ABSTRACT
The aim of this study was to develop a mixture of dimethacrylate isomers (PG6EMA) as a potential monomer for dental adhesives and composites. PG6EMA was synthesized de novo and characterized in the presence of ethanol (3%, 6% or 9%). BisGMA/TEGDMA (BTEG, 50/50 wt.%) was used as the resin control. Composites were formulated with 60 wt.% of either PG6EMA or BisGMA (40 wt.% TEGDMA and 70 wt.% filler). DMPA (0.2 wt.%) and DPI-PF6 (0.4 wt.%) were added as photoinitiators, irradiated with a mercury arc lamp (320-500 nm, 500 mW/cm2; Acticure). All materials were tested for polymerization kinetics (near-infrared), viscosity (η) and storage modulus (G', oscillatory rheometry). The composites were further characterized for water sorption/solubility, wet/dry flexural strength/modulus and polymerization stress. Data were analyzed with one-way ANOVA/Tukey's test (α = 0.05). The PG6EMA resins showed lower rates of polymerization compared with BTEG (p = 0.001) but high degrees of conversion (p = 0.002). Solvent concentration did not affect RPMAX but the 6% and 9% mixtures showed higher final DC, likely due to reduced viscosity. PG6EMA had much higher viscosity than BTEG (p <0.001) and lower G' (p = 0.003). Composites modified with PG6EMA have slower polymerization rates (p = 0.001) but higher final DC (p = 0.04) than the control. PG6EMA/TEGDMA showed lower dry/wet flexural strength and comparable dry modulus. The PG6EMA/TEGDMA composite showed a 18.4% polymerization stress reduction compared to the BTEG composite. Both base monomers had similar WS/SL and G'. Within its limitations, this study demonstrated that the newly synthesized PG6EMA was a viable alternative to BisGMA in dental composites.
Subject(s)
Bisphenol A-Glycidyl Methacrylate , Composite Resins , Materials Testing , Methacrylates , Polymerization , Polymethacrylic Acids , Composite Resins/chemistry , Composite Resins/radiation effects , Bisphenol A-Glycidyl Methacrylate/chemistry , Methacrylates/chemistry , Viscosity , Polymethacrylic Acids/chemistry , Analysis of Variance , Time Factors , Reproducibility of Results , Reference Values , Flexural Strength , Polyethylene Glycols/chemistry , Surface Properties , Solubility , Kinetics , Rheology , Dental Cements/chemistry , Light-Curing of Dental Adhesives/methodsABSTRACT
OBJECTIVES: To analyze the incorporation of cardanol trimethacrylate monomer (CTMA), derived from the cashew nut shell liquid, as a substitute for Bis-GMA in acrylic resins formulations and its effect on experimental resin composites' physicochemical and mechanical properties. MATERIALS AND METHODS: The intermediary cardanol epoxy was synthesized via cardanol epoxidation, followed by the synthesis of CTMA through methacrylic anhydride solvent-free esterification. Experimental resin composites were formulated with an organic matrix composed of Bis-GMA/TEGDMA (50/50 wt %) (control). CTMA was gradually added to replace different proportions of Bis-GMA: 10 wt % (CTMA-10), 20 wt % (CTMA-20), 40 wt % (CTMA-40), and 50 wt % (CTMA-50). The composites were characterized by degree of conversion, water sorption and solubility, viscosity, thermogravimetric analysis, dynamic mechanical analysis, flexural strength and elastic modulus. Data were analyzed with one-way ANOVA and Tukey's post-hoc test (α = 0.05), except for water sorption data, which were analyzed by Kruskall-Wallis and Dunn's method. RESULTS: CTMA-based and control composites did not show statistically significant differences regarding degree of conversion, flexural strength and elastic modulus. CTMA reduced the viscosity and solubility compared to the Bis-GMA-based composite. The CTMA-40 and CTMA-50 exhibited significantly lower water sorption compared to the control. Also, acceptable thermal stability and viscoelastic properties were obtained for safe use in the oral cavity. CONCLUSIONS: Incorporating CTMA into composites resulted in similar chemical and mechanical properties compared to Bis-GMA-based material while reducing viscosity, water sorption and solubility. CLINICAL RELEVANCE: CTMA could be used as a trimethacrylate monomer replacing Bis-GMA in resin composites, thereby minimizing BPA exposure.
