Bioactive nanoparticles derived from marine brown seaweeds and their biological applications: a review.

The biosynthesis of novel nanoparticles with varied morphologies, which has good implications for their biological capabilities, has attracted increasing attention in the field of nanotechnology. Bioactive compounds present in the extract of fungi, bacteria, plants and algae are responsible for nanoparticle synthesis. In comparison to other biological resources, brown seaweeds can also be useful to convert metal ions to metal nanoparticles because of the presence of richer bioactive chemicals. Carbohydrates, proteins, polysaccharides, vitamins, enzymes, pigments, and secondary metabolites in brown seaweeds act as natural reducing, capping, and stabilizing agents in the nanoparticle's synthesis. There are around 2000 species of seaweed that dominate marine resources, but only a few have been reported for nanoparticle synthesis. The presence of bioactive chemicals in the biosynthesized metal nanoparticles confers biological activity. The biosynthesized metal and non-metal nanoparticles from brown seaweeds possess different biological activities because of their different physiochemical properties. Compared with terrestrial resources, marine resources are not much explored for nanoparticle synthesis. To confirm their morphology, characterization methods are used, such as absorption spectrophotometer, X-ray diffraction, Fourier transforms infrared spectroscopy, scanning electron microscope, and transmission electron microscopy. This review attempts to include the vital role of brown seaweed in the synthesis of metal and non-metal nanoparticles, as well as the method of synthesis and biological applications such as anticancer, antibacterial, antioxidant, anti-diabetic, and other functions.

Potentials of roots, stems, leaves, flowers, fruits, and seeds extract for the synthesis of silver nanoparticles.

Silver nanoparticles (AgNPs) have gained significant attention in various applications due to their unique properties that differ from bulk or macro-sized counterparts. In the advancement of nanotechnology, a reliable, non-toxic, and eco-friendly green synthesis has widely been developed as an alternative method for the production of AgNPs, overcoming limitations associated with the traditional physical and chemical methods. Green synthesis of AgNPs involves the utilization of biological sources including plant extracts with silver salt as the precursor. The potential of phytochemicals in plant extracts serves as a reducing/capping and stabilizing agent to aid in the bio-reduction of Ag+ ions into a stable nanoform, Ag0. This review provides insights into the potentials of various plant parts like root, stem, leaf, flower, fruit, and seed extracts that have been extensively reported for the synthesis of AgNPs.

Natural Deep Eutectic Solvents as Rust Removal Agents from Lithic and Cellulosic Substrates.

The peculiar physicochemical features of deep eutectic solvents (DESs), in particular their tunability, make them ideal media for various applications. Despite their ability to solubilize metal oxides, their use as rust removers from valuable substrates has not yet been thoroughly investigated. In this study, we chose three known DESs, consisting of choline chloride and acetic, oxalic or citric acid for evaluating their ability to remove corrosion products from a cellulose-based material as linen fabric and two different lithotypes, as travertine and granite. The artificial staining was achieved by placing a rusty iron grid on their surfaces. The DESs were applied by means of cellulose poultice on the linen fabrics, while on the rusted stone surfaces with a cotton swab. Macro- and microscopic observations, colorimetry and SEM/EDS analysis were employed to ascertain the cleaning effectiveness and the absence of side effects on the samples after treatment. Oxalic acid-based DES was capable of removing rust stains from both stone and cellulose-based samples, while choline chloride/citric acid DES was effective only on stone specimens. The results suggest a new practical application of DESs for the elimination of rust from lithic and cellulosic substrates of precious and artistic value.

The effect of food and acid-reducing agents on the pharmacokinetic profile of capivasertib: Results from a randomized, crossover study.

