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1.
Res Vet Sci ; 171: 105247, 2024 May.
Article in English | MEDLINE | ID: mdl-38554611

ABSTRACT

To characterize wild-type bacteriophages and their effect on Salmonella Heidelberg intestinal colonization in broilers, phages combined in a cocktail were continuously delivered via drinking water since the first day after hatching. After challenge with a field strain, broilers were evaluated at regular intervals for S. Heidelberg and bacteriophages in tissues and cecum, and gross and microscopic lesions in organs. Phages were highly virulent against S. Heidelberg by efficiency of plating. One-step growth curves exhibited eclipse period from 20 to 25 min, whereas the lowest latent period and higher burst size found were 45 min and 54 PFU/cell, respectively. Bacteriophage whole genomic sequencing analyses revealed a lack of genes related to lysogeny, antimicrobial resistance, and virulence factors. Relevant gross or microscopic lesions were absent in tissues analyzed from treated broilers. Although numerically stable bacteriophage concentrations were detected in the cecal contents of treated broilers, no significant difference was found for the S. Heidelberg cecal load in comparison to the untreated group and for the prevalence of positive tissues throughout the evaluated period. The phages produced turbid plaques against some S. Heidelberg re-isolated from treated broilers, suggesting the evolving of a resistant subpopulation. Overall, the results provide new evidence of the safety and in vitro replication of such phages in S. Heidelberg. Nevertheless, continuous administration of the phage suspension most likely induced the development of bacteriophage-resistant mutants, which might have affected the in vivo effect. Therefore, a putative administration protocol should be based on other strategies, such as short-term therapy at pre-harvest age.


Subject(s)
Bacteriophages , Animals , Chickens , Salmonella , Intestines
2.
Virol J ; 20(1): 181, 2023 08 16.
Article in English | MEDLINE | ID: mdl-37587490

ABSTRACT

BACKGROUND: Influenza A virus (IAV) is endemic in pigs globally and co-circulation of genetically and antigenically diverse virus lineages of subtypes H1N1, H1N2 and H3N2 is a challenge for the development of effective vaccines. Virosomes are virus-like particles that mimic virus infection and have proven to be a successful vaccine platform against several animal and human viruses. METHODS: This study evaluated the immunogenicity of a virosome-based influenza vaccine containing the surface glycoproteins of H1N1 pandemic, H1N2 and H3N2 in pigs. RESULTS: A robust humoral and cellular immune response was induced against the three IAV subtypes in pigs after two vaccine doses. The influenza virosome vaccine elicited hemagglutinin-specific antibodies and virus-neutralizing activity. Furthermore, it induced a significant maturation of macrophages, and proliferation of B lymphocytes, effector and central memory CD4+ and CD8+ T cells, and CD8+ T lymphocytes producing interferon-γ. Also, the vaccine demonstrated potential to confer long-lasting immunity until the market age of pigs and proved to be safe and non-cytotoxic to pigs. CONCLUSIONS: This virosome platform allows flexibility to adjust the vaccine content to reflect the diversity of circulating IAVs in swine in Brazil. The vaccination of pigs may reduce the impact of the disease on swine production and the risk of swine-to-human transmission.


Subject(s)
Influenza A Virus, H1N1 Subtype , Influenza A virus , Influenza Vaccines , Influenza, Human , Humans , Animals , Swine , Vaccines, Combined , Immunity, Humoral , CD8-Positive T-Lymphocytes , Influenza A Virus, H3N2 Subtype , Virosomes
3.
Virol J ; 20(1): 187, 2023 08 21.
Article in English | MEDLINE | ID: mdl-37605141