Subject(s)
Bisphenol A-Glycidyl Methacrylate , Composite Resins , Flexural Strength , Materials Testing , Phenols , Polymethacrylic Acids , Solubility , Composite Resins/chemistry , Bisphenol A-Glycidyl Methacrylate/chemistry , Phenols/chemistry , Viscosity , Polymethacrylic Acids/chemistry , Elastic Modulus , Methacrylates/chemistry , Thermogravimetry , Polyethylene Glycols/chemistry , Anacardium/chemistryABSTRACT
This study aimed to assess the formation of nevirapine (NVP) co-amorphs systems (CAM) with different co-formers (lamivudine-3TC, citric acid-CAc, and urea) through combined screening techniques as computational and thermal studies, solubility studies; in addition to develop and characterize suitable NVP-CAM. NVP-CAM were obtained using the quench-cooling method, and characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), Fourier Transform Infrared Spectroscopy (FTIR), and polarized light microscopy (PLM), in addition to in vitro dissolution in pH 6.8. The screening results indicated intermolecular interactions occurring between NVP and 3TC; NVP and CAc, where shifts in the melting temperature of NVP were verified. The presence of CAc impacted the NVP equilibrium solubility, due to hydrogen bonds. DSC thermograms evidenced the reduction and shifting of the endothermic peaks of NVP in the presence of its co-formers, suggesting partial miscibility of the compounds. Amorphization was proven by XRD and PLM assays. In vitro dissolution study exhibited a significant increase in solubility and dissolution efficiency of NVP-CAM compared to free NVP. Combined use of screening studies was useful for the development of stable and amorphous NVP-CAM, with increased NVP solubility, making CAM promising systems for combined antiretroviral therapy.
Subject(s)
Calorimetry, Differential Scanning , Chemistry, Pharmaceutical , Nevirapine , Solubility , X-Ray Diffraction , Nevirapine/chemistry , Calorimetry, Differential Scanning/methods , X-Ray Diffraction/methods , Chemistry, Pharmaceutical/methods , Spectroscopy, Fourier Transform Infrared/methods , Drug Compounding/methods , Lamivudine/chemistry , Hydrogen Bonding , Anti-HIV Agents/chemistryABSTRACT
Triacontanol is a long-chain primary alcohol derived from policosanol, known for its diverse biological activities, including functioning as a plant growth regulator and exhibiting anti-inflammatory and antitumoral effects. However, its application is limited due to its high hydrophobicity, resulting in poor absorption and reduced therapeutic effectiveness. A potential solution to this problem is the use of niosomes. Niosomes are carriers composed of non-ionic surfactants, cholesterol, charge-inducing agents, and a hydration medium. They are effective in encapsulating drugs, improving their solubility and bioavailability. The objective of this study was to optimize and synthesize nano-niosomes for the encapsulation of triacontanol. Niosomes were synthesized using a thin-film hydration method combined with ultrasonication, following a Box-Behnken design. Niosomes were characterized using various techniques including dynamic light scattering, Fourier-transform infrared spectroscopy (FTIR), confocal microscopy, high-resolution scanning electron microscopy, and transmission electron microscopy (TEM). Formulation 14 of niosomes achieved the desired size, polydispersity index (0.198 ± 0.008), and zeta potential (-31.28 ± 1.21). FTIR analysis revealed a characteristic signal in the 3400-300 cm-1 range, indicating intermolecular interactions due to a bifurcated hydrogen bond between cholesterol and S60. Confocal microscopy confirmed the presence of triacontanol through Nile Red fluorescence. TEM revealed the spherical structure of niosomes.
Subject(s)
Fatty Alcohols , Liposomes , Liposomes/chemistry , Fatty Alcohols/chemistry , Particle Size , Spectroscopy, Fourier Transform Infrared , Nanoparticles/chemistry , Drug Carriers/chemistry , Solubility , Drug Compounding/methods , Cholesterol/chemistry , Surface-Active Agents/chemistryABSTRACT
OBJECTIVE: this study sought to evaluate the effect of isobornyl methacrylate (IBOMA) as a diluent monomer on the physicochemical properties of experimental flowable resin composites. METHODOLOGY: the organic resin matrix of a modal flowable resin composite was formulated with 50 wt.% of bisphenol-A-glycidyl methacrylate (Bis-GMA) and 50 wt.% of a diluent monomer, in which IBOMA was used as a combining or substituent diluent monomer to triethylene glycol dimethacrylate (TEGDMA). The resin matrices were filled with 55 wt.% particles, of which 10 wt.% was 0.05-µm fumed silica, and 45 wt.% was 0.7-µm BaBSiO2 glass. Polymerization shrinkage stress (PSS; n=10), degree of conversion (DC; n=3), maximum rate of polymerization (Rpmax; n=3), film thickness (FT; n=10), sorption (Wsp; n=10), solubility (Wsl; n=10), flexural strength (FS; n=10), flexural modulus (FM; n=10), Knoop microhardness (KH; n=10), and microhardness reduction after chemical softening (HR; n=10) were evaluated. Data were analyzed using one-way ANOVA, followed by Tukey's test (α=0.05; ß=0.2). RESULTS: the results showed that the substitution or addition of IBOMA reduced FT (p=0.001), PSS (p=0.013), Rpmax (p=0.001), DC (p=0.001), FM (p=0.006) Wsp (p=0.032), and Wsl (p=0.021). However, when used as a complete substituent, IBOMA demonstrated significantly lower FS (p=0.017) and KH (p=0.008), while TEGDMA demonstrated significantly lower HR (p=0.022). CONCLUSION: the flowable composite containing IBOMA combined with TEGDMA showed no effect in KH and FS and effectively reduced the PSS, RP, FT, Wsp, and Wsl. However, it showed a reduction in DC, FS, and an increase in HR.
