ABSTRACT
In this work, we provide proof-of-concept of formation, physical characteristics and potential use as a drug delivery formulation of Pickering emulsions (PE) obtained by a novel method that combines nanoprecipitation with subsequent spontaneous emulsification process. To this end, pre-formed ultra-small (d.â¼10â¯nm) nanoprecipitated nanoparticles of hydrophobic derivatives of cashew tree gum grafted with polylactide (CGPLAP), were conceived to stabilize Pickering emulsions obtained by spontaneous emulsification. These were also loaded with Amphotericin B (AmB), a drug of low oral bioavailability used in the therapy of neglected diseases such as leishmaniasis. The graft reaction was performed in two CG/PLA molar ratio conditions (1:1 and 1:10). Emulsions were prepared by adding the organic phase (Miglyol 812®) in the aqueous phase (nanoprecipitated CGPLAP), resulting the immediate emulsion formation. The isolation by centrifugation does not destabilize or separate the nanoparticles from oil droplets of the PE emulsion. Emulsions with CGPLAP 1:1 presented unimodal distributions at different CGPLA concentration, lower values in size and PDI and the best stability over time. The AmB was incorporated in the emulsions with a process efficiency of 21-47%, as determined by UV-vis. AmB in CGPLAP emulsions is in less aggregated state than observed in commercial AmB formulation.
Subject(s)
Amphotericin B/pharmacology , Anacardium/chemistry , Drug Compounding , Nanoparticles/chemistry , Plant Gums/chemical synthesis , Polyesters/chemical synthesis , Amphotericin B/chemistry , Chemical Precipitation , Emulsions/chemistry , Particle Size , Plant Gums/chemistry , Spectrophotometry, Ultraviolet , Static ElectricityABSTRACT
Dimorphandra gardneriana galactomannan (DG) was sulfated in pyridine:formamide using chlorosulfonic acid as the sulfation agent. The degree of substitution was 0.32, determined from the sulfur percentage. Confirmation of sulfation was obtained by FTIR spectroscopy through the presence of an asymmetrical SO stretching vibration at 1,259 cm(-1). NMR data showed that the sulfation occurred on primary hydroxyl groups. NMR and GPC data indicate degradation during reaction with elimination of galactose. At the maximum tested concentration of 1,000 µg/mL, unmodified DG polysaccharide did not show a statistically significant cytotoxicity in Vero cells by the MTT method. Therefore, the CC50>1,000 µg/mL obtained for the sulfated polysaccharides from D. gardneriana in Vero cells point to its lower cytotoxicity than the sulfated galactomannan from Mimosa scabrella.
Subject(s)
Fabaceae/chemistry , Mannans/chemistry , Mannans/toxicity , Sulfates/chemistry , Toxicity Tests , Animals , Chlorocebus aethiops , Galactose/analogs & derivatives , Mannans/isolation & purification , Seeds/chemistry , Vero CellsABSTRACT
The search for bioactive molecules to be employed as recognition elements in biosensors has stimulated researchers to pore over the rich Brazilian biodiversity. In this sense, we introduce the use of natural cashew gum (Anacardium occidentale L.) as an active biomaterial to be used in the form of layer-by-layer films, in conjunction with phthalocyanines, which were tested as electrochemical sensors for dopamine detection. We investigated the effects of chemical composition of cashew gum from two different regions of Brazil (Piauí and Ceará states) on the physico-chemical characteristics of these nanostructures. The morphology of the nanostructures containing cashew gum was studied by atomic force microscopy which indicates that smooth films punctuated by globular features were formed that showed low roughness values. The results indicate that, independent of the origin, cashew gum stands out as an excellent film forming material with potential application in nanobiomedical devices as electrochemical sensors.
