Mixture Of PEG Research Articles

Optimization of Soursop (Annona muricata L.) Leaf Extract in Nanoemulgel and Antiacnes Activity Test Against Propionibacterium acnes, Staphylococcus aureus, Staphylococcus epidermidis Bacteria

Soursop leaf extract (Annona muricata L.) has antibacterial activity with active components of alkaloids, flavonoids, steroids, and saponins. This research aims to optimize the use of VCO, Tween 80, and PEG 400 in the nanoemulsion system, which will be added Carbopol 940 as a gelling agent to form a nanoemulgel and to determine antibacterial activity. By utilizing the simplex lattice design method in Design Expert 13.0, the nanoemulsion formula has been successfully optimized involving a mixture of VCO, Tween 80, and PEG 400. A total of 14 different nanoemulsion formulas were produced through this process. The process of making nanoemulsion is carried out by mixing extracts, oils, surfactants and cosurfactants, homogenized using a vortex, then sonicated. Evaluation of % transmittance, emulsification time, and pH were carried out to determine nanoemulsion physical properties. The nanoemulsion optimal formula was evaluated for particle size, polydispersity index, and zeta potential and made into nanoemulgel with the addition of Carbopol 940. The optimal formula has a composition of 10.86% VCO, 67.33% Tween 80, 21.81% PEG 400 form homogeneous and clear nanoemulsion with % transmittance of 91.97±1.11%, emulsification time of 56.42±0.72 seconds, and pH of 5.67±0.24. Particle size, polydispersity index, and zeta potential of the optimal formula were 229.47±38.79 nm, 0.41±0.10, and -39.13±0.19 mV, respectively. Evaluation of nanoemulgel physical properties showed homogeneous, pH value of 5.83±0.24, spreadability of 5.57±0.25 cm, adhesive force of 3.80±0.25 seconds, viscosity of 11479.33±167.49 cP, antibacterial activity against P. acnes, Staphylococcus aureus, and Staphylococcus epidermidis with inhibition zone diameters of 9.67±0.47 mm, 7.33±0.47 mm, and 5.67±0.47 mm. respectively. Nanoemulgel soursop leaf extract has suitable physical properties, and antibacterial activity is in the medium category.

The impact of polymer mixture composition on the properties of electrospun membranes for drug delivery applications

Orally dispersible films (ODFs) prepared by an electrospinning are a novel type of pharmaceutical formulation. This dosage form has the potential to be beneficial for small children and the elderly, who can have problems with administration of classical tablets due to the increased risk of choking and difficulty with swallowing. Due to the highly porous nanofiber morphology, the ODFs examined in this study achieve rapid disintegration into drug microparticles when in contact with saliva. The suspension is then easier to swallow. In this study, we focus on the impact of film composition (polymer matrix composition) on the properties of electrospun membranes. In particular, we prepared ODFs composed of a mixture of PEG 100 000 with HPMC E5 and PVP k90 with HPMC E5. We found significant differences in the structure of electrospinned membranes, where samples containing PEG 100 000 and HPMC E5 exhibited much narrower distribution of fibers. Furthermore, nanofibers containing PVP k90 exhibit a faster disintegration rate, while dissolution of the drug was faster in the case of PEG 100 000 containing ODFs. The improvement was caused by both the structure and composition of the membranes.

Enzymatic post-crosslinking of printed hydrogels of methacrylated gelatin and tyramine-conjugated 8-arm poly(ethylene glycol) to prepare interpenetrating 3D network structures.