ABSTRACT

BACKGROUND: Influenza A virus (IAV) causes respiratory disease in pigs and is a major concern for public health. Vaccination of pigs is the most successful measure to mitigate the impact of the disease in the herds. Influenza-based virosome is an effective immunomodulating carrier that replicates the natural antigen presentation pathway and has tolerability profile due to their purity and biocompatibility. METHODS: This study aimed to develop a polyvalent virosome influenza vaccine containing the hemagglutinin and neuraminidase proteins derived from the swine IAVs (swIAVs) H1N1, H1N2 and H3N2 subtypes, and to investigate its effectiveness in mice as a potential vaccine for swine. Mice were immunized with two vaccine doses (1 and 15 days), intramuscularly and intranasally. At 21 days and eight months later after the second vaccine dose, mice were euthanized. The humoral and cellular immune responses in mice vaccinated intranasally or intramuscularly with a polyvalent influenza virosomal vaccine were investigated. RESULTS: Only intramuscular vaccination induced high hemagglutination inhibition (HI) titers. Seroconversion and seroprotection (> 4-fold rise in HI antibody titers, reaching a titer of ≥ 1:40) were achieved in 80% of mice (intramuscularly vaccinated group) at 21 days after booster immunization. Virus-neutralizing antibody titers against IAV were detected at 8 months after vaccination, indicating long-lasting immunity. Overall, mice immunized with the virosome displayed greater ability for B, effector-T and memory-T cells from the spleen to respond to H1N1, H1N2 and H3N2 antigens. CONCLUSIONS: All findings showed an efficient immune response against IAVs in mice vaccinated with a polyvalent virosome-based influenza vaccine.


Subject(s)
Influenza Vaccines , Influenza, Human , Vaccines, Virosome , Bronchoalveolar Lavage , Influenza A Virus, H1N1 Subtype , Influenza A Virus, H1N2 Subtype , Influenza A Virus, H3N2 Subtype , Influenza Vaccines/administration & dosage , Influenza Vaccines/immunology , Influenza, Human/immunology , Spleen/cytology , Spleen/immunology , Vaccines, Combined/administration & dosage , Vaccines, Virosome/administration & dosage , Vaccines, Virosome/immunology , Virosomes/ultrastructure , Humans , Animals , Mice
4.
Drug Deliv Transl Res ; 13(2): 642-657, 2023 02.
Article in English | MEDLINE | ID: mdl-36008703

ABSTRACT

Buccal drug administration may be chosen as a medication route to treat various diseases for local or systemic effects. This study proposes the development of a thermosensitive hydrogel containing curcumin-loaded lipid-core nanocapsules coated with chitosan to increase mucoadhesion, circumventing several limitations of this route of administration. Hydroxypropylmethylcellulose and Poloxamer® 407 were incorporated for hydrogel production. Physicochemical characterization parameters, such as particle size distribution, mean diameter, polydispersity index, zeta potential, and morphology, were analyzed. Spherical homogeneous particles were obtained with average diameter, of 173 ± 22 nm for LNCc (curcumin lipid-core nanocapsules) and 179 ± 48 nm for CLNCc (chitosan-curcumin lipid-core nanocapsules). A PDI equal to 0.09 ± 0.02 for LNCc and 0.26 ± 0.01 for CLNCc confirmed homogeneity. Tensile analysis and washability test on porcine buccal mucosa indicated higher mucoadhesion for hydrogels in comparison to the nanocapsules in suspension, remaining on the mucous membrane up to 8 h (10.92 ± 3.95 µg of curcumin washed for H-LNCc and 28.41 ± 24.47 µg for H-CLNCc) versus the latter, which remained washed on the membrane for 90 min only (62.60 ± 4.72 µg for LNCc and 52.08 ± 1.63 µg for CLNCc). The irritant potential (IR) of the formulations was evaluated by the hen's egg chorioallantoic membrane test (HET-CAM), with no irritation phenomena observed. Formulations were tested for their efficacy in an in vitro model against oral squamous cancer cell line, showing a significant reduction in cell viability on all tested groups. These findings demonstrated that the proposed nanosystem is mucoadhesive and has potential to deliver buccal treatments.