AIMS: This two-part, adaptive study assessed the effect of food and an acid-reducing agent (rabeprazole) on the pharmacokinetics (PK) and safety of capivasertib, a potent AKT inhibitor, in clinical development for cancer treatment. METHODS: In Part 1, healthy participants (n = 24) were randomized to receive single-dose capivasertib after overnight fasting, a high-fat, high-calorie meal and with rabeprazole postovernight fasting in one of six treatment sequences. Based on Part 1 results, a new group of participants (n = 24) were randomized (Part 2) to receive capivasertib after overnight fasting, a low-fat, low-calorie meal and modified fasting (food restricted from 2 h before dosing to 1 h postdose) in one of six treatment sequences. Blood samples were collected for PK analyses. RESULTS: Following a high-fat, high-calorie meal, capivasertib exposure increased versus overnight fasting (geometric mean ratio [GMR] [90% confidence interval (CI)]: area under the concentration-time curve [AUCinf ] 1.32 [1.22, 1.43], maximum concentration [Cmax ] 1.23 [1.08, 1.41]), but was comparable to that postmodified fasting (GMR: AUCinf 1.13 [0.99, 1.29], Cmax 0.85 [0.70, 1.04]). AUCinf was similar and Cmax was lower with/without rabeprazole (GMR: AUCinf 0.94 [0.87, 1.02]), Cmax 0.73 [0.64, 0.84]). Capivasertib exposure was similar after a low-fat, low-calorie meal versus overnight fasting (GMR: AUCinf 1.14 [1.05, 1.25], Cmax 1.21 [0.99, 1.48]) or modified fasting (GMR: AUCinf 0.96 [0.88, 1.05], Cmax 0.86 [0.70, 1.06]). Safety was consistent with that in larger trials. CONCLUSIONS: This study demonstrates that administering capivasertib with food or acid-reducing agents does not lead to clinically relevant PK or safety profile changes.

In situ capping of silver nanoparticles with cellulosic matrices from wheat straws in enhancing their antimicrobial activity: Synthesis and characterization.

Silver nanoparticles have gained worldwide attention in the scientific community due to their high antimicrobial activity. However, they tend to agglomerate and lose their shape and properties, thus capping agents necessary to protect their shapes, sizes, and properties. To enhance their antimicrobial activity, this research aimed to cap silver nanoparticles with cellulosic matrices from wheat straws. The wheat straw was delignified with 6% HNO3, and the residual was treated with 1% NaOH and NaClO: CH3COOH (1:1), then used to synthesize cellulose nanocrystals via acid hydrolysis. AgNPs were incorporated into the CPC and CNCs by in-situ synthesis using NaHB4 as the reducing agent. Fourier Transform Infrared, Scanning Electron Microscopy, and X-ray diffraction were used to investigate their features. The findings exhibited crystallinity increased with subsequent treatments, according to XRD analysis. Ultraviolet-visible, FTIR, TEM, and XRD analysis confirmed the capping of AgNPs onto the cellulosic materials. Antibacterial activity against Staphylococcus aureus and Escherichia coli, with CNCs-AgNPs composite, exhibited higher activity compared to CPC-AgNPs composite due to the increased surface area and excellent binding on the surface of the composite.

Conversion and reducing agent effect on zero valent iron into Fe3O4 for photocatalytic degradation under UV light irradiation.

Conversion and reducing agent (NaBH4) effect on zero valent iron into Fe3O4 nanoparticles with diverse molar ratios of reducing agent was produced through chemical reduction technique. The structural, optical, vibrational analyses were executed via XRD, UV-Vis, Raman, and FT-IR analysis. The crystallite size obtained were 35 nm, 27 nm, and 18 nm for Fe:NaBH4 (1:1), Fe:NaBH4 (1:2) and Fe:NaBH4 (1:3). The morphology of the Fe:NaBH4 (1:1) was not in good orientation with higher dimensions. As explored in Fe:NaBH4 (1:2) and (1:3) samples, there is a proper growth of nanoneedles and nanosheets formation. This was due to the addition of reducing agent which greatly helped in enhancement of morphology. The prepared photocatalysts were tested to reduce Malachite Green (MG) under UV illumination. The pure dye solution obtained 57% efficiency after irradiation. Fe:NaBH4 (1:3) photocatalyst achieved 97% efficiency on reducing pollutants. The rate constant values calculated was 0.007, 0.013, 0.02 and 0.03 min-1 for pure, Fe: NaBH4 (1:1), Fe: NaBH4 (1:2) and Fe: NaBH4 (1:3) assisted MG samples. The as prepared photocatalyst is more potential one on removal of toxic pollutants from wastewater which is due to the better enhancement of nanoneedles and nanosheets oriented by the effect of reducing agent. The advantage of Fe3O4 nanoparticles for wastewater is that the removal of these nanoparticles can be ease with magnetic separation methods. On considering the advantage of removing of photocatalyst and efficiency, this prepared product is suitable one for wastewater remediation process in future days.

