nitric oxide, and purinergic enzymes was also investigated. Antibacterial activity was measured through minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and antibiofilm activity, in addition to genotoxicity in plasmid DNA. Five major masses were identified D-glucopyranose II, allyl disulfide, γ-lactones, pharbilignoside, and one mass was not identified. V. breviflora exhibited relevant antioxidant and cytotoxic activity against the HeLa cell line and enhanced expression effect in modulation of purinergic signaling. Antibacterial activities in the assays in 7 ATCC strains and 8 multidrug-resistant clinical isolates were found. V. breviflora blocked biofilm formation in producing bacteria at the highest concentrations tested. However, there was no plasmid DNA cleavage at the concentrations tested. Data demonstrated that V. breviflora exhibited an antioxidant effect through several methods and proved to be a promising therapeutic alternative for use against tumor cells via purinergic signaling and multidrug-resistant microorganisms, presenting an anti-biofilm effect.

Eucalyptus oil nanoemulsions against eggs and larvae of Haemonchus contortus.

Haemonchus contortus is a highly pathogenic and prevalent helminth that causes many deaths in sheep herds. Anthelmintics are usually employed to overcome this issue; however, they do not guarantee immediate and lasting efficacy because of the occurrence of drug-resistant parasites. Among substances that are used in scientific studies for parasitic control, essential oils are known to have different pharmacological properties. However, they demonstrate instability owing to several factors, and therefore, nanoemulsification is considered an alternative to control the instability and degradability of these compounds. The objective of this study was to evaluate the cytotoxicity of nanoemulsions containing essential oil of Eucalyptus globulus against the blood of healthy sheep and to verify their activity against the parasite H. contortus in sheep. The results presented adequate nanotechnological characteristics (diameter 72 nm, PDI 0.2, zeta -11 mV, and acidic pH) and adequate morphology. Further, the corona effect and cytotoxic profiles of the free oil and nanoemulsion against blood cells from healthy sheep were evaluated. The tests results did not present a toxicity profile. For evaluating efficacy, we observed an important anthelmintic action of the nanoemulsion containing oil in comparison to the free oil; the results demonstrate a potential role of the nanoemulsion in the inhibition of egg hatchability and the development of larvae L1 to L3 (infective stage). Based on these results, we developed an important and potential anthelmintic alternative for the control of the parasite H. contortus.

Antioxidant and Nematocidal Effects of Several Oyster Mushroom Species of Genus Pleurotus (Agaricomycetes).

Cyathostomins are common intestinal nematodes that parasitize horses and can affect animal health and welfare. Alternative treatments are essential for sustainable parasite control, reducing the indiscriminate use of anthelmintics and their impacts on the environment, animals, and humans. Pleurotus spp. are edible medicinal mushrooms that possess several therapeutic properties, including antiparasitic and nematocidal activities. This study aimed to evaluate the antioxidant and nematocidal activity of aqueous extracts of three oyster species (P. florida, P. ostreatus, and P. djamor) on cyathostomine eggs in vitro. P. florida showed the highest activity against test organisms, inhibiting the hatching of eggs in up to 92.19% at the highest concentration (10%) of aqueous extract, with a mean lethal concentration (LC50) of 2.13%. In the aqueous extracts of P. ostreatus and P. djamor, nematocidal activity was reduced, inhibiting egg hatching by 55.46% (LC50, 7.44%) and 23.67%, respectively, at a concentration of 10%. P. florida showed higher antioxidant activity than that of the other species tested. Thus, P. florida may be considered a potential alternative for biological control in in vivo experiments with cyathostomins.

Development, characterisation, stability study and antileukemic evaluation of nanoemulsions containing Astrocaryum aculeatum extract.

The objective of this work was to produce and characterise nanoemulsions containing tucumã extract and to evaluate the performance of the nanostructure and the free compound regarding antitumor activity, cytotoxicity, and oxidative metabolism in NB4/APL cells. The nanoemulsions showed adequate physicochemical characteristics (average size approx. 200 nm, polydispersity index less than 0.3, negative zeta potential and acid pH) maintained stable up to 90 days of storage in refrigeration condition. The nanoformulations did not present protein corona formation. Blank nanoemulsion treatments showed moderate toxicity. Furthermore, the nanoemulsion loaded with extract showed better antileukemic results than the free extract. However, nanoemulsions can be promising carriers of natural compounds, emphasising their biological properties and constituting alternatives in treating diseases.