Subject(s)
Bisphenol A-Glycidyl Methacrylate , Composite Resins , Flexural Strength , Materials Testing , Methacrylates , Polyethylene Glycols , Polymerization , Polymethacrylic Acids , Solubility , Surface Properties , Composite Resins/chemistry , Methacrylates/chemistry , Polymethacrylic Acids/chemistry , Polyethylene Glycols/chemistry , Bisphenol A-Glycidyl Methacrylate/chemistry , Analysis of Variance , Reproducibility of Results , Reference Values , Time Factors , Hardness Tests , Silicon Dioxide/chemistryABSTRACT
This study aimed to produce water-soluble oat extract enriched with mango peel flour (MPF) as a source of active compounds and to use this ingredient as a partial substitute for whole milk in Greek yogurt (GY) for its nutritional enrichment. Enriched water-soluble oat extracts (EWSOE) were produced with different concentrations of MPF (0%, 1%, 1.5% and 2%) and characterized in relation to pH, titratable acidity, soluble proteins and total phenolics. Three GY formulations were prepared by partially replacing whole milk with EWSOE and the best formulation (in relation to sensory analyzes and phenolics compounds) was selected for storage study, chemical characterization, and sensory acceptance testing. MPF addition increased soluble proteins and total phenolics in EWSOE. GY formulations prepared with EWSOE had similar sensory scores. During storage, GY prepared with EWSOE containing 2% MPF exhibited changes in pH and titratable acidity and a reduction in total phenolics. Color parameters, cholesterol, and fatty acid composition did not change over 21 days of storage. The major fatty acids in GY were oleic and palmitic acids. The selected product had low lactose content (1.2%), achieved satisfactory sensory acceptance in relation to the evaluated attributes, and had lipid (~6.19%) and protein (~3.96%) contents within regulatory requirements. Additionally, EWSOE is a valuable ingredient in GY preparation, offering beneficial nutritional and functional properties.
Subject(s)
Avena , Mangifera , Plant Extracts , Yogurt , Yogurt/analysis , Plant Extracts/chemistry , Plant Extracts/analysis , Mangifera/chemistry , Avena/chemistry , Flour/analysis , Hydrogen-Ion Concentration , Solubility , Water/chemistry , Water/analysis , Taste , Phenols/analysis , HumansABSTRACT
Glass ionomer cements (GICs) are the common materials employed in pediatric dentistry because of their specific applications in class I restorations and atraumatic restoration treatments (ART) of deciduous teeth in populations at high risk of caries. Studies show a limited clinical durability of these materials. Attempts have thus been made to incorporate nanoparticles (NPs) into the glass ionomer for improving resistance and make it like the tooth structure. An in vitro experimental study was conducted using the required samples dimensions and prepared based on the test being carried out on the three groups with or without the modification of light-cured glass ionomer. Samples were grouped as follows: control group (G1_C), 2% silver phosphate/hydroxyapatite NPs group (G2_SPH), and 2% titanium dioxide NPs group (G3_TiO2). The physical tests regarding flexural strength (n = 10 per group), solubility (n = 10 per group), and radiopacity (n = 3 per group) were performed. The data were analyzed by Shapiro Wilks test, and one-way analysis of variance (one-way ANOVA), and multiple comparisons by post hoc Tukey's test. The p-value of < 0.05 was considered significant. No statistically significant difference was observed between the control group (G1_C) and (G2_SPH) (p = 0.704) in the flexural strength test, however differences were found between G2_SPH and G3_TiO2 groups, ANOVA (p = 0.006); post hoc Tukey's test (p = 0.014). Pertaining to the solubility, G2_SPH obtained the lowest among the three groups, ANOVA (p = 0.010); post hoc Tukey's test (p = 0.009). The three study groups obtained an adequate radiopacity of >1 mm Al, respectively. The resin-modified glass ionomer cement (RMGIC) was further modified with 2% silver phosphate/hydroxyapatite NPs to improve the physical properties such as enhancing the solubility and sorption without compromising the flexural strength and radiopacity behavior of modified RMGIC. The incorporation of 2% titanium dioxide NPs did not improve the properties studied.