Methacrylated gelatin (GelMA) has been intensively studied as a 3D printable scaffold material in tissue regeneration fields, which can be attributed to its well-known biological functions. However, the long-term stability of photo-crosslinked GelMA scaffolds is hampered by a combination of its fast degradation in the presence of collagenase and the loss of physical crosslinks at higher temperatures. To increase the longer-term shape stability of printed scaffolds, a mixture of GelMA and tyramine-conjugated 8-arm PEG (8PEGTA) was used to create filaments composed of an interpenetrating network (IPN). Photo-crosslinking during filament deposition of the GelMA and subsequent enzymatic crosslinking of the 8PEGTA were applied to the printed 3D scaffolds. Although both crosslinking mechanisms are radical based, they operate without interference of each other. Rheological data of bulk hydrogels showed that the IPN was an elastic hydrogel, having a storage modulus of 6 kPa, independent of temperature in the range of 10 - 40°C. Tensile and compression moduli were 110 kPa and 80 kPa, respectively. On enzymatic degradation in the presence of collagenase, the gelatin content of the IPN fully degraded in 7 days, leaving a stable secondary crosslinked 8PEGTA network. Using a BioMaker bioprinter, hydrogels without and with human osteosarcoma cells (hMG-63) were printed. On culturing for 21 days, hMG-63 in the GelMA/8PEGTA IPN showed a high cell viability (>90%). Thus, the presence of the photoinitiator, incubation with H2O2, and mechanical forces during printing did not hamper cell viability. This study shows that the GelMA/8PEGTA ink is a good candidate to generate cell-laden bioinks for extrusion-based printing of constructs for tissue engineering applications.

Aqueous two-phase extraction: A non-thermal technique to separate and concentrate betalains from Bougainvillea glabra Choisy bracts

The purple bracts of Bougainvillea glabra Choisy contain betalains that can be used as pigmenting agents. The objective was to evaluate the use of aqueous two-phase extraction systems to separate betalains from B. glabra bracts in order to improve the potential of this species as a source of natural pigments. A binodal phase diagram for the mixture of polyethylene glycol 4000 (PEG 4000) and trisodium citrate (Na3Cit; Na3C6H5O7) was studied to select betalain extraction conditions. The separation and concentration of betalains was evaluated and the feasibility of partitioning into betacyanins and betaxanthins was assessed. Mixtures of Na3Cit and PEG 4000 were prepared with concentrations in the ranges of 3.02–39.69% and 0.28–36.98%, respectively, and formed aqueous biphasic systems, with top phases composed mainly by PEG 4000 and bottom phases composed mainly by Na3Cit. The betalains showed a tendency to migrate towards the top phase, with an average separation yield of 92.41% and a concentration of 176.57 mg/L, while in the bottom phase an average content of 4.53 mg/L was found. Such situation was caused by a salting-out phenomenon and by a non-thermal concentration of compounds given by a reduction of the volume ratio between phases. The partition coefficient varied between 18.95 and 183.4 in betacyanins (Bc) and between 6.85 and 80.0 in betaxanthins (Bx). The Bc/Bx ratio varied between 2.82 and 3.26 in top phases and between 1.26 and 1.45 in bottom phases. The use of aqueous two-phase extraction systems allowed betalains to be separated and concentrated, although only a partial partitioning of Bc and Bx was achieved.

Enhanced Transdermal Delivery of Acyclovir via Hydrogel Microneedle Arrays

Hydrogel microneedles represent a promising approach to deliver drug molecules across skin into systemic circulation in a sustained release manner and without any polymer residue within skin. Acyclovir is an antiviral drug used for the treatment of several viral infections. However, the oral administration of acyclovir may cause gastrointestinal tract (GIT) disturbances with low bioavailability and poor patient compliance due to its requirement of five daily administrations to produce the desired effect. Therefore, it is thought that the preparation of hydrogel microneedle arrays containing acyclovir would improve the bioavailability and patient compliance by reducing the frequency of administration to once daily as well as overcome the GIT side effects associated with oral administration. A mixture of PEG 10,000 Da and PMVE/MA co-polymer 1,980,000 Da at a ratio of 1:3 (7.5%:22.5% w/w) with Na2CO3 3% w/w was found to produce the optimum hydrogel microneedle array formulation (F8) which showed suitable needle formation with an appropriate mechanical strength and excellent insertion ability, high drug content, sufficient swelling property and a sustained drug release over a period of 24 hours. The Ex vivo permeation study across human skin has demonstrated that the permeation of acyclovir from F8 hydrogel microneedle array was significantly (P≤ 0.05) increased by 39 times in comparison with microneedle-free film (control). The microneedle array has delivered 75.56% ± 4.2 of its loading dose over 24 hours, while the control film was only able to deliver 1.94% ± 0.14 of the total loading dose during the same period. Accordingly, these findings propose the potential application of hydrogel microneedle arrays for the transdermal delivery of acyclovir in a sustained release manner over 24 hours.