Subject(s)
Carcinoma, Squamous Cell , Chitosan , Curcumin , Head and Neck Neoplasms , Mouth Neoplasms , Nanocapsules , Animals , Female , Swine , Nanocapsules/chemistry , Hydrogels , Chitosan/chemistry , Squamous Cell Carcinoma of Head and Neck , Chickens , Mouth Neoplasms/drug therapy , Lipids/chemistry
5.
Pharmaceutics ; 14(2)2022 Feb 10.
Article in English | MEDLINE | ID: mdl-35214122

ABSTRACT

Coccidiosis is a disease caused by intracellular protozoan parasites of the genus Eimeria that affect the intestinal tract of poultry. However, strain resistance and drug residue in the carcass have drawn the attention of the productive sector. The nanotechnology can improve the biological effect of drugs, reducing of administered doses and toxic effects. Due to this, toltrazuril-load polymeric nanoparticles based on Eudragit® S100 (NCt) or poly-ε-caprolactone (LNCt) were developed to prevent coccidiosis in broilers. Nanoformulations were produced and showed homogeneous particle diameter distribution in the nanometer range (z-average and D (4.3) < 200 nm), negative zeta potential (<-8.93 mV), drug content ~100%, and encapsulation efficiency >90%. Cell viability assays using avian fibroblasts showed that LNCt presented no relevant toxicity up to 72 h. LNCt was then prophylactically administrated to chicken followed by challenge with Eimeria oocysts. The evaluation of the small intestine and cecum showed that the treatment with LNCt (3.5 mg/kg/day) in drinking water reduced the lesion scores and oocysts excretion, similar to the reference medicine containing toltrazuril (Baycox®, 7 mg/kg/day). The current study shows the potential protective use of nanoencapsulating anticoccidial drugs as a promising approach for the control of coccidiosis in poultry.

6.
PLoS One ; 16(5): e0249366, 2021.
Article in English | MEDLINE | ID: mdl-33939699

ABSTRACT

Piglets are highly vulnerable to infections, but colostrum provides them with some protection. The function of colostrum components is unknown, as is if the amount and subsets of leukocytes in colostrum differ between gilts and sows. This study serially characterized leukocyte populations in colostrum for differential leukocyte counts. Differences in humoral and cellular composition of colostrum between 40 gilts and 40 sows (parities orders 3-4) from a commercial herd were examined. Flow cytometry is a useful tool to identify and quantify leukocyte subsets in sow colostrum. Overall, there were no (p ≥ 0.05) parity differences in total macrophages, granulocytes, and T and B cells. However, the sows' colostrum presented significantly higher (p ≤ 0.05) T lymphocyte subsets than gilts, such as central memory CD4+T cells, effector memory CD4+T cells, and central memory CD8+T cells. Among B-lymphocytes, percentages of SWC7+CD5+ cells were significantly higher in sow colostrum than in that of gilts. As expected, IgG concentrations were significantly higher in sows than in gilts. Colostrum from sows had significantly greater mitogenic activity than colostrum from gilts and this fact can be associated with the potential to accelerate the maturation of a newborn's gastrointestinal tract. Our findings suggest that parity order may be one among other factors influencing the cell population and, consequently, the immune adaptive response in piglets that induces neutralizing antibodies and cellular immune responses to antigens.


Subject(s)
B-Lymphocytes/immunology , Colostrum/cytology , Swine/immunology , T-Lymphocytes/immunology , Animals , Cell Line , Cells, Cultured , Female , Immunoglobulin G/analysis , Immunophenotyping/veterinary , Lymphocyte Subsets , Rats , Swine/growth & development , Swine/physiology
7.
Braz. J. Vet. Res. Anim. Sci. (Online) ; 56(1): e150479, jun. 2019. graf
Article in English | LILACS, VETINDEX | ID: biblio-1007833