Subject(s)
Durapatite , Glass Ionomer Cements , Nanoparticles , Phosphates , Titanium , Titanium/chemistry , Glass Ionomer Cements/chemistry , Durapatite/chemistry , Nanoparticles/chemistry , Phosphates/chemistry , In Vitro Techniques , Materials Testing , Humans , Silver Compounds/chemistry , Solubility , Flexural StrengthABSTRACT
Fenbendazole is an antiparasitic drug widely used in veterinary medicine to treat parasitic infections caused in animals like cattle, horses, sheep, and dogs. Recently, it has been repositioned as a potential alternative for cancer treatment. However, it is a highly hydrophobic molecule (0.9 ug/mL), which can compromise its dissolution rate and absorption. Thus, this work aimed to apply a nanotechnological approach to improve drug solubility and dissolution performance. Fenbendazole nanoparticles stabilized by different poloxamers were obtained by lyophilization without cryoprotectants. The behavior of the drug in the solid state was analyzed by X-ray diffractometry, differential scanning calorimetry, and infrared spectroscopy. The nanosystems were also evaluated for solubility and dissolution rate. A long-term stability evaluation was performed for three years at room temperature. The yields of the lyophilization ranged between 75 and 81% for each lot. The nanoparticles showed a submicron size (< 340 nm) and a low polydispersity depending on the stabilizer. The physicochemical properties of the prepared systems indicated a remarkable amorphization of the drug, which influenced its solubility and dissolution performance. The drug dissolution from both the fresh and aged nanosystems was significantly higher than that of the raw drug. In particular, nanoparticles prepared with poloxamer 407 showed no significant modifications in their particle size in three years of storage. Physical stability studies indicated that the obtained systems prepared with P188, P237, and P407 suffered certain recrystallization during long storage at 25 °C. These findings confirm that selected poloxamers exhibited an important effect in formulating fenbendazole nanosystems with improved dissolution.
Subject(s)
Drug Stability , Fenbendazole , Freeze Drying , Nanoparticles , Solubility , Nanoparticles/chemistry , Fenbendazole/chemistry , Freeze Drying/methods , Calorimetry, Differential Scanning/methods , Drug Storage , Particle Size , X-Ray Diffraction/methods , Drug Liberation , Chemistry, Pharmaceutical/methods , Poloxamer/chemistry , Cryoprotective Agents/chemistryABSTRACT
Insoluble phosphorous compounds solubilization by soil bacteria is of great relevance since it puts available the phosphorus to be used by plants. The production of organic acids is the main microbiological mechanism by which insoluble inorganic phosphorus compounds are solubilized. In Gram negative bacteria, gluconic acid is synthesized by the activity of the holoenzyme glucose dehydrogenase-pyrroloquinoline quinine named GDH-PQQ. The use of marker genes is a very useful tool to evaluate the persistence of the introduced bacteria and allow to follow-up the effect of biotic and abiotic factors on these beneficial microorganisms in the soil. In previous studies we detected the presence of the pqqE gene in a great percentage of both non-culturable and culturable native soil bacteria. The objective of this study was to analyze the phylogeny of the sequence of pqqE gene and its potential for the study of phosphate solubilizing bacteria from pure and mixed bacterial cultures and rhizospheric soil samples. For this, the presence of the pqqE gene in the genome of phosphate solubilizing bacteria that belong to several bacteria was determined by PCR. Also, this gene was analyzed from mixed bacterial cultures and rhizospheric soil associated to peanut plants inoculated or not with phosphate solubilizing bacteria. For this, degenerate primers designed from several bacterial genera and specific primers for the genus Pseudomonas spp., designed in this study, were used. DNA template used from simple or mixed bacterial cultures and from rhizospheric soil samples was obtained using two different DNA extraction techniques. Results indicated that pqqE gene amplification product was found in the genome of all Gram negative phosphate solubilizing bacteria analyzed. It was possible to detect this gene in the DNA obtained from mixed cultures where these bacteria grew in interaction with other microorganisms and in that obtained from rhizospheric soil samples inoculated or not with these bacteria. The phylogenetic analysis indicated that pqqE gene is a conserved gene within related genera. In conclusion, pqqE gene could be a potential marker for the study of phosphate solubilizing bacterial populations.