Subject(s)
Anacardium/chemistry , Biocompatible Materials/chemistry , Nanostructures/chemistry , Biosensing Techniques/methods , Dopamine/chemistry , Indoles/chemistry , IsoindolesABSTRACT
This work aims to assess the potential of the green seaweed Ulva fasciata Delile as an alternative source of dietary fibre (DF). Total DF content was determined, some of its physico-chemical properties described and the physiological effects of U. fasciata meal on rats fed a hypercholesterolemic diet were investigated. U. fasciata may be considered a potential alternative source of DF with a total content of about 400 g.kg-1 (dry basis) and interesting physico-chemical properties: water retention capacity of 8.74 g/water.g-1 dry sample (seaweed meal) and 0.90 (seaweed carbohydrate extract), lipid adsorption capacity of 4.52 g/oil.g-1 dry sample (seaweed meal) and 5.70 (seaweed carbohydrate extract), intrinsic viscosity of 2.4 dl.g-1 (seaweed carbohydrate extract) and cation exchange capacity of 3.51 Eq.kg-1 (seaweed carbohydrate extract). The diet containing seaweed meal was able to keep rats' total cholesterol (TC) down without causing any undesirable increase in LDL-C fraction. No evidence of toxic and/or antinutritional components in the seaweed meal was detected. Rats showed a fecal volume much greater (13 g) than that fed on cellulose diet (7 g) (p < 0.05). These properties confer on the seaweed the potential to be used in food technology for the acquisition of low-calorie food and might be important in body weight control, reduction of blood TC and LDL-C as well as in prevention of gastrointestinal diseases.
Subject(s)
Dietary Fiber/metabolism , Hypercholesterolemia/diet therapy , Lipids/blood , Seaweed/chemistry , Ulva/chemistry , Animals , Cholesterol, Dietary/administration & dosage , Dietary Fiber/analysis , Dietary Fiber/therapeutic use , Feces , Rats , Seaweed/metabolism , Seaweed/physiology , Ulva/metabolism , Ulva/physiologyABSTRACT
This work aims to assess the potential of the green seaweed Ulva fasciata Delile as an alternative source of dietary fibre (DF). Total DF content was determined, some of its physico-chemical properties described and the physiological effects of U. fasciata meal on rats fed a hypercholesterolemic diet were investigated. U. fasciata may be considered a potential alternative source of DF with a total content of about 400 g.kg-1 (dry basis) and interesting physico-chemical properties: water retention capacity of 8.74 g/water.g-1 dry sample (seaweed meal) and 0.90 (seaweed carbohydrate extract), lipid adsorption capacity of 4.52 g/oil.g-1 dry sample (seaweed meal) and 5.70 (seaweed carbohydrate extract), intrinsic viscosity of 2.4 dl.g-1 (seaweed carbohydrate extract) and cation exchange capacity of 3.51 Eq.kg-1 (seaweed carbohydrate extract). The diet containing seaweed meal was able to keep rats' total cholesterol (TC) down without causing any undesirable increase in LDL-C fraction. No evidence of toxic and/or antinutritional components in the seaweed meal was detected. Rats showed a fecal volume much greater (13 g) than that fed on cellulose diet ( 7 g) (p < 0.05). These properties confer on the seaweed the potential to be used in food technology for the acquisition of low-calorie food and might be important in body weight control, reduction of blood TC and LDL-C as well as in prevention of gastrointestinal diseases.
Este trabalho objetivou avaliar o potencial da alga marinha verde Ulva fasciata Delile como fonte alternativa de fibra alimentar. Foram realizadas a determinação do teor de fibra alimentar total e a descrição de algumas propriedades físico-químicas, e os efeitos fisiológicos da farinha da alga seca sobre ratos alimentados com dieta hipercolesterolemizante foram investigados. Esta alga pode ser considerada uma fonte alternativa potencial de fibra com cerca de 400 g.kg-1 (base seca) e propriedades físico-químicas interessantes: uma capacidade de retenção de água de 8,74 g/água.g-1 de amostra seca (farinha de alga) e 0,90 (extrato de carboidratos), uma capacidade de adsorção de lipídeos de 4,52 g/óleo.g-1 de amostra seca (farinha de alga) e 5,70 (extrato de carboidratos), uma viscosidade intrínseca de 2,4 dl.g-1 (extrato de carboidrato da alga) e capacidade de troca iônica de 3,51 Eq.kg-1 (extrato de carboidrato). A dieta contendo farinha de alga foi capaz de manter baixos os níveis de colesterol total de ratos sem causar aumento indesejável na fração LDL-C. Nenhuma evidência de componentes tóxicos e/ou antinutricionais na farinha de alga foi encontrada. Os ratos mostraram um volume fecal maior (13 g) do que aqueles alimentados com dieta contendo celulose como fonte de fibra (7 g) (p < 0,05). Essas propriedades conferem a alga o potencial de ser utilizada na tecnologia de alimentos para a aquisição de alimentos de baixas calorias, podendo ser importante para o controle do peso corporal, redução do colesterol sanguíneo total e da fração LDL-C, como também na prevenção de doenças gastrintestinais.
