Pharmacokinetic Parameters of HIV-1 Protease Inhibitors

Since the beginning of the HIV epidemic, research has been carried out to control the virus. Understanding the mechanisms of replication has given access to the various classes of drugs that over time have transformed AIDS into a manageable chronic disease. The class of protease inhibitors (PIs) gained notice in anti-retroviral therapy, once it was found that peptidomimetic molecules act by blocking the active catalytic center of the aspartic protease, which is directly related to HIV maturation. However, mutations in enzymatic internal residues are the biggest issue for these drugs, because a small change in biochemical interaction can generate resistance. Low plasma concentrations of PIs favor viral natural selection; high concentrations can inhibit even partially resistant enzymes. Food-drug/drug-drug interactions can decrease the bioavailability of PIs and are related to many side effects. Therefore, this review summarizes the pharmacokinetic properties of current PIs, the changes when pharmacological boosters are used and also lists the major mutations to help understanding of how long the continuous treatment can ensure a low viral load in patients.     

The Anti-Inflammatory Effects of the Methanolic Extract and Fractions from Davilla elliptica St. Hil. (Dilleniaceae) on Bothrops jararaca Envenomation

Inflammation and haemorrhage are the main characteristics of tissue injury in botropic envenomation. Although some studies have shown that anti-venom prevents systemic reactions, it is not efficient in preventing tissue injury at the site of the bite. Therefore, this work was undertaken to investigate the anti-inflammatory effects of the methanolic extract and fractions from D. elliptica and to evaluate the role of matrix metalloproteinases (MMPs) in this process. Effects of the extract and fractions from D. elliptica were evaluated using a carrageenan-induced paw oedema model in rats, and leukocyte rolling was visualized by intravital. The quantification of MMPs activities (MMP-2 and MMP-9) extracted from the dermis of mice treated with extract and fractions alone or incubated with venom was determined by zymographic analyses. Our results show that intraperitoneal (i.p.) injection of fractions significantly reduced paw oedema after the carrageenan challenge. Treatment with the tannins fraction also resulted in considerable inhibition of the rolling of leukocytes and this fraction was able to decrease the activation of MMP-9. These results confirmed the anti-inflammatory activity of the methanolic extract and tannins fraction of D. elliptica and showed that the dermonecrosis properties of B. jararaca venom might be mediated through the inhibition of MMP-9 activity.     

Recovery of polyphenols from camu-camu (Myrciaria dubia H.B.K. McVaugh) depulping residue by cloud point extraction

In this study the potential of cloud point extraction formed by a non-ionic surfactant was used in order to separate polyphenols from industrial residues of camu-camu. The effects of operational conditions of the cloud point extraction (CPE) on the polyphenol recovery and volumetric ratio were investigated. The results showed a maximum recovery of 95.71% that was obtained using 7.0 wt% Triton X-114, native pH (3.25), and 80 wt% polyphenol extract at 30 °C. The use of cloud point extraction was successful to recover the polyphenols from agroindustrial residue since it is a simple as well as of low-cost technique.     

Enrichment,in vitro,and quantification study of antidiabetic compounds from neglected weed Mimosa pudica using supercritical CO2 and CO2-Soxhlet

Supercritical fluid extraction (SFE) using carbon dioxide (CO₂) and liquid CO₂ using Soxhlet (CO₂-Soxhlet) extraction were employed to extract three (3) antidiabetic compounds viz. stigmasterol, quercetin, and avicularin from Mimosa pudica. Various extraction parameters were studied. Extracts were analyzed pharmacologically, qualitatively and quantitatively to ascertain enrichment levels. All three antidiabetic compounds were effectively enriched under optimized conditions of temperature 60°C, pressure 40 MPa, co-solvent ratio 30%, and CO₂ flow rate of 5 ml min^?1. SFE was found to be the better method for enrichment of the antidiabetic compounds than the CO₂-Soxhlet method. Extraction conditions were seen to affect the enrichment of desired compounds.     