Subject(s)
Phosphates , Phylogeny , Soil Microbiology , Phosphates/metabolism , Gram-Negative Bacteria/genetics , Gram-Negative Bacteria/isolation & purification , Gram-Negative Bacteria/classification , Solubility , Genetic Markers , Rhizosphere , Plants/microbiologyABSTRACT
This study assessed the physicochemical and antibiofilm properties of white mineral trioxide aggregate (MTA) associated with 1 or 2% of farnesol. Setting time was evaluated based on ISO 6876/2012. Radiopacity was evaluated by radiographic analysis. pH was assessed after time intervals of 1, 3, 7, 14, 21, and 28 days. Solubility (% mass loss) and volumetric change (by micro-CT) of the cements were evaluated after immersion in distilled water. The presence of voids inside the materials was assessed by using micro-CT. Antibiofilm activity against Enterococcus faecalis was evaluated by crystal violet assay and the modified direct contact test performed with biofilm previously formed on bovine root dentin for 14 days. Data were submitted to ANOVA/Tukey tests with 5% significance level. The incorporation of farnesol into MTA increased its setting time, but decreased its solubility at 30 days and its volumetric loss in all periods (p < 0.05). Radiopacity and solubility after 7 days were similar among the materials (p > 0.05). The association of farnesol showed the highest pH value after 1 and 3 days (p < 0.05). The association of farnesol with MTA promoted a decrease in the presence of voids, and increased the antimicrobial activity on biofilm biomass of E. faecalis (p < 0.05). In conclusion, the addition of farnesol can be suggested to improve the antimicrobial properties and the consistency of MTA.
Subject(s)
Aluminum Compounds , Biofilms , Calcium Compounds , Drug Combinations , Enterococcus faecalis , Farnesol , Materials Testing , Oxides , Root Canal Filling Materials , Silicates , Solubility , Silicates/pharmacology , Silicates/chemistry , Oxides/pharmacology , Oxides/chemistry , Biofilms/drug effects , Calcium Compounds/pharmacology , Calcium Compounds/chemistry , Enterococcus faecalis/drug effects , Aluminum Compounds/pharmacology , Aluminum Compounds/chemistry , Farnesol/pharmacology , Farnesol/chemistry , Hydrogen-Ion Concentration , Time Factors , Cattle , Root Canal Filling Materials/pharmacology , Root Canal Filling Materials/chemistry , Animals , Analysis of Variance , Reproducibility of Results , Dentin/drug effects , Reference Values , Surface Properties/drug effectsABSTRACT
Aim: Benznidazole (BNZ), a class-II drug, is the primary treatment for Chagas disease, but its low aqueous solubility presents challenges in formulation and efficacy. Nanosuspensions (NS) could potentially address these issues.Methods: BNZ-NS were prepared using a simple, organic solvents-free nano-milling approach. Physicochemical characterizations were conducted on both NS and lyophilized solid-state BNZ-nanocrystals (NC).Results: BNZ-NS exhibited particle size <500 nm, an acceptable polydispersity index (0.23), high Z-potential, and physical stability for at least 90 days. BNZ-NC showed tenfold higher solubility than pure BNZ. Dissolution assays revealed rapid BNZ-NS dissolution. BNZ-NC demonstrated biocompatibility on an eukaryotic cell and enhanced BNZ efficacy against trypomastigotes of Trypanosoma cruzi.Conclusion: BNZ-NS offers a promising alternative, overcoming limitations associated with BNZ for optimized pharmacotherapy.
[Box: see text].
Subject(s)
Chagas Disease , Nanoparticles , Nitroimidazoles , Particle Size , Solubility , Trypanocidal Agents , Trypanosoma cruzi , Nitroimidazoles/chemistry , Nitroimidazoles/administration & dosage , Chagas Disease/drug therapy , Trypanosoma cruzi/drug effects , Nanoparticles/chemistry , Trypanocidal Agents/administration & dosage , Trypanocidal Agents/chemistry , Trypanocidal Agents/pharmacology , Animals , Humans , Suspensions , Drug Stability , Chemistry, Pharmaceutical/methods , Solvents/chemistry , Freeze DryingABSTRACT
Bacteria can solubilize phosphorus (P) through the secretion of low-molecular-weight organic acids and acidification. However, the genes involved in the production of these organic acids are poorly understood. The objectives of this study were to verify the calcium phosphate solubilization and the production of low-molecular-weight organic acids by diverse genera of phosphate solubilizing bacterial strains (PSBS); to identify the genes related to the synthesis of the organic acids in the genomes of these strains and; to evaluate growth and nutrient accumulation of maize plants inoculated with PSBS and fertilized with Bayóvar rock phosphate. Genomic DNA was extracted for strain identification and annotation of genes related to the organic acids production. A greenhouse experiment was performed with five strains plus 150 mg dm- 3 P2O5 as Bayóvar rock phosphate (BRP) to assess phosphate solubilization contribution to maize growth and nutrition. Paraburkholderia fungorum UFLA 04-21 and Pseudomonas anuradhapurensis UFPI B5-8A solubilized over 60% of Ca phosphate and produced high amounts of citric/maleic and gluconic acids in vitro, respectively. Eleven organic acids were identified in total, although not all strains produced all acids. Besides, enzymes related to the organic acids production were found in all bacterial genomes. Plants inoculated with strains UFPI B5-6 (Enterobacter bugandensis), UFPI B5-8A, and UFLA 03-10 (Paenibacillus peoriae) accumulated more biomass than the plants fertilized with BRP only. Strains UFLA 03-10 and UFPI B5-8A increased the accumulation of most macronutrients, including P. Collectively, the results show that PSBS can increase maize growth and nutrient accumulation based on Bayóvar rock phosphate fertilization.