ABSTRACT

Cases of salmonellosis in humans have been associated with consumption of eggs contaminated with this bacterial pathogen due to insufficient heat treatment. The most prevalent serotypes of Salmonella in Brazil include serotypes Enteritidis, Typhimurium, and Heidelberg. The first two serotypes are major causes for eggs to be withheld from sale and for recalls over Salmonella contamination concerns in both domestic and foreign markets. Eggs may be contaminated through transovarian infection (transovarial transmission) due to the presence of the microorganism in the hen's oviduct and bacterial penetration of the eggshell. There is little data in the literature on the susceptibility of egg contamination and eggshell penetration by Brazilian serotypes of Salmonella. The present study aimed to evaluate the ability of S. Heidelberg and S. Typhimurium serotypes to penetrate through the eggshell and detect these bacteria in the albumen and yolk according to the thickness of the eggshell. SPF (specific-pathogen-free) eggs were artificially contaminated by contact with moist cotton containing Salmonella (15 x 108 CFU/ml). Eggs were divided into the following groups: negative control (not contaminated), S. Heidelberg, and S. Typhimurium. Subsequently, these eggs were incubated at 37°C, and their contents analyzed after 4 h and 24 h of incubation. The evaluation (assessment) of the contamination was performed by traditional bacteriology and confirmed by biochemical and serological tests. Treatments were compared with Fisher's test using a SAS statistical software. For S. Heidelberg, the percentage of positivity (positive cases) was lower in both albumen and yolk at 4 h and 24 h intervals (33.33% and 3.7%, and 3.7% and 3.7%, respectively) compared to S. Typhimurium (26.63% and 7.41%, and 33.33% and 33.33%, respectively). These findings suggest that the former strain (S. Heidelberg) was unable to survive in the hostile environment of the albumen. In contrast, eggshell thickness had no significant correlation with the number of positive samples. In conclusion, the results obtained in the egg infection model show that the Salmonella strains tested were able to penetrate the eggshell and multiply in both the albumen and yolk and that S. Typhimurium proved to be the most efficient to grow within these portions of the egg.(AU)


Salmonelose em humanos é frequentemente associada ao consumo de ovos contaminados sem o devido processamento térmico. No Brasil, os sorotipos mais prevalentes são: Enteritidis, Typhimurium e Heidelberg, alvo de barreiras sanitárias na comercialização de ovos. O ovo pode ser contaminado por via transovariana, pela presença da bactéria no oviduto da ave e também por penetração da bactéria através da casca do ovo. Existem poucas informações acerca da capacidade de contaminação no ovo por sorotipos isolados no Brasil. Este estudo teve como objetivo avaliar a capacidade dos sorotipos S. Heidelberg e S. Typhimurium penetrar através da casca do ovo e colonizar a albumina e gema, relacionando à espessura da casca. Os ovos SPF (livres de patógenos específicos) foram contaminados artificialmente pelo contato com algodão umedecido (15 x 108 CF/mL). Os ovos foram divididos nos seguintes grupos: controle negativo (sem contaminação), S. Heidelberg e S. Typhimurium. Posteriormente foram incubadas a 37°C e seu conteúdo foi analisado após 4 e 24 h. A avaliação da contaminação foi realizada por bacteriologia tradicional e confirmada por testes bioquímicos e sorológicos. Os tratamentos foram comparados com o teste de Fisher usando o software estatístico SAS. Para S. Heidelberg, a percentagem de positividade foi menor no albúmen e gema às 4 e 24 h (33,33% e 3,7%, 3,7% e 3,7%, respectivamente) em comparação com S. Typhimurium (26,63% e 7,41%, 33,33% e 33,33%, respectivamente), sugerindo que a primeira estirpe foi mais vulnerável as condições hostis da albumina. Por outro lado, a espessura da casca do ovo não teve relação significativa com a positividade das amostras. Em conclusão, o modelo de infecção do ovo mostrou que as cepas foram capazes de penetrar a casca do ovo e sobreviver na albumina e gema, sendo que o sorotipo S. Typhimurium foi mais eficiente.(AU)