Subject(s)
Animals , Rats , Dietary Fiber/metabolism , Hypercholesterolemia/diet therapy , Lipids/blood , Seaweed/chemistry , Ulva/chemistry , Cholesterol, Dietary/administration & dosage , Dietary Fiber/analysis , Dietary Fiber/therapeutic use , Feces , Seaweed/metabolism , Seaweed/physiology , Ulva/metabolism , Ulva/physiologyABSTRACT
AIM: To evaluate ex vivo degradation of gutta-percha following six thermoplastic obturation techniques. METHODOLOGY: Ninety human-extracted mandibular premolars were selected and divided randomly into nine groups for filling. Group 1: thermomechanical compaction for 3 s with Konne gutta-percha points (Konne Ind. e Com. de Mat. Odontol., Belo Horizonte, MG, Brazil); Group 2: thermomechanical compaction for 3 s with Dentsply TP gutta-percha points (Dentsply Indústria e Comércio Ltda, Petrópolis, R.J. Brazil); Group 3: thermomechanical compaction for 10 s with Konne; Group 4: thermomechanical compaction for 10 s with Dentsply TP; Group 5: warm vertical condensation using System B (EIE/Analytic, Richmond, WA, USA) with Konne; Group 6: warm vertical condensation using System B with Dentsply TP; Group 7: vertical condensation with Konne; Group 8: vertical condensation with Dentsply TP; Group 9: Microseal cone (Analytic Endodontics, Glendora, CA, USA). A further four groups were assessed without using teeth, Group 10: Microseal microflow (Analytic Endodontics); Group 11: Obtura (Obtura Corporation, Penton, MO, USA); Group 12: Obtura flow (Obtura Corporation); Group 13: Thermafil (Dentsply Maillefer, Tulsa, OK, USA). The filling material was removed from the root canal and trans-1,4-polyisoprene isolated by solubilization of the root filling remnants in chloroform followed by filtration and centrifugation. By gel permeation chromatography and infrared spectroscopy, the occurrence and degree of degradation were assessed. The results were analysed statistically using the Kruskal-Wallis test. With differential scanning calorimetry, the thermal behaviour of the gutta-percha was determined. RESULTS: A significant decrease in polymer molar mass and the production of carboxyl and hydroxyl groups in the polymer were observed with thermomechanical compaction used for 10 s and vertical condensation filling techniques (P = 0.0001 and P = 0.0005, respectively). Other techniques caused no polymer degradation. CONCLUSION: Polyisoprene degrades with high temperature. Thermomechanical compaction for 10 s and vertical condensation were associated with the greatest degradative process.
Subject(s)
Gutta-Percha/chemistry , Root Canal Filling Materials/chemistry , Bicuspid , Calorimetry, Differential Scanning , Chromatography, Gel , Hemiterpenes/chemistry , Hot Temperature , Humans , Materials Testing , Molecular Weight , Root Canal Obturation , Spectroscopy, Fourier Transform Infrared , Statistics, NonparametricABSTRACT
AIM: To evaluate in vivo degradation of root filling materials over time. METHODOLOGY: Thirty-six root filled teeth with or without periapical lesions were selected. Teeth with poor coronal restoration were not included. The teeth had been root filled 3-30 years previous and were scheduled for conventional retreatment. The association of root canal treatment, age, periapical lesion and root filling degradation was investigated. The filling material was removed from the root canal using files and no solvent. Trans-1,4-polyisoprene was isolated through solubilization of root filling remnants in chloroform followed by filtration and centrifugation. Gel permeation chromatography (GPC) and infrared spectroscopy (FT-IR) were utilized to study the occurrence and degree of degradation. The GPC and FT-IR data were collected for each sample and analysed statistically using the Kruskal-Wallis test. RESULTS: Degradation of trans-1,4-polyisoprene was a slow process. The process was identified as an oxidation reaction through the production of carboxyl and hydroxyl groups. Compared with the control group, significant molar mass decrease was noted after 15 years (P = 0.0146) in teeth with no periapical lesions. However, in teeth associated with periapical lesions the number of years for significant degradation was reduced to 5 (P = 0.0009). CONCLUSION: Polyisoprene degrades inside root canals as an oxidative process. The presence of periapical lesions was associated with a more rapid onset of degradation.