Subject(s)
Bacteria , Phosphates , Zea mays , Zea mays/growth & development , Zea mays/microbiology , Zea mays/metabolism , Phosphates/metabolism , Bacteria/genetics , Bacteria/metabolism , Bacteria/classification , Calcium Phosphates/metabolism , Soil Microbiology , Genome, Bacterial , Plant Development , Solubility , Gluconates/metabolism , Genomics , Phosphorus/metabolism , PhylogenyABSTRACT
Legumes are abundant sources of proteins, and white common bean proteins play an important role in air-water interface properties. This study aims to investigate the technical-functional properties of white common bean protein isolate (BPI) as a function of pH, protein concentration, and guar gum (GG) presence. BPI physicochemical properties were analyzed in terms of solubility, zeta potential, and mean particle diameter at pH ranging from 2 to 9, in addition to water-holding capacity (WHC), oil-holding capacity (OHC), and thermogravimetric analysis. Protein dispersions were evaluated in terms of dynamic, interfacial, and foam-forming properties. BPI showed higher solubility (>80 %) at pH 2 and above 7. Zeta potential and mean diameter ranged from 15.43 to -34.08 mV and from 129.55 to 139.90 nm, respectively. BPI exhibited WHC and OHC of 1.37 and 4.97 g/g, respectively. Thermograms indicated decomposition temperature (295.81 °C) and mass loss (64.73 %). Flow curves indicated pseudoplastic behavior, with higher η100 values observed in treatments containing guar gum. The behavior was predominantly viscous (tg δ > 1) at lower frequencies, at all pH levels, shifting to predominantly elastic at higher frequencies. Equilibrium surface tension (γeq) ranged from 43.87 to 41.95 mN.m-1 and did not decrease with increasing protein concentration under all pH conditions. All treatments exhibited Ï < 15°, indicating predominantly elastic surface films. Foaming properties were influenced by higher protein concentration and guar gum addition, and the potential formation of protein-polysaccharide complexes favored the kinetic stability of the system.
Subject(s)
Galactans , Mannans , Phaseolus , Plant Gums , Plant Proteins , Solubility , Surface Properties , Plant Gums/chemistry , Galactans/chemistry , Mannans/chemistry , Hydrogen-Ion Concentration , Plant Proteins/chemistry , Phaseolus/chemistry , Particle Size , Water/chemistryABSTRACT
This study demonstrates the application of Langmuir and Langmuir-Blodgett films as biomimetic drug reservoirs and delivery systems to investigate the effect of an anthelmintic on cancer cell culture. The repurposing of benzimidazole anthelmintics for cancer therapy due to their microtubule-inhibiting properties has gained attention, showing promising anticancer effects and tumor-suppressive properties. Although widely used in medicine, the low aqueous solubility of benzimidazole compounds poses challenges for studying their effects on cancer cells, requiring incorporation into various formulations. Our study demonstrates that incorporating albendazole into stable Palmitic Acid Langmuir monolayers, forming Langmuir-Blodgett films, significantly affects the proliferation of liver carcinoma cells. This report presents the initial findings of the effect of an antitumoral drug on cancer cell culture using a simple and repeatable methodology.
Subject(s)
Albendazole , Antineoplastic Agents , Cell Proliferation , Drug Delivery Systems , Albendazole/chemistry , Albendazole/administration & dosage , Albendazole/pharmacology , Humans , Drug Delivery Systems/methods , Antineoplastic Agents/chemistry , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/pharmacology , Cell Proliferation/drug effects , Hep G2 Cells , Cell Line, Tumor , Anthelmintics/chemistry , Anthelmintics/administration & dosage , Anthelmintics/pharmacology , Solubility , Surface PropertiesABSTRACT
The present study utilizes molecular dynamics simulations to examine how different anions compete for protein solvation in aqueous solutions of ionic liquids (ILs). Ubiquitin is used as model protein and studied in IL mixtures sharing the same cation, 1-ethyl-3-methylimidazolium (EMIM), and two different anions in the same solution, from combinations of dicyanamide (DCA), chloride (Cl), nitrate (NO3), and tetrafluoroborate (BF4). Our findings reveal that specific interactions between anions and the protein are paramount in IL solvation, but that combinations of anions are not additive. For example, DCA exhibits a remarkable ability to form hydrogen bonds with the protein, resulting in a significantly stronger preferential binding to the protein than other anions. However, the combination of DCA with NO3, which also forms hydrogen bonds with the protein, results in a smaller preferential solvation of the protein than the combination of DCA with chloride ions, which are weaker binders. Thus, combining anions with varying affinities for the protein surface modulates the overall ion accumulation through nonadditive mechanisms, highlighting the importance of the understanding of competition for specific interaction sites, cooperative binding, bulk-solution affinity, and overall charge compensations, on the overall solvation capacity of the solution. Such knowledge may allow for the design of novel IL-based processes in biotechnology and material science, where fine-tuning protein solvation is crucial for optimizing performance and functionality.