Subject(s)
Animals , Salmonella Infections/diagnosis , Salmonella Infections/microbiology , Food Supply , Chickens
8.
Zygote ; 26(4): 286-293, 2018 Aug.
Article in English | MEDLINE | ID: mdl-30210017

ABSTRACT

SummaryThe aim of this study was to optimize protocols for electroporation (EP) and polyfection (PLF) using polyethyleneimine (PEI) for pig sperm transfection and to determine which method was the most efficient. For EP standardization, different voltages, amounts and times of electric pulses were tested using propidium iodide (PI) as reporter. For PLF standardization, different concentrations of fluorescein isothiocyanate (FITC)-labelled PEI (PEI/FITC) were incubated with sperm for different periods of time. Flow cytometry was performed to evaluate the best protocol in terms of cell viability, including cytoplasmic membrane, acrosome, chromatin integrities and mitochondrial potential using the FITC probe, PI, acridine orange (AO) and JC1. Transfections with the plasmid pmhyGENIE-5 were carried out under optimum conditions for each procedure (EP: 500 volts, 500 µs and two pulses; PLF: PEI 0.5 mg/ml and incubation time 10 min). Transfection efficacy was assessed by fluorescence in situ hybridization (FISH). A lower transfection rate was observed for sperm in the control group (17.8%) compared with EP (36.7%), with PLF (76.8%) being the most efficient. These results suggest that the EP and PEI could be an efficient and low cost transfection method for swine sperm. Notably, treated cells showed higher plasmatic the membrane damage (PMD) and/or acrosome damage (AD) indexes, therefore the combination of this procedure with biotechniques that facilitate fecundation (i.e. in vitro fertilization or intracytoplasmic sperm injection) or even inclusion of antioxidant or anti-apoptotic drugs to improve spermatozoa viability would be important.


Subject(s)
Electroporation/veterinary , Polyethyleneimine/chemistry , Semen Preservation/veterinary , Spermatozoa/cytology , Transfection/veterinary , Animals , Cell Survival , Fertilization in Vitro , Male , Sperm Motility , Spermatozoa/physiology , Swine
9.
Oxid Med Cell Longev ; 2018: 8194849, 2018.
Article in English | MEDLINE | ID: mdl-30647816

ABSTRACT

Contact dermatitis produces an inflammatory reaction primarily via stimulation of keratinocytes and cells of the immune system, which promote the release of cytokines, reactive oxygen species (ROS), and other chemical mediators. Eugenol (EUG, phenylpropanoid of essential oils) has attracted attention due to its anti-inflammatory properties, as well as antioxidant effect. On the other hand, it is volatile and insoluble and is a skin irritant. In this case, nanostructured systems have been successfully employed as a drug carrier for skin diseases since they improve both biological and pharmaceutical properties of active compounds. The cytotoxic, antioxidant, and anti-inflammatory effects of EUG were assessed in human neutrophils and keratinocytes. Additionally, polymeric nanocarries (NCEUG) were prepared to improve the chemical and irritant characteristics of EUG. EUG presented apparent safety and antioxidant and anti-inflammatory effects on human neutrophils, but presented cytotoxic effects on keratinocytes. However, the nanocapsules were able to reduce its cytotoxicity. An in vivo experiment of irritant contact dermatitis (ICD) in mice induced by TPA showed that NCEUG reduced significantly the ear edema in mice when compared to the EUG solution, as well as the leukocyte infiltration and IL-6 level, possibly due to better skin permeation and irritancy blockage. These findings suggest that EUG is a promising bioactive molecule, and its nanoencapsulation seems to be an interesting approach for the treatment of ICD.