The Influence of the Polymer Type on the Quality of Newly Developed Oral Immediate-Release Tablets Containing Amiodarone Solid Dispersions Obtained by Hot-Melt Extrusion.

The present study aims to demonstrate the influence of the polymer-carrier type and proportion on the quality performance of newly developed oral immediate-release tablets containing amiodarone solid dispersions obtained by hot-melt extrusion. Twelve solid dispersions including amiodarone and different polymers (PEG 1500, PEG 4000; PEG 8000, Soluplus®, and Kolliphor® 188) were developed and prepared by hot-melt extrusion using a horizontal extruder realized by the authors in their own laboratory. Only eleven of the dispersions presented suitable physical characteristics and they were used as active ingredients in eleven tablet formulations that contain the same amounts of the same excipients, varying only in solid dispersion type. The solid dispersions’ properties were established by optical microscopy with reflected light, volumetric controls and particle size evaluation. In order to prove that the complex powders have appropriate physical characteristics for the direct compression process, they were subjected to different analyses regarding their flowability and compressibility behavior. Additionally, the Fourier transform infrared spectroscopy and X-ray diffraction analysis were performed on the obtained solid dispersions. After confirming the proper physical attributes for all blends, they were processed into the form of tablets by direct compression technology. The manufactured tablets were evaluated for pharmacotechnical (dimensions–diameter and thickness, mass uniformity, hardness and friability) and in vitro biopharmaceutical (disintegration time and drug release) performances. Furthermore, the influence of the polymer matrix on their quality was determined. The high differences in flow and compression performances of the solid dispersions prove the relevant influence of the polymer type and their concentration-dependent plasticizing properties. The increase in flowability and compressibility characteristics of the solid dispersions could be noticed after combining them with direct compression excipients owning superior mechanical qualities. The influence of the polymer type is best detected in the disintegration test, where the obtained values are quite different between the studied formulations. The use of PEG 1500 alone or combined in various proportions with Soluplus® leads to rapid disintegration. In contrast, the mixture of PEG 4000 and Poloxamer 188 in equal proportions determined the increase in disintegration time to 120 s. The use of Poloxamer 188 alone and a 3:1 combination of PEG 4000 and Soluplus® also generates a prolonged disintegration time for the tablets.

Andrographolide Liquisolid using Porous-Starch as the Adsorbent with Enhanced Oral Bioavailability in Rats

Andrographolide (AGL) is the major component of Andrographispaniculata. The poor water solubility and low dissolution strongly affect its oral absorption. Liquisolid technology has been used to improve its dissolution and oral bioavailability. Liquisolid powders of AGL (AGL-LS-PSG) were obtained by firstly dissolving AGL in the mixture of NMP, PEG 6000 and Soluplus®, and solidified by absorption of the blend in porous starch. Angle of repose, Carr index and Hauser ratio presented good powder fluidity and compressibility characteristics of AGL-LS-PSG. The results of optical microscopic observation, PXRD and DSC analysis indicated that AGL has been completely adsorbed in porous starch granules and existed in an amorphous or molecularly dispersing state. AGL-LS-PSG can obviously increase the drug dissolution rate compared to commercial guttate pills and raw drug. In vivo pharmacokinetic behavior of AGL-LS-PSG was investigated following a single oral administration to rats. The Cmax (0.37 ± 0.06 μg mL−1) and AUC0−2h (13.55 ± 2.67 μg h mL−1) of AGL-LS-PSG were evidently increased compared to commercial guttate pills (Cmax = 0.30 ± 0.21 μg mL−1, AUC0–2h = 9.88 ± 3.57 μg h mL−1). This study indicated great potential of liquisolid technology in effectively improving the dissolution and bioavailability of AGL.