Subject(s)
Anions , Ionic Liquids , Molecular Dynamics Simulation , Water , Ionic Liquids/chemistry , Anions/chemistry , Water/chemistry , Ubiquitin/chemistry , Hydrogen Bonding , Solubility , Imidazoles/chemistryABSTRACT
Moisture activated dry granulation (MADG) is an attractive granulation process. However, only a few works have explored modified drug release achieved by MADG, and to the best of the authors knowledge, none of them have explored gastroretention. The aim of this study was to explore the applicability of MADG process for developing gastroretentive placebo tablets, aided by SeDeM diagram. Floating and swelling capacities have been identified as critical quality attributes (CQAs). After a formulation screening step, the type and concentration of floating matrix formers and of binders were identified as the most relevant critical material attributes (CMAs) to investigate in ten formulations. A multiple linear regression analysis (MLRA) was applied against the factors that were varied to find the design space. An optimized product based on principal component analysis (PCA) results and MLRA was prepared and characterized. The granulate was also assessed by SeDeM. In conclusion, granulates lead to floating tablets with short floating lag time (<2 min), long floating duration (>4 h), and showing good swelling characteristics. The results obtained so far are promising enough to consider MADG as an advantageous granulation method to obtain gastroretentive tablets or even other controlled delivery systems requiring a relatively high content of absorbent materials in their composition.
Subject(s)
Chemistry, Pharmaceutical , Drug Compounding , Drug Liberation , Excipients , Tablets , Drug Compounding/methods , Chemistry, Pharmaceutical/methods , Excipients/chemistry , Delayed-Action Preparations , Solubility , Water/chemistry , Principal Component AnalysisABSTRACT
The present study examined different concentrations of the butylated hydroxytoluene (BHT) inhibitor on the kinetics of conversion, polymerization shrinkage stress, and other correlated physicochemical properties of experimental resin composites (ERC). A model composite was formulated with 75 wt% filler containing 0.5 wt% camphorquinone and 1 wt% amine with BHT concentrations of 0.01 wt% (BHT-0.01); 0.1 wt% (BHT-0.1); 0.25 wt% (BHT-0.25); 0.5 wt% (BHT-0.5); 1 wt% (BHT-1), and control (no BHT). They were tested on polymerization shrinkage stress (PSS; n = 5), degree of conversion (DC; n = 3), maximum polymerization rate (RpMAX; n = 5), water sorption (Wsp; n = 0), and solubility (Wsl; n = 10), flexural strength (FS; n = 10), flexural modulus (FM; n = 10), Knoop microhardness (KH; n = 10), and microhardness reduction (HR; n = 10). Data concerning these tests were submitted to one-way ANOVA and Tukey's test (α = 0.05; ß = 0.2). BHT-0.25, BHT-0.5, and BHT-1 showed a gradually significant decrease in PSS (p = 0.037); however, BHT-1 demonstrated a decrease in the physicochemical properties tested. Thus, within the limitations of this study, it was possible to conclude that BHT concentrations between 0.25 and 0.5 wt% are optimal for reducing shrinkage stress without affecting other physicochemical properties of ERCs.
Subject(s)
Butylated Hydroxytoluene , Composite Resins , Materials Testing , Polymerization , Stress, Mechanical , Butylated Hydroxytoluene/chemistry , Composite Resins/chemistry , Chemical Phenomena , Solubility , Water/chemistry , HardnessABSTRACT
This study evaluated the setting time, pH, calcium ion release, solubility, and chemical structure of four calcium silicate sealers after ultrasonic activation (UA). Five sealers were evaluated: Sealer Plus (SP - control); Sealer Plus BC (SPBC), Bio C Sealers (BCS), Endosequence BC Sealer (EBC), and BioRoot RCS (BR). Ten groups were created based on the use or not of ultrasonic activation: SP; SP/UA; SPBC; SPBC/UA; BCS; BCS/UA; EBC; EBC/UA; BR; and BR/UA. Setting time was performed based on ISO 6876:2012 and ASTM C266-07 specifications. Solubility at 24hs, based on ISO 6876:2012. pH and calcium release were evaluated at 1, 24, 72, and 168hs. Raman spectroscopy was used to evaluate structural changes. Quantitative data were analyzed using One-Way ANOVA and Tukey post-hoc test (α=5%). Raman spectroscopy results were qualitatively analyzed. Setting times and solubility of all sealers were not affected by UA (p>0.05). The highest solubility was found for BCS, BCS/UA; and BR, BR/UA (p<0.05). After 24hs, calcium silicate sealers had higher pH than SP and SP/UA (p<0.05). BR and BR/UA had the highest pH at all time points. SP and SP/UA had stable pH at all time points. SP and SP/UA had the lowest calcium release values at all time points (p<0.05). EBC and EBC/UA calcium release significantly differ at 24,72 and 168hs (p<0.05). No chemical changes were observed during Raman spectroscopy. In conclusion, ultrasonic activation affected calcium ion release only for EndoSequence BC Sealer. Ultrasonic activation did not influence the initial and final setting time, solubility, pH, and chemical structure of any investigated sealers.