Subject(s)
Butadienes/chemistry , Gutta-Percha/chemistry , Hemiterpenes/chemistry , Pentanes/chemistry , Root Canal Filling Materials/chemistry , Biotransformation , Chromatography, Gel , Dental Restoration Failure , Humans , Oxidation-Reduction , Periapical Periodontitis/therapy , Retreatment , Root Canal Obturation , Spectroscopy, Fourier Transform Infrared , Statistics, Nonparametric , Time FactorsABSTRACT
AIM: To compare the ability of five different commercially available gutta-percha points to fill simulated lateral canals when subjected to warm vertical compaction. METHODOLOGY: Fifty clear plastic teeth with a lateral canal in each third of the root were used. All teeth were filled using warm vertical compaction. Backfilling was completed with a sealer and the same gutta-percha point used during the apical condensation. After this, they were horizontally sectioned using a diamond disc adapted to a low-speed saw. The resulting sections were embedded in epoxy resin. The extent of gutta-percha and sealer filling were measured in each lateral canal using an IMAGE-PRO 4.0 software system. The voids in each canal were measured using the same system. Data were ranked and analysed using the Kruskal-Wallis statistical test. RESULTS: The mean percentage of the three lateral canals filled with gutta-percha and sealer were respectively: Konne (68.23% and 24.50%), Analytic (67.90% and 25.28%), Obtura (63.80% and 29.60%), Tanari (49.42% and 45.86%) and Dentsply (44.60% and 47.05%). There was significantly (P < 0.05) more gutta-percha in the lateral canal filled with Analytic, Obtura and Konne points than with Tanari and Dentsply points. CONCLUSIONS: The brand of gutta-percha cone had an influence on the length of filling within lateral canals. This may be a reflection of the chemical formulation of the gutta-percha points.
Subject(s)
Dental Pulp Cavity/anatomy & histology , Gutta-Percha/therapeutic use , Root Canal Filling Materials/therapeutic use , Gutta-Percha/chemistry , Humans , Image Processing, Computer-Assisted , Microscopy , Rheology , Root Canal Filling Materials/chemistry , Root Canal Obturation/methods , Surface PropertiesABSTRACT
Bryothamnion seaforthii, a red alga common to the Northeastern coast of Brazil, was used to prepare the protein fraction F0/60 by ammonium sulfate precipitation. The chromatography of F0/60 on DEAE-Sephadel column resulted in two lectin fractions, PI and PII, which have antinociceptive properties in rodents. We determined the antinociceptive activity of the PII fraction and of a carbohydrate-containing fraction (CF) in mice. The CF was prepared from the dried algae, after digestion with 100 mM sodium acetate, pH 6.0, containing 5 mM cysteine, EDTA and 0.4% papain, at 60 masculine C. A 10% cetylpyridinium chloride was added to the filtrate, and the precipitate was dissolved with 2 M NaCl:ethanol (100:15, v/v) followed by the carbohydrate precipitation with ethanol. The final precipitate, in acetone, was dried at 25 masculine C. The PII fraction markedly inhibited acetic acid-induced abdominal writhing after ip administration (control: 27.1 +/- 2.20; PII 0.1 mg/kg: 5.5 +/- 1.85; 1 mg/kg: 1.6 +/- 0.72 writhes/20 min) and after oral administration (control: 32.0 +/- 3.32; PII 0.1 mg/kg: 13.1 +/- 2.50; 1 mg/kg: 9.4 +/- 3.96 writhes/20 min). PII was also effective against both phases of pain induced by 1% formalin (control, ip: 48.2 +/- 2.40 and 27.7 +/- 2.56 s; PII: 1 mg/kg, ip: 34.3 +/- 5.13 and 5.6 +/- 2.14 s; control, po: 44.5 +/- 3.52 and 25.6 +/- 2.39 s; PII 5 mg/kg, po: 26.5 +/- 4.67 and 15.3 +/- 3.54 s for the 1st and 2nd phases, respectively) and in the hot-plate test. The CF (ip) also