Açaí (Euterpe oleracea Mart.) presents anti-neuroinflammatory capacity in LPS-activated microglia cells.

INTRODUCTION: Neuropsychiatric diseases are responsible for one of the highest burden of morbidity and mortality worldwide. These illnesses include schizophrenia, bipolar disorder, and major depression. Individuals affected by these diseases may present mitochondrial dysfunction and oxidative stress. Additionally, patients also have increased peripheral and neural chronic inflammation. The Brazilian fruit, açaí, has been demonstrated to be a neuroprotective agent through its recovery of mitochondrial complex I activity. This extract has previously shown anti-inflammatory effects in inflammatory cells. However, there is a lack of understanding of potential anti-neuroinflammatory mechanisms, such as cell cycle involvement. OBJECTIVE: The objective of this study is to evaluate the anti-neuroinflammatory potential of an açaí extract in lipopolysaccharide-activated BV-2 microglia cells. METHODS: Açaí extract was produced and characterized through high performance liquid chromatography. Following açaí extraction and characterization, BV-2 microglia cells were activated with LPS and a dose-response curve was generated to select the most effective açaí dose to reduce cellular proliferation. This dose was then used to assess reactive oxygen species (ROS) production, double-strand DNA release, cell cycle modulation, and cytokine and caspase protein expression. RESULTS: Characterization of the açaí extract revealed 10 bioactive molecules. The extract reduced cellular proliferation, ROS production, and reduced pro-inflammatory cytokines and caspase 1 protein expression under 1 µg/mL in LPS-activated BV-2 microglia cells but had no effect on double strand DNA release. Additionally, açaí treatment caused cell cycle arrest, specifically within synthesis and G2/Mitosis phases. CONCLUSION: These results suggest that the freeze-dried hydroalcoholic açaí extract presents high anti-neuroinflammatory potential.

Evaluation of the in vivo safety of tucumã oil nanocapsules in an experimental model of silver catfish Rhamdia quelen.

The aim of this study was to evaluate the toxicity of tucumã oil nanocapsules from the Amazon region in silver catfish, Rhamdia quelen. Fish were exposed to water treated with different concentrations of tucumã nanocapsules, white, solubilized oil and surfactant vehicles. After three days of exposure, fish were euthanized and liver, gills and brain removed for analysis of the dichlorofluorescein, nitric oxide and PicoGreen® assays. Plasma was collected for assay of hepatic transaminases. The nanocapsules had a diameter of 221 ± 1.27 nm, confirmed by atomic force microscopy. The oil nanocapsules were not toxic to this species of fish, but white nanocapsules and surfactant increased the levels of reactive oxygen species. Thus, nanocapsules are promising for the transport of tucumã oil. In view of the anti-inflammatory properties of this oil, it is possible to envisage its application in skin diseases for example, since they present essentially inflammatory conditions.HighlightsThe most abundant carotenoid in tucumã oil was all-trans-beta-carotene.Nanocapsules are good carriers for tucumã oil.Tucumã oil nanocapsules does nothas toxicity effect in catfish.

Protective Effect of Indomethacin-loaded Polymeric Nanoparticles Against Oxidative Stress-Induced Cytotoxicity in Human Breast Adenocarcinoma Cell Model / Efeito Protetor de Nanopartículas Poliméricas com Indometacina contra Citotoxicidade Induzida por Estresse Oxidativo em Modelo Celular de Adenocarcinoma de Mama Humano / Efecto Protector de Nanopartículas Poliméricas con Indometacina contra la Citotoxicidad Inducida por Estrés Oxidativo en Modelo de Células de Adenocarcinoma de Mama Humano