PBT/adipic acid modified PEG solid-solid phase change composites

The complicated preparation process and difficulty of recycling were serious obstacles to the widespread use of solid-solid phase change materials (PCMs). Herein, we reported a novel thermoplastic solid-solid PCMs prepared by a facile one-step feeding method. In this study, the esterification and transesterification among the molten mixture of PBT, PEG and adipic acid were conducted to prepare thermoplastic PEG/PBT/Adipic acid copolymer-based PCMs. Adipic acid, as an auxiliary encapsulation agent, could prevent effectively PEG leakage of PEG/PBT/Adipic acid copolymer-based PCMs with high PEG and low PBT content during the phase change process. For PCM-6 containing 91 wt% PEG, 8 wt% PBT and 1 wt% adipic acid, there were no changes in the shape and chemical structure after multiple thermal cycles. The TG results presented that the initial thermal degradation temperature of PCMs-6 was above 200 °C, which was much higher than the processing and working temperature of PCMs-6. The latent heat of PCMs-6 could reach 136.8 J/g, showing great potential for energy storage, especially in the field of green buildings.

A promising patterned mesoscopic CuInS2 solar cell

Bulk heterojunction (BHJ) film is potential for the solar cells based on the photon-absorbers with a limited charge diffusion length. Here, for the first time, a patterned mesoporous film featuring the voids surrounded by the mesoporous walls of TiO2 nanoparticles is created for loading CuInS2 nanoparticles to prepare CuInS2-based BHJ film, resulting in a patterned mesoscopic CuInS2 solar cell with an efficiency of 6.23%. The voids are derived from the phase-separated poly (ethylene glycol) (PEG) aggregates during spin-casting the mixture of TiO2 slurry and PEG. It is demonstrated that the patterned mesoscopic CuInS2 solar cell is much more efficient than conventional/non-patterned counterpart device.

Multichromatic near-infrared imaging to assess interstitial lymphatic and venous uptake in vivo.

.Significance: Changes in interstitial fluid clearance are implicated in many diseases. Using near-infrared (NIR) imaging with properly sized tracers could enhance our understanding of how venous and lymphatic drainage are involved in disease progression or enhance drug delivery strategies.Aim: We investigated multichromatic NIR imaging with multiple tracers to assess in vivo microvascular clearance kinetics and pathways in different tissue spaces.Approach: We used a chemically inert IR Dye 800CW (D800) to target venous capillaries and a purified conjugate of IR dye 680RD with 40 kDa PEG (P40D680) to target lymphatic capillaries in vivo. Optical imaging settings were validated and tuned in vitro using tissue phantoms. We investigated multichromatic NIR imaging’s utility in two in vivo tissue beds: the mouse tail and rat knee joint. We then tested the ability of the approach to detect interstitial fluid perturbations due to exercise.Results: In an in vitro simulated tissue environment, free dye and PEG mixture allowed for simultaneous detection without interference. In the mouse tail, co-injected NIR tracers cleared from the interstitial space via distinct routes, suggestive of lymphatic and venous uptake mechanisms. In the rat knee, we determined that exercise after injection transiently increased lymphatic drainage as measured by lower normalized intensity immediately after exercise, whereas exercise pre-injection exhibited a transient delay in clearance from the joint.Conclusions: NIR imaging enables simultaneous imaging of lymphatic and venous-mediated fluid clearance with great sensitivity and can be used to measure temporal changes in clearance rates and pathways.

High-pressure density measurements of poly(ethylene glycol) 600 [PEG600] saturated with carbon dioxide with an oscillating device of advanced accuracy

Density measurements of poly(ethylene glycol) 600 (PEG600) and its mixture with carbon dioxide are presented for temperatures of up to 353 K and at pressures up to 40 MPa (PEG600) and up to 20 MPa (PEG600-CO2). The applied Anton Paar DMA HPM vibrating tube densimeter was calibrated using water, toluene, squalane, and glycerol. The averaged relative expanded uncertainty of the measurements is ± 0.63% for the pure PEG600 and the mixture’s measurements. A modified Tait equation was fitted to the pure PEG’s density results, which correlates well with literature values. The density of the equilibrated mixture with carbon dioxide as a function of pressure correlates well with other density trends of low molecular weight PEG mixtures reported in the literature. However, the absolute values are found to be lower than previously published results of the same fluid system.