displayed significant antinociceptive properties in all tests but at higher doses (1 and 5 mg/kg, ip and po). Thus, CF at the dose of 5 mg/kg significantly inhibited writhes (ip: 7.1 +/- 2.47 and po: 14.5 +/- 2.40 writhes/20 min) as well as the 1st (po: 19.6 +/- 1.74 s) and 2nd (po: 7.1 +/- 2.24 s) phases of the formalin test compared to controls ip and po. The antinociceptive effects of both the PII and CF in the formalin and hot-plate tests were prevented at least partially by pretreatment with the opioid receptor antagonist naloxone (2 mg/kg, sc). Moreover, both fractions retained antinociceptive activity in the acetic acid-induced writhing test following heating, a procedure which abolished the hemagglutinating activity of the fraction, presumably due to lectins also present. Finally, both fractions also prolonged the barbiturate-induced sleeping time. These results indicate that carbohydrate molecules present in the PII (26.8% carbohydrate) and CF (21% of the alga dried weight) obtained from B. seaforthii display pronounced antinociceptive activity which is resistant to heat denaturation and is mediated by an opioid mechanism, as indicated by naloxone inhibition.
Subject(s)
Analgesics/pharmacology , Carbohydrates/pharmacology , Eukaryota/chemistry , Animals , Female , Male , Mice , Pain MeasurementABSTRACT
Bryothamnion seaforthii, a red alga common to the Northeastern coast of Brazil, was used to prepare the protein fraction F0/60 by ammonium sulfate precipitation. The chromatography of F0/60 on DEAE-Sephadel column resulted in two lectin fractions, PI and PII, which have antinociceptive properties in rodents. We determined the antinociceptive activity of the PII fraction and of a carbohydrate-containing fraction (CF) in mice. The CF was prepared from the dried algae, after digestion with 100 mM sodium acetate, pH 6.0, containing 5 mM cysteine, EDTA and 0.4 percent papain, at 60ºC. A 10 percent cetylpyridinium chloride was added to the filtrate, and the precipitate was dissolved with 2 M NaCl:ethanol (100:15, v/v) followed by the carbohydrate precipitation with ethanol. The final precipitate, in acetone, was dried at 25ºC. The PII fraction markedly inhibited acetic acid-induced abdominal writhing after ip administration (control: 27.1 ± 2.20; PII 0.1 mg/kg: 5.5 ± 1.85; 1 mg/kg: 1.6 ± 0.72 writhes/20 min) and after oral administration (control: 32.0 ± 3.32; PII 0.1 mg/kg: 13.1 ± 2.50; 1 mg/kg: 9.4 ± 3.96 writhes/20 min). PII was also effective against both phases of pain induced by 1 percent formalin (control, ip: 48.2 ± 2.40 and 27.7 ± 2.56 s; PII: 1 mg/kg, ip: 34.3 ± 5.13 and 5.6 ± 2.14 s; control, po: 44.5 ± 3.52 and 25.6 ± 2.39 s; PII 5 mg/kg, po: 26.5 ± 4.67 and 15.3 ± 3.54 s for the 1st and 2nd phases, respectively) and in the hot-plate test. The CF (ip) also displayed significant antinociceptive properties in all tests but at higher doses (1 and 5 mg/kg, ip and po). Thus, CF at the dose of 5 mg/kg significantly inhibited writhes (ip: 7.1 ± 2.47 and po: 14.5 ± 2.40 writhes/20 min) as well as the 1st (po: 19.6 ± 1.74 s) and 2nd (po: 7.1 ± 2.24 s) phases of the formalin test compared to controls ip and po. The antinociceptive effects of both the PII and CF in the formalin and hot-plate tests were prevented at least partially by pretreatment with the opioid receptor antagonist naloxone (2 mg/kg, sc). Moreover, both fractions retained antinociceptive activity in the acetic acid-induced writhing test following heating, a procedure which abolished the hemagglutinating activity of the fraction, presumably due to lectins also present. Finally, both fractions also prolonged the barbiturate-induced sleeping time...