Introduction: Anti-inflammatory drugs are being utilized to treat cancer because of its inflammatory microenvironment. Objective: The objective of this study is to investigate the antioxidant potential of indomethacin and its genotoxicity, since free or loaded in polymeric nanocapsules using MCF-7 (human breast cancer) cells as an in vitro model. Method: Development of indomethacin-loaded polyepsilon-caprolactone (PCL) nanocapsules by interfacial deposition method. It is characterized by pH determination by potentiometer, mean diameter and polydispersity index by dynamic light scattering; zeta potential by electrophoretic mobility; encapsulation efficacy by high performance liquid chromatography method; corona effect formation; 2',7'-dichlorofluorescin diacetate (DCFH-DA) method by spectrofluorimetric assay; nitric oxide (NO) determination by spectrophotometric and genotoxicity assay by plasmid DNA cleavage method. Results: The results showed a mild acidic pH (4.78 ± 0.10), sizes around 200 nm and PDI<0.2 with a zeta potential around -20 mV and encapsulation efficiency of 99% (1 mg mL-1), showing a dose-dependent corona formation profile in 24h incubation. Conclusion: DCFH-DA assay showed no production of reactive oxygen species (ROS) while NO determination showed that Ind-OH-NC from 26.7 to 100 µM increased reactive nitrogen species (RNS), demonstrating antioxidant potential against MCF-7 cells. No sample at the concentrations evaluated induced DNA cleavage, being considered a safe treatment

Introdução: Anti-inflamatórios estão sendo empregados para tratamento de câncer por causa do seu ambiente inflamado. Objetivo: Investigar o potencial antioxidante da indometacina e sua genotoxicidade, livre ou carreada em nanocápsulas poliméricas, usando como modelo in vitrocélulas MCF-7 (câncer de mama humano). Método: Desenvolvimento de nanocápsulas de poliepsilon-caprolactona (PCL) por método de deposição interfacial, caracterizada por determinação de pH por potenciômetro; diâmetro médio e índice de polidispersão por espalhamento dinâmico de luz; potencial zeta por mobilidade eletroforética; eficiência de encapsulação por cromatografia líquida de alta eficiência; formação de efeito corona; método de 2',7'-diclorofluoresceína diacetato (DCFH-DA) por ensaio espectrofluorimétrico; determinação de óxido nítrico (NO) por espectrometria e ensaio de genotoxicidade por método de clivagem do DNA plasmidial. Resultados: Os resultados mostraram leve pH ácido (4,78 ± 0,10), tamanhos em torno de 200 nm e PDI<0,2 com potencial zeta em torno de -20 mV e eficiência de encapsulação de 99% (1 mg mL-1), apresentando perfil de formação de corona dose-dependente em 24 horas de incubação. Conclusão: O ensaio DCFH-DA mostrou que não há produção de espécies reativas de oxigênio (ROS), enquanto a determinação de NO mostrou que Ind-OH-NC de 26,7 a 100 µM aumentou as espécies reativas de nitrogênio (RNS), demonstrando potencial antioxidante contra MCF-7. Nenhuma amostra nas concentrações avaliadas induziu clivagem do DNA, sendo considerado um tratamento seguro

Introducción: Se están utilizando antiinflamatorios para tratamiento de cáncer debido a su entorno inflamado. Objetivo: Investigar el potencial antioxidante de la indometacina y su genotoxicidad, libre o acarreada en nanocápsulas poliméricas utilizando como modelo in vitro células MCF-7 (cáncer de mama humano). Método: Desarrollo de nanocápsulas de poli epsilon-caprolactona (PCL) por método de deposición interfacial, caracterizada por determinación de pH por potenciómetro; diámetro medio e índice de polidispersión por esparcimiento dinámico de luz; potencial zeta por movilidad electroforética; eficiencia de encapsulación por cromatografía líquida de alta eficiencia; formación de efecto corona; método de 2',7'-diclorofluoresceína diacetato (DCFH-DA) por ensayo espectrofluorímetro; determinación de óxido nítrico (NO) por espectrometría y ensayo de genotoxicidad por método de clivaje del ADN plasmídico. Resultados: Los resultados mostraron ligero pH ácido (4,78 ± 0,10), tamaños alrededor de 200 nm y PDI<0,2 con potencial zeta alrededor de -20 mV y eficiencia de encapsulación de 99% (1 mg mL-1), presentando perfil de formación de corona dosis-dependiente en 24h de incubación. Conclusión: El ensayo DCFDA mostró que no hay producción de especies reactivas de oxígeno (ROS) mientras que la determinación de NO mostró que Ind-OH-NC de 26,7 a 100 µM aumentó las especies reactivas de nitrógeno (RNS), demostrando potencial antioxidante contra MCF-7. Ninguna muestra en las concentraciones evaluadas indujo clivaje del ADN, siendo considerado un tratamiento seguro