Densities, speeds of sound, refractive indices, excess and partial molar properties of polyethylene glycol 200 + benzyl methacrylate binary mixtures at temperatures from 293.15 to 318.15 K

Green and biodegradable solvents are requisite replacements to volatile organic solvents. Polyethylene glycols have been recognized as alternatives to volatile organic solvents in numerous industrial and pharmaceutical applications because of their unique properties. In this work the measurements of physicochemical properties, viz., densities, ρ, speeds of sound, u and refractive indices, nD of the binary mixtures of PEG 200 with benzyl methacrylate, including pure liquids, over the entire mole fraction range at the temperatures, T/K = 293.15 to 318.15 and at atmospheric pressure, p = 101 kPa. The experimental data were used to calculate the excess molar volume, VmE, excess isentropic compressibility, κsE, excess speed of sound, uE, excess acoustic impedance, ZE, excess molar isentropic compressibility, Ks,mE, excess refractive index, nDE and deviation in molar refraction, ΔRM . These excess properties were fitted with the Redlich-Kister polynomial equation. In addition, the partial molar volumes and partial molar compressibilities and excess partial molar volumes and excess partial molar compressibilities over the entire mole fraction range; and at infinite dilution were also calculated. The trends of these parameters with composition and temperature were discoursed from the point of view of intermolecular interactions existed in these mixtures.

Solubility of 6-phenyl-4,5-dihydropyridazin-3(2H)-one in aqueous mixtures of Transcutol and PEG 400 revisited: Correlation and preferential solvation

Reported equilibrium mole fraction solubility values of 6-phenyl-4,5-dihydropyridazin-3(2H)-one (PDP-6) (3) in {Transcutol (1) + water (2)} and {PEG 400 (1) + water (2)} mixtures at five temperatures from T = (293.15 to 313.15) K were analyzed based on the Hildebrand solubility parameter of the respective aqueous mixtures. Cosolvency models for representing the equilibrium solubility of PDP-6 in both binary solvent systems at various temperatures were also provided for correlation/prediction purposes. Moreover, the preferential solvation parameters of PDP-6 in these aqueous-cosolvent mixtures at T = (298.15 and 313.15) K were determined by means of the “inverse Kirkwood-Buff integrals” (IKBI). PDP-6 is preferentially solvated by water in water-rich mixtures of {Transcutol (1) + water (2)} system but preferentially solvated by Transcutol in mixtures of 0.13 < x1 < 1.00. In the former case this result could be due to hydrophobic hydration around the non-polar moieties of PDP-6. Otherwise, PDP-6 is preferentially solvated by PEG 400 in all the aqueous mixtures. Moreover, in the systems where preferentially solvation of PDP-6 by cosolvents are observed, these results could be due to the Lewis acidic behavior of PDP-6 in front of Transcutol or PEG 400 molecules because these cosolvents exhibit higher Lewis basic behavior than water.

Binary System of Polyethylene Glycol 200 (1) + 3-Dimethylamino-1-propylamine (2) for CO2 Absorption: Thermophysical Properties and Spectroscopic Study.

As the concentration of CO2 in the atmosphere keeps increasing, the development of a highly efficient CO2 absorbent is highly desired. In this work, a binary mixture system of polyethylene glycol 200 (PEG 200) (1) + 3-dimethylamino-propylamine (DMAPA) (2) was used for CO2 absorption. Considering the importance of thermophysical properties to binary solutions, the densities and viscosities of the PEG 200 (1) + DMAPA (2) mixture were measured at T = (298.15, 303.15, 308.15, 313.15, and 318.15) K and atmospheric pressure over the entire composition range. Based on the density and viscosity data, the excess properties and viscous flow thermodynamic parameters were calculated, respectively. To obtain the coefficients and to estimate the standard deviations between the experimental and calculated quantities, the excess molar volume (VmE), the viscosity deviation (Δη), and the excess Gibbs free energies of activation for viscous flow (ΔG*E) were fitted to the Redlich–Kister equation. Furthermore, based on the results of UV–vis, FTIR, and 1H NMR spectra, the intermolecular interaction of PEG 200 and DMAPA was discussed. Particularly, a strong intermolecular bonding is formed when the molar ratio of PEG 200 to DMAPA is about 1:2 because of the excess molar volume (VmE). On that account, a mixture of PEG 200 and DMAPA in a ratio of 1:2 was used for studying CO2 absorption, and a CO2 absorption of about 0.19 g per gram of absorbent was achieved at room temperature and atmosphere.