Subject(s)
Calcium Compounds , Calcium , Root Canal Filling Materials , Silicates , Solubility , Hydrogen-Ion Concentration , Silicates/chemistry , Calcium Compounds/chemistry , Calcium/chemistry , Root Canal Filling Materials/chemistry , Ultrasonics , Spectrum Analysis, RamanABSTRACT
3D printing technology is revolutionizing pharmaceuticals, offering tailored solutions for solid dosage forms. This innovation is particularly significant for conditions like Chagas disease, which require weight-dependent treatments. In this work, a formulation of benznidazole (BNZ), the primary treatment for this infection, was developed to be utilized with the Melting Solidification Printing Process (MESO-PP) 3D printing technique. Considering the limited aqueous solubility of BNZ, an interpolyelectrolyte complex (IPEC), composed of chitosan and pectin, was integrated to improve its dissolution profile. The formulations, also called inks in this context, with and without IPEC were integrally characterized and compared. The printing process was studied, the release of BNZ from 3D-prints (3DP) was exhaustively analyzed and a physiologically based pharmacokinetic model (PKPB) was developed to forecast their pharmacokinetic performance. 3DP were successfully achieved loading 25, 50 and 100 mg of BNZ. The presence of the IPEC in the ink caused a decrease in the crystalline domain of BNZ and facilitated the printing process, reaching a print success rate of 83.3 %. Interestingly, 3DP-IPEC showed accelerated release dissolution profiles, releasing over 85 % of BNZ in 90 min, while 3DP took up to 48 h for doses above 25 mg. The PBPK model demonstrated that 3DP-IPEC tablets would present high bioavailability (0.92), higher than 3DP (0.36) and similar to the commercial product. This breakthrough holds immense potential for improving treatment outcomes for neglected diseases.
Subject(s)
Chagas Disease , Drug Liberation , Nitroimidazoles , Printing, Three-Dimensional , Tablets , Trypanocidal Agents , Nitroimidazoles/chemistry , Nitroimidazoles/administration & dosage , Nitroimidazoles/pharmacokinetics , Chagas Disease/drug therapy , Trypanocidal Agents/chemistry , Trypanocidal Agents/administration & dosage , Trypanocidal Agents/pharmacokinetics , Solubility , Chitosan/chemistry , Precision Medicine/methods , Drug Compounding/methods , Chemistry, Pharmaceutical/methodsABSTRACT
Acne affects most of the world's population, causing an impact on the self-esteem of adolescents and young adults. One of the causes is the presence of the bacteria Cutibacterium acnes which are part of the natural microbiota of the skin. Topical treatments consist of anti-inflammatory and antibiotics, which could select resistant strains. Alternatives to the antibiotic are biocomposites that have antimicrobial activity like biosurfactants which are produced by bacteria. An innovative way of applying these compounds is bioadhesive polymeric films that adhere to the skin and release the active principle topically. Rhamnolipids have great potential to be used in the treatment of acne because they present antimicrobial activity against C. acnes in low and safe concentrations (MIC of 15.62 µg/mL, CBM of 31.25 µg/mL and CC50 of 181.93 µg/mL). Four films with different rhamnolipids concentrations (0.0; 0.1; 0.2; and 0.3%, w/w) were obtained as to visual appearance, mass variation, thickness, density, solubility, pH, water vapor transmission, mechanical properties (folding endurance, bioadhesion strength, tensile strength, elongation at break and Young's modulus), scanning electron microscopy and infrared. The results show that these formulations had a homogeneous appearance; elastic mechanical properties; pH similar to human skin and bioadhesive. The polymeric films containing rhamnolipids were effective against C. acnes, in the in vitro test, at the three concentrations tested, the film with the highest concentration (0.3%, w/w) being the most promising for presenting the highest antimicrobial activity. Thus, the polymeric film containing rhamnolipids has the potential to be used in the treatment of acne.