Protective Effect of Indomethacin-loaded Polymeric Nanoparticles Against Oxidative Stress-Induced Cytotoxicity in Human Breast Adenocarcinoma Cell Model / Efeito Protetor de Nanopartículas Poliméricas com Indometacina contra Citotoxicidade Induzida por Estresse Oxidativo em Modelo Celular de Adenocarcinoma de Mama Humano / Efecto Protector de Nanopartículas Poliméricas con Indometacina contra la Citotoxicidad Inducida por Estrés Oxidativo en Modelo de Células de Adenocarcinoma de Mama Humano

Anti-inflammatory drugs are being utilized to treat cancer because of its inflammatory microenvironment. Objective: The objective of this study is to investigate the antioxidant potential of indomethacin and its genotoxicity, since free or loaded in polymeric nanocapsules using MCF-7 (human breast cancer) cells as an in vitro model. Method: Development of indomethacin-loaded polyepsilon-caprolactone (PCL) nanocapsules by interfacial deposition method. It is characterized by pH determination by potentiometer, mean diameter and polydispersity index by dynamic light scattering; zeta potential by electrophoretic mobility; encapsulation efficacy by high performance liquid chromatography method; corona effect formation; 2',7'-dichlorofluorescin diacetate (DCFH-DA) method by spectrofluorimetric assay; nitric oxide (NO) determination by spectrophotometric and genotoxicity assay by plasmid DNA cleavage method. Results: The results showed a mild acidic pH (4.78 ± 0.10), sizes around 200 nm and PDI PDI<0.2 with a zeta potential around -20 mV and encapsulation efficiency of 99% (1 mg mL-1), showing a dose-dependent corona formation profile in 24h incubation. Conclusion: DCFH-DA assay showed no production of reactive oxygen species (ROS) while NO determination showed that Ind-OH-NC from 26.7 to 100 µM increased reactive nitrogen species (RNS), demonstrating antioxidant potential against MCF-7 cells. No sample at the concentrations evaluated induced DNA cleavage, being considered a safe treatment

Introdução: Anti-inflamatórios estão sendo empregados para tratamento de câncer por causa do seu ambiente inflamado. Objetivo: Investigar o potencial antioxidante da indometacina e sua genotoxicidade, livre ou carreada em nanocápsulas poliméricas, usando como modelo in vitro células MCF-7 (câncer de mama humano). Método: Desenvolvimento de nanocápsulas de poliepsilon-caprolactona (PCL) por método de deposição interfacial, caracterizada por determinação de pH por potenciômetro; diâmetro médio e índice de polidispersão por espalhamento dinâmico de luz; potencial zeta por mobilidade eletroforética; eficiência de encapsulação por cromatografia líquida de alta eficiência; formação de efeito corona; método de 2',7'-diclorofluoresceína diacetato (DCFH-DA) por ensaio espectrofluorimétrico; determinação de óxido nítrico (NO) por espectrometria e ensaio de genotoxicidade por método de clivagem do DNA plasmidial. Resultados: Os resultados mostraram leve pH ácido (4,78 ± 0,10), tamanhos em torno de 200 nm e PDI<0,2 com potencial zeta em torno de -20 mV e eficiência de encapsulação de 99% (1 mg mL-1), apresentando perfil de formação de corona dose-dependente em 24 horas de incubação. Conclusão: O ensaio DCFH-DA mostrou que não há produção de espécies reativas de oxigênio (ROS), enquanto a determinação de NO mostrou que Ind-OH-NC de 26,7 a 100 µM aumentou as espécies reativas de nitrogênio (RNS), demonstrando potencial antioxidante contra MCF-7. Nenhuma amostra nas concentrações avaliadas induziu clivagem do DNA, sendo considerado um tratamento seguro