The combination of simplex lattice design and chemometrics in the formulation of green tea leaves as transdermal matrix patch

Aim: This study was aimed to formulate a transdermal matrix patch using green tea leaf extract. Materials and methods: The transdermal matrix patch formulation was optimized by the simplex lattice design method. The correlation between responses was analyzed using chemometrics. The observed responses were: 1. the physical properties of the matrix patch, and 2. the percentage of dissolution efficiency of catechins, caffeine, and epigallocatechin gallate released from the patch. The determination of drug release kinetics was based on the curve-fitting analysis using zero-order, first-order, Higuchi, and Korsmeyer-Peppas models. Results: The results showed that the optimal formula was obtained using the mixture of HPMC K100, HPMC K4M, and PEG 400 at a ratio of 4.0: 4.5: 0.5. The principal component analysis (PCA) showed that %DE300 values of catechin caffeine and epigallocatechin gallate positively correlate. A similar condition was observed between the weight and thickness of the matrix. Drug release kinetics follows the Korsmeyer-Peppas model.

Modulating the rheological response of shear thickening fluids by variation in molecular weight of carrier fluid and its correlation with impact resistance of treated p-aramid fabrics

The present study deals with the effect of molecular weight of carrier fluid on the rheological behaviour of shear thickening fluid (STF) and impact energy absorption by treated p-aramid fabrics. High molecular weight polyethylene glycols (HMW-PEG: 1000, 3000 and 6000 g mol−1) were individually added to a mixture of PEG 200 and PEG 600 to prepare ternary mixtures of carrier fluids. Increase in average molecular weight of the carrier fluid via addition of PEG 1000 and PEG 3000 enhanced the dilatant behaviour of STF. On the other hand, addition of PEG 6000 led to a rheological response inferior to that obtained via addition of PEG 3000 owing to solidification of the former at room temperature resulting in fusion of silica particles. However, an inverse relation was observed between the rheological behaviour of HMW-PEG based STFs and impact resistance of p-aramid fabrics treated with them. The diminution in impact energy absorption occurred due to lubrication effect caused by long polymer chains of HMW-PEG. On the other hand, fusion of solidified PEG 6000 and silica particles created rough microstructures over the yarn surface, which enhanced inter-yarn friction, resulting in improved impact energy absorption.

Crosslinking Dynamics and Gelation Characteristics of Photo- and Thermally Polymerized Poly(Ethylene Glycol) Hydrogels.

The crosslinking behaviors and gelation features of poly(ethylene glycol) (PEG) hydrogels were scrutinized during the UV and thermal polymerizations of mixtures of poly(ethylene glycol) methacrylate (PEGMA, monomer) and poly(ethylene glycol) dimethacrylates (PEGDMAs, crosslinkers). The real-time crosslinking behavior of the PEG hydrogels was quantified as a function of the UV irradiation time and reaction temperature during the UV and thermal polymerization, respectively, using real-time FT-IR spectrometry and rotational rheometry. The gelation characteristics of UV- and thermally crosslinked hydrogels were compared through the analysis of the gel fraction, swelling ratio, surface hardness, and the loading and release of rhodamine-B. The gelation properties of the cured hydrogel films were suitably correlated with the real-time rheological properties and crosslinked network state of the PEG mixtures. The crosslinking and gelation properties of the cured hydrogels could be optimally tuned by not only the molecular weight of the crosslinker but also the UV or thermal polymerization conditions.