Subject(s)
Anti-Infective Agents/therapeutic use , Dermatitis/drug therapy , Eugenol/therapeutic use , Animals , Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents , Antioxidants , Dermatitis/pathology , Eugenol/pharmacology , Humans , Male , Mice
10.
Pharmacogn Mag ; 12(48): 307-312, 2016.
Article in English | MEDLINE | ID: mdl-27867274

ABSTRACT

BACKGROUND: Erythrina velutina is a tree common in the northeast of Brazil extensively used by traditional medicine for the treatment of central nervous system disorders. OBJECTIVE: To develop a standardized ethanol extract of E. velutina (EEEV) and to investigate the neuroprotective potential of the extract and rizonic acid (RA) from E. velutina on neuronal cells. MATERIALS AND METHODS: The plant drug of E. velutina previously characterized was used for the production of EEEV. Three methods were evaluated in order to obtain an extract with higher content of phenols. The neuroprotective effect of standardized EEEV (HPLC-PDA) and RA was investigated on SH-SY5Y cell exposure to the neurotoxin 6-hydroxydopamine (6-OHDA). RESULTS: The powder of the plant drug was classified as moderately coarse and several quality control parameters were determined. EEEV produced by percolation gave the highest phenol content when related to others extractive methods, and its HPLC-PDA analysis allowed to identify four flavonoids and RA, some reported for the first time for the species. EEEV and RA reduced significantly the neurotoxicity induced by 6-OHDA in SH-SY5Y cells determined by the MTT assay and the nitrite concentration. EEEV also showed a free radical scavenging activity. CONCLUSION: This is the first pharmacological study about E. velutina which used a controlled standardized extract since the preparation of the herbal drug. This extract and RA, acting as an antioxidant, presents a neuroprotective effect suggesting that they have potential for future development as a therapeutic agent in neurodegenerative disease as Parkinson. SUMMARY: The powder of Erythrina velutina was classified as moderately coarse and several quality-control parameters were determined.Ethanolic extract from E. velutina (EEEV) produced by percolation gave the highest phenol content when related to others extractive methods and its HPLC-PDA analysis of EEEV allowed to identify four flavonoids and rizonic acid (RA), some reported for the first time for the species.The EEEV and RA reduced significantly the neurotoxicity induced by 6-OHDA in SH-SY5Y cells determined by the MTT assay and the nitrite concentration.The EEEV also showed a free radical scavenging activity. Abbreviations used: ±: More or less, %: Percentage, °C: Degree Celsius, <: Less than, µg: Microgram, µL: Microliter, µM: Micromol, [1D] MNR: One-dimensional nuclear magnetic resonance spectroscopy, [2D] MNR:Two-dimensional nuclear magnetic resonance spectroscopy, 6-OHDA: [6-] Hydroxydopamine. Abs: Absorbance, CFU: Colony forming units, CH2Cl2: Dichloromethane, CHCl3: Chloroform cmCentimeter, DMEM/F12: Dulbecco's Modified Eagle's Medium: Nutrient Mixture F-12. DMSO: Dimethyl sulfoxide, DPPH: 1,1-Diphenyl-2-picrylhydrazyl, EAG: Gallic acid equivalents, EEEV: Ethanolic extract of Erythrina velutina, EtOAc: Ethyl acetate, g: Gram, h: Hour, H2O: Water, HPLC: High-performance liquid chromatography, H REIMS: Hydrogen rapid evaporative ionization mass spectrometry, Kg: Kilogram M: Molar, m: Metro, MeOH: Methanol, mg: Milligram, min: Minute, mL: Milliliter, mm: Millimeter, MTT: Bromide 3 [4,5-dimethylthiazol-2-yl] -2,5-diphenyltetrazolium, N: Normal, NBT: Nitroblue tetrazolium, nm: Nanometer, PDA: Photodiode array detector, TPC: Total polyphenol content, RA: Rizonic acid, RP: Reverse phase, SOD: Superoxide dismutase, v/v: Volume per volume, Vs: Versus W: Watts.