Amperometric urea biosensors based on the entrapment of urease in polypyrrole films

Urease (Urs) was immobilized in electrochemically prepared polypyrrole (PPy) and the resulting films were characterized by cyclic voltammetry, scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and ultraviolet visible spectroscopy (UV-VIS). The enzymatic activity of Urs entrapped in the PPy matrix was confirmed by the catalytic conversion of urea into carbon dioxide and ammonia, when urea was detected amperometrically at different concentrations in standard samples and commercial fertilizers. The PPy/Urs biosensors exhibited selectivity, a relatively high efficiency at urea concentrations below 3.0 mmol L⁻¹, and a sensitivity to urea of 2.41 μA cm⁻² mmol⁻¹ L.     

Calcium phosphate substrates with emulsion-derived roughness: Processing,characterisation and interaction with human mesenchymal stem cells

Calcium phosphates (CaP) have been the subject of several studies that often lack a systematic approach to understanding how their properties affect biological response. CaP particles functionalised with a pH-responsive polymer (BCS) were used to prepare microporous substrates (porosity between 70 and 75% and pore sizes of 5–20 μm) through the aggregation of oil-in-water emulsions by controlling solid loading, emulsification energy, pH, drying and sintering conditions. The combined effect of surface roughness (roughness amplitude, R_a between 0.9–1.7 μm) and chemistry (varying Hydroxyapatite/β-Tricalcium phosphate ratio) on human mesenchymal stem cells was evaluated. HA substrates stimulated higher cell adhesion and proliferation (especially with lower R_a), but cell area increased with β-TCP content. The effect of surface roughness depended of chemistry: HA promoted higher mineralising activity when R_a ～ 1.5 μm, whereas β-TCP substrates stimulated a more osteogenic profile when R_a ～ 1.7 μm. A novel templating method to fabricate microporous CaP substrates was developed, opening possibilities for bone substitutes with controlled features.     

Characterization of a water-based paint for corrosion protection

Corrosion of steel rebars in reinforced concrete is one of the major problems in the construction industry. Carbonation reactions of concrete with carbon dioxide and, mainly, the chloride salts action are the main causes responsible for concrete degradation. Protective coatings help to improve the durability of concrete structures by acting as a physical barrier against the corrosion agents. Waterborne paints are usually used for concrete protection rather than solvent-based paints since they are less pollutant. The aim of this work is to investigate the influence of the pore size and porosity on the permeability of the paints films toward sodium chloride. Three characterization methods from membrane science were implemented to characterize paint coatings. The time-lag method was used to determine the permeability toward the sodium chloride and toward helium and argon, these for approximately 100% relative humidity. From the seven waterborne paints formulated, only one was found to be suitable for surface protection of reinforced concrete, since its permeability toward NaCl was smaller than 10⁻¹⁴ m² s⁻¹, the threshold value required by National Laboratory of Civil Engineering (LNEC) in Portugal. For the formulated paints, it was observed that the average pore size correlates well with the permeability toward sodium chloride. This is an important result since obtaining the permeability toward sodium chloride of corrosion protective paints is very time consuming, while the average pore size can be obtained in a much shorter time.     

Synthesis and characterization of cellulose acetate from royal palm tree agroindustrial waste

This study provides a novel value‐added utilization of the agroindustrial waste of royal palm tree leaf sheath to produce cellulose acetate. One of the motivations of this work was the fact that Brazil is one of the largest heart of palm producers in the world. However, as a result of extraction and processing, tons of waste are generated and discharged to the environment. Such waste is rich in lignocellulosic material, which could be reused to obtain derivatives of interest and commercial value. The synthesis of cellulose acetate was performed through a homogeneous acetylation reaction. Three different conditions were tested for delignification of the raw material, which resulted in a reduction in lignin content from 17.75 to 7.72%. The highest yield of cellulose acetate reached 99.5%, with degree of substitutions ranging between 2.08 and 2.82, which indicates satisfactory conversion. The Fourier transform infrared spectrum showed that practically all hydroxyl groups were replaced by acetate groups; this was also confirmed by nuclear magnetic resonance analysis. X‐ray diffraction analysis showed that the cellulose acetate crystallinity index was 8.9%. This demonstrates the viable potential of cellulose acetate production with low cost and use of highly available agroindustrial waste. POLYM. ENG. SCI., 59:891–898, 2019. © 2018 Society of Plastics Engineers