Introducción: Se están utilizando antiinflamatorios para tratamiento de cáncer debido a su entorno inflamado. Objetivo: Investigar el potencial antioxidante de la indometacina y su genotoxicidad, libre o acarreada en nanocápsulas poliméricas utilizando como modelo in vitro células MCF7 (cáncer de mama humano). Método: Desarrollo de nanocápsulas de poli epsilon-caprolactona (PCL) por método de deposición interfacial, caracterizada por determinación de pH por potenciómetro; diámetro medio e índice de polidispersión por esparcimiento dinámico de luz; potencial zeta por movilidad electroforética; eficiencia de encapsulación por cromatografía líquida de alta eficiencia; formación de efecto corona; método de 2',7'-diclorofluoresceína diacetato (DCFH-DA) por ensayo espectrofluorímetro; determinación de óxido nítrico (NO) por espectrometría y ensayo de genotoxicidad por método de clivaje del ADN plasmídico. Resultados: Los resultados mostraron ligero pH ácido (4,78 ± 0,10), tamaños alrededor de 200 nm y PDI<0,2 con potencial zeta alrededor de -20 mV y eficiencia de encapsulación de 99% (1 mg mL-1), presentando perfil de formación de corona dosis-dependiente en 24h de incubación. Conclusión: El ensayo DCFDA mostró que no hay producción de especies reactivas de oxígeno (ROS) mientras que la determinación de NO mostró que Ind-OH-NC de 26,7 a 100 µM aumentó las especies reactivas de nitrógeno (RNS), demostrando potencial antioxidante contra MCF-7. Ninguna muestra en las concentraciones evaluadas indujo clivaje del ADN, siendo considerado un tratamiento seguro

Vitamin C as a shelf-life extender in liposomes

Abstract The objective of this study was to evaluate the influence of vitamin C (VC) on the stability of stored liposomes under different climatic conditions. Liposomal formulations containing 1 mg/mL of VC (LIP-VC) and blank formulations (LIP-B) were prepared by the reverse-phase evaporation method. After preparation, they were characterized according to their refractive index, average vesicle diameter, polydispersity index (PDI), zeta potential, pH, content, encapsulation efficiency (EE%), morphology, stability and antioxidant activity. For stability, LIP-VC and LIP-B were stored in different climatic conditions (4 °C, 25 °C and 40 °C) for 30 days. The LIP-VC presented 1.3365 refractive index, 161 nm of mean diameter, 0.231 PDI, -7.3 mV zeta potential, 3.2 pH, 19.4% EE%, spherical morphology, 1 mg/mL of VC content, and antioxidant activity of 12 and 11.4 μmol of TE/mL for the radical DPPH and ABTS+, respectively. During stability, the LIP-B stored in 40 °C showed an instability in the parameters: PDI, vesicle size and zeta potential after 15 days, while the LIP-VC remained stable in its size and PDI for 30 days. After that, it is shown that VC can be used as an antioxidant and stabilizer in liposomes to increase the stability and shelf-life of vesicles.

Dietary supplementation with curcumin-loaded nanocapsules in lambs: Nanotechnology as a new tool for nutrition.