Fat mimicking compounds as grease thickeners in Poly(ethylene glycol)/water: Adopting the solution from history

Water-based lubricants are thought to be the next generation green lubricants, however, there are very few developments of aqueous grease lubricants. Here, water-based grease lubricants were developed using the food fat replacers. The concept of using fat replacers was inspired by the historical usage of fat as a lubricant. Dextrins were chosen as the fat replacers and mixture of water and PEG as the base fluid. Dextrins with different molecular weights were selected to study its effect on the rheological, tribological and thermal behavior of the gels. It was found that only higher molecular weight dextrins will form the colloidal gels, whereas low molecular weight dextrins will form the colloidal solution. The SEM images of the dried samples showed the agglomerated micro-spherical network with the void to hold the base fluid. It was found that, at an optimum concentration, the fat replacers showed 35–58% lower friction and 29–41% lower wear than the pure PEG200/water solution regardless of their molecular weight. The spherical shaped colloidal particles will form the film over the metal surface by nano-filling and these particles will act as nano-bearings which will reduce the wear and friction. These gel lubricants can be used where the highly biodegradable and bio-compatible green lubricant is needed.

Nankeen ink model for histological distribution of solutions used in post mortem CT-angiography

• It was possible to identify impregnation in capilar lumen on histological slices. • Nankeen ink allow histological distribution evaluation of the contrast used in PMCTA. • PEG and contrast mixtures reached the minor vessels of all the evaluated organs. • Soybean oil and contrast mixtures reached the minor vessels of all the evaluated organs. • No artifacts or histological damages were seen after the mixture injection. Post mortem computed tomography angiography (PMCTA) is an imaging modality that uses several different contrast solutions in order to highlight blood vessel paths in cadavers. This technique shows similar results when compared to conventional necropsy, especially for traumatic or vascular diseases. However, it is still unknown whether the chemical and histological features remain preserved after the intravascular injection of contrast solution for PMCTA. The aim of this study was to establish the histological regions reached by the contrast medium solution after a PMCTA procedure and to verify if the tissue architecture was preserved, using two different types of fluids to compose the solution (watery and oil fluid). A nankeen ink model was used in 2 dog cadavers with 2 different contrast solution, and a histological evaluation of the lung, liver and kidney was carried out. Nankeen ink impregnation was observed in all samples collected after the mixture injection showing the presence of ink impregnation within the blood vessel lumens. No histological artifacts were found and, moreover, histological architecture damages were not observed in those samples collected. It had been demonstrated that this nankeen ink model can be used for further studies in due to better understand the histological distribution of the contrast solution used in PMCTA procedures.

Pharmacokinetics of a potent soluble epoxide hydrolase inhibitor in three formulations

Inhibition of soluble epoxide hydrolase (sEHI) was shown to be potent to reduce the inflammation, lower the blood pressure in hypertension and is being developed for indication of chronic pain treatment. Guiding by in vitro potency screening, pharmacokinetics and in vivo efficacy studies, a potent sEHI (EC5026) is optimized for the followed clinical trials. Besides its own properties, formulation method is an important factor to be considered to reach ideal exposure time span and concentration in vivo, therefore for the efficacy in vivo.Here, we compared three different formulation methods: PEG mixtures, hot melt extrusion (HME), spray‐dried dispersion (SDD) for EC5026 by comparing the pharmacokinetics in Sprague Dawley rats. A sensitive UHPLC/MS/MS method was developed to measure the concentration of EC 5026 in the blood of rats after oral dosing at 3mg/Kg as a single dose. The pharmacokinetics parameters including Cmax, Tmax, AUC were calculated using non‐compartment modeling analysis. The result shows that three different formulations have similar pharmacokinetics properties with the highest Cmax in SDD (1,557 ng/mL) followed by HME (1,432 ng/mL) and PEG mixture (1,329 ng/mL). Tmax are all about the same at 2.5 and 3 hour respectively. The T1/2s are between 75–90 hours.The results above indicates all three formulations are proper for decent exposure of EC5026 with AUC from 6759–8516 ng/mL hr. The similarity among these three formulations allow the translation to the clinical trials using the new formulations (HME/SDD) from the preclinical studies with PEG mixture.Support or Funding InformationSupport or Funding InformationThis work was supported in part by NIEHS grant R35 ES030443, NIEHS Superfund Basic Research Program grant P42 ES04699.