11.
Saúde debate ; 38(102): 551-561, 09/2014. tab
Article in Portuguese | LILACS-Express | LILACS | ID: lil-726388

ABSTRACT

Analisa a influência dos grupos terapêuticos em Centro de Atenção Psicossocial entre usuários com dependência de cocaína/crack, em Fortaleza - Ceará. Estudo descritivo e retrospectivo, entre 2009 e 2010. Realizou-se uma análise bivariada entre as variáveis dependentes e independentes. Os grupos terapêuticos foram influenciados pela profissão, por abandono de tratamento, drogas ilícitas, número de consultas e prescrições. Observa-se a necessidade de elaborar estratégias para melhorar as ações preventivas comunitárias, visando a aumentar a adesão dos dependentes de cocaína/crack às atividades terapêuticas, conforme a legislação vigente de saúde mental.


It analyzes the influence of the therapeutic groups at Psychosocial Care Center among users with cocaine/crack dependence, Fortaleza - Ceará. Descriptive and retrospective study between 2009 and 2010. A bivariate analysis between the dependent and independent variables was performed. The therapeutic groups were influenced by the occupation, treatment abandonment, illegal drugs, number of visits to the doctors and prescriptions. It is observed the necessity to elaborate strategies in order to improve communitarian preventive actions, aiming to increase the cocaine/crack dependents adherence to the therapeutic activities, in accordance to the current mental health legislation.

12.
Curr Pharm Des ; 19(41): 7294-300, 2013.
Article in English | MEDLINE | ID: mdl-23489206

ABSTRACT

In nanomedicine, different nanomaterials and nanoparticles have been proposed as therapeutic agents or adjuvants, as well as diagnosis devices. Considering that the principal cause of the ulcerations is the imbalance among the gastric juice secretion and the protection provided by the mucosal barrier and the neutralization of the gastric acid, as well as that nanoparticles are able to accumulate in the gastro-intestinal tissues, we proposed a 2(2) factorial design to evaluate the influence of the chemical composition and the volume fraction of the dispersed phase on the gastric protective effect against ulceration induced by ethanol. Cocoa-theospheres (CT) and lipid-core nanocapsules (LNC) (two different kinds of surfaces: lipid and polymeric, respectively) prepared at two different concentrations of soft materials: 4% and 12% (w/v) were produced by high pressure homogenization and solvent displacement methods, respectively. Laser diffraction showed volume-weighted mean diameters ranging from 133 to 207 nm, number median diameters lower than 100 nm and specific surfaces between 41.2 and 51.2 m(2) g(-1). The formulations had pH ranging from 4.7 to 6.3; and zeta potential close to -9 mV due to their coating with polysorbate 80. The ulcer indexes were 0.40 (LNC(4)) and 0.48 (CT(4)) for the lower total administered areas (3.3 and 4.1 m(2)g(-1), respectively), and 0.09 (LNC(12) and CT(12)) for the higher administered areas (10.0 and 12.0 m(2) g(-1), respectively). LNC(4), LNC(12) and CT(12) showed lower levels in the lipid peroxidation assay when compared either to the negative control (saline) or to CT(4). LNC(12) and CT(12) showed similar TBARS levels, as well as CT(4) was similar to the negative control. SEM analysis of the stomach mucosa showed coatings more homogenous and cohesive when LNC formulations were administered compared to the correspondent CT formulations. The higher total area of administered nanoparticles showed film formation. Moreover, LNC(12) provided a more thick and cohesive film, completely covering the mucosal surface. In conclusion, both kinds of formulations are able to prevent ulceration induced by ethanol in rats. The 2(2) factorial design showed that the chemical composition had a strong influence when the lower areas of nanoparticles are administered, while when the higher areas are used this is the more influencing parameter on the gastroprotection.