Curcumin-containing nanocapsule powder formulations have not been used in ruminant feed to date, despite the fact that curcumin is known to be a functional food additive. The objective of this study was to determine whether ethyl polymethacrylate (Eudragit L-100) nanocapsules loaded with curcumin (N-CU) would improve health and growth of lambs. Thirty-two male Lacaune lambs (body weight [BW] = 16 ± 0.99 kg; 45 d of age) were randomly assigned to 1 of 4 treatments: T0, T1, T2 and T4, representing supplementation of curcumin at 0, 1, 2, and 4 mg/kg concentrate, respectively. The animals in each treatment were allocated in 4 pens of 2 lambs each (8 lambs per treatment). The experiment lasted 17 d, with samples and measurements collected on d 0, 7, 12, and 17. The T2 lambs had greater average daily gain than T0 lambs. Regression analysis showed that the ideal dose of N-CU to enhance weight gain was 1.89 mg/kg concentrate. There were significant interactions (P < 0.05) between treatments × time for hematological variables, particularly for increases in erythrocytes (T2) and reductions in counts of leukocytes, neutrophils, and lymphocytes in T1 and T2. There were significant interactions between treatment × time for total protein, globulin, urea, and triglyceride levels. Stimulation of the antioxidant system was also observed. There were increased levels of non-protein thiols (NPSH), as well as increased activities of superoxide dismutase (SOD) and glutathione S-transferase (GST) in the supplemented animals. Levels of reactive oxygen species (ROS) were lower in the serum of supplemented lambs. In general, the 4 mg/kg dose had no positive effects on growth or health. This was an unexpected result, given the known properties of curcumin. Taken together, these findings suggest that addition of low concentrations of nanoencapsulated curcumin (T1 and T2) in lamb feed improves health, minimizing oxidative stress and generates anti-inflammatory effects that may have contributed indirectly to greater weight gain. Nanocapsules potentiate the effects of curcumin and may emerge as a new tool in animal nutrition.

Phytochemical analysis and evaluation of the antioxidant and antiproliferative effects of Tucumã oil nanocapsules in breast adenocarcinoma cells (MCF-7).

In this work was to develop an inedited nanocapsule with tucumã oil (Astrocaryum vulgare). The oil presents of phytosterols (squalene and ß-sitosterol), all-trans-beta-carotene, acids oleic and palmitic. Antioxidant activity showed a good performance in DPPH and ABTS assays. The nanocapsules were prepared and demonstrated in their characterization particle size (206 ± 0.69 nm). The cytogenotoxicity evaluation was performed using the MTT, dichlorofluorescein, nitric oxide and dsDNA PicoGreen® assays. Antitumor efficacy assays in MCF-7 cells demonstrated that free oil and tucumã nanocapsules had IC50 of 130 and 50 µg/mL, respectively. Thus, previous studies of toxicity are relevant, as they generate future subsidies, aiming at the potential application of nanostructures and in addition, the promising effect of NCs of tucumã oil on the antiproliferative effect in breast adenocarcinoma cells was evidenced.

In vitro and in vivo activity of the essential oil and nanoemulsion of Cymbopogon flexuosus against Trichomonas gallinae.

OBJECTIVE: This study was done to evaluate the in vitro and in vivo effects of the essential oil (OE-CL) and nanoemulsion (N-CL) of Cymbopogon flexuosus against Trichomonas gallinae. MATERIALS AND METHODS: In vitro assays were done with 106 parasites and OE-CL and N-CL in the concentrations: 110, 220, 330, 440, 550, 660, 770 and 880 µg/ml and four controls: CN (culture medium and trophozoites), MTZ (trophozoites plus 800 µg/ml of metronidazole), TW (trophozoites plus vehicles used for solubilization of derivatives (0.01% Tween) and NB (blank nanoemulsion 880 µg/ml). The in vivo assay was done in 35 quails (Coturnix coturnix) infected experimentally 4x104 mg/kg, were divided in seven groups (n=5): A (control-healthy), B (control infected), C (control TW 0.01%), D (NB 0.88 mg/kg), E (drug MTZ 25 mg/kg, F (OE-CL at 0.55 mg/kg) and G (N-CL at 0.44 mg/kg), during 7 consecutive days. RESULTS: The in vitro test showed that the OE-CL (550 µg/ml) and N-CL (440 µg/ml) concentrations reduced the trophozoites viability in 100%. In the in vivo test, the treatment with OE-CL was efficient on the 4th treatment day and the N-CL after the 3rd day, and the MTZ in the therapeutic concentration was efficient on the 7th day. CONCLUSION: It can be observed in this study that the lemon grass has natural potential antitrichomonal activity against T. gallinae in vitro and in vivo.