Subject(s)
Cacao , Gastric Mucosa/drug effects , Nanoparticles/administration & dosage , Stomach Ulcer/prevention & control , Animals , Cacao/chemistry , Chemistry, Pharmaceutical , Gastric Mucosa/pathology , Male , Nanoparticles/chemistry , Protective Agents/administration & dosage , Protective Agents/chemistry , Rats , Rats, Wistar , Stomach Ulcer/pathology
13.
Expert Opin Drug Deliv ; 10(5): 623-38, 2013 May.
Article in English | MEDLINE | ID: mdl-23387432

ABSTRACT

INTRODUCTION: Poly(ϵ-caprolactone) (PCL), a biodegradable and biocompatible polymer, is useful to encapsulate a wide range of drugs making it an interesting material for the preparation of carriers with potential applications in therapeutics. AREAS COVERED: The design and development of those carriers to modulate drug release, to improve the drug stability or apparent solubility in aqueous media, as well as to target tissues and organs are discussed. EXPERT OPINION: Microencapsulation is a well-established process in pharmaceutical industry to protect drugs from chemical degradation and to control drug release. In this context, PCL is a useful polymer to prepare microcapsules. Nanoencapsulation, a more recent approach, offers new possibilities in drug delivery. PCL can be used as polymer to prepare different types of nanocapsules presenting diverse flexibility according to the chemical nature of the core. Those nanocapsules are capable of controlling drug release and improving photochemical stability. In addition, they can modulate cutaneous drug penetration/permeation and act as physical sunscreen due to their capability of light scattering. Considering the pharmaceutical point of view, PCL nanocapsules are versatile formulations, once they can be used in the liquid form, as well as incorporated into semi-solid or solid dosage forms.


Subject(s)
Capsules/chemistry , Drug Delivery Systems , Nanocapsules/chemistry , Polyesters/chemistry , Animals , Biocompatible Materials , Chemistry, Pharmaceutical , Drug Compounding , Drug Stability , Humans , Polymers/administration & dosage , Skin/metabolism , Solubility , Sunscreening Agents/administration & dosage , Sunscreening Agents/pharmacokinetics
14.
Planta Med ; 74(5): 497-502, 2008 Apr.
Article in English | MEDLINE | ID: mdl-18404596

ABSTRACT

The aim of this study was to investigate the possible beneficial effects of amburoside A, AMB [4-(O-beta- D-glycopyranosyl)benzyl protocatechoate], against carbon tetrachloride (CCl (4)) toxicity in rats. AMB is a phenol glucoside from the Brazilian medicinal plant Amburana cearensis, popularly used for the treatment of respiratory tract affections. Acute AMB (25 and 50 mg/kg, I. P. or P. O.) treatments of CCl (4)-intoxicated rats significantly inhibited the increase in serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT) levels, as compared to the group treated with CCl (4) only. Histological studies showed less centrolobular necrosis and inflammatory cell infiltrates in the liver of animals treated with AMB plus CCl (4), when compared to the group treated with CCl (4) alone. In hepatic tissues, AMB at both doses inhibited CCl (4)-induced thiobarbituric acid-reactive substances (TBARS) formation, indicating a blockade of CCl (4)-induced lipid peroxidation. AMB also reversed the decrement in glutathione contents of hepatic tissues in CCl (4)-intoxicated rats. Furthermore, it restored catalase activity to normal values, which was significantly increased after CCl (4) treatment. Our results indicate that CCl (4)-induced oxidative damage in hepatic tissues is reversed by AMB treatment. The protective effect of AMB is probably due to the phenolic nature of this glucoside.


Subject(s)
Chemical and Drug Induced Liver Injury/prevention & control , Fabaceae/chemistry , Glucosides/therapeutic use , Phytotherapy , Plant Extracts/therapeutic use , Alanine Transaminase/blood , Animals , Aspartate Aminotransferases/blood , Carbon Tetrachloride , Carbon Tetrachloride Poisoning/drug therapy , Carbon Tetrachloride Poisoning/metabolism , Carbon Tetrachloride Poisoning/pathology , Catalase/metabolism , Chemical and Drug Induced Liver Injury/blood , Chemical and Drug Induced Liver Injury/pathology , Glucosides/isolation & purification , Glutathione/metabolism , Liver/enzymology , Liver/metabolism , Liver/pathology , Male , Plant Extracts/chemistry , Rats , Rats, Wistar , Thiobarbituric Acid Reactive Substances/metabolism
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