Handheld, Low-Cost, Aptamer-Based Sensing Device for Rapid SARS-CoV-2 RNA Detection Using Novelly Synthesized Gold Nanoparticles.

The development of a cost-efficient device to rapidly detect pandemic viruses is paramount. Hence, an innovative and scalable synthesis of metal nanoparticles followed by its usage for rapid detection of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has been reported in this work. The simple synthesis of metal nanoparticles utilizing tin as a solid-state reusable reducing agent is used for the SARS-CoV-2 ribonucleic acid (RNA) detection. Moreover, the solid-state reduction process occurs faster and leads to the enhanced formation of silver and gold nanoparticles (AuNPs) with voltage. By adding tin as a solid-state reducing agent with the precursor, the nanoparticles are formed within 30 s. This synthesis method can be easily scaled up for a commercially viable process to obtain different-sized metal nanoparticles. This is the first disclosure of the usage of tin as a reusable solid-state reducing agent for metal nanoparticle synthesis. An electronic device, consisting of AuNPs functionalized with a deoxyribonucleic acid (DNA)-based aptamer, can detect SARS-CoV-2 RNA in less than 5 min. With an increase in SARS-CoV-2 variants, such as Delta and Omicron, the detection device could be used for identifying the nucleic acids of the COVID-19 variants by modifying the aptamer sequence. The reported work overcomes the drawbacks of complex instrumentation, trained labor, and increased turnaround time.

Synthesis of Ultrathin Metal Nanowires with Chemically Exfoliated Tungsten Disulfide Nanosheets.

Transition metal dichalcogenides (TMDs) have attracted great interest owing to their fascinating properties with atomically thin nature. Although TMDs have been exploited for diverse applications, the effective role of TMDs in the synthesis of metal nanowires has not been explored. Here, we propose a new approach to synthesize ultrathin metal nanowires using TMDs for the first time. High-quality ultrathin nanowires with an average diameter of 11.3 nm are successfully synthesized for realizing high-performance transparent conductors that exhibit excellent conductivity and transparency with low haze. The growth mechanism is carefully investigated using high-resolution transmission electron microscopy, and growth of nanowires with tunable diameters is achieved by controlling the nanosheet dimension. Finally, we unravel the important role of TMDs acting as both reducing and nucleating agents. Therefore, our work provides a new strategy of the TMD as an innovative material for the growth of metal nanowires as a promising building block in next-generation optoelectronics.

UV responsive quercetin derived and functionalized CuO/ZnO nanocomposite in ameliorating photocatalytic degradation of rhodamine B dye and enhanced biocidal activity against selected pathogenic strains.

Quercetin was investigated for its role as a reducing agent in biosynthesizing CuO/ZnO nanocomposite, its subsequent surface functionalization and influence in Rhodamine B dye degradation and biocidal activity. The as synthesized quercetin functionalized CuO/ZnO nanocomposite (CuO/ZnO@Q) was analyzed using X-ray diffraction (XRD), Fourier transform infra red spectroscopy (FTIR), Transmission electron microscopy (TEM), Energy dispersive spectroscopy (EDS) and Ultraviolet-visible spectroscopy (UV-Vis). XRD showed the formation of crystalline CuO, ZnO phases and FTIR analysis revealed the incorporation of quercetin functional groups in the synthesized nanocomposite. TEM image displayed the formation of quercetin deposited spherical CuO/ZnO nanostructure with the EDAX results confirming the presence of organic carbon composition from quercetin. The UV absorption spectra ascertained the presence and role of quercetin in the enhanced absorption of radiation in the UV range. CuO/ZnO@Q showed improved photocatalysis with complete Rhodamine B dye degradation after 75 min of UV irradiation, as against pure CuO/ZnO, which exhibited incomplete dye degradation even after 90 min of irradiation. Moreover, quercetin surface functionalization effectively ameliorated its antimicrobial activity against E. coli, S. aureus, Shigella, B. subtilis, A. niger and C. albicans, proving its potential in significantly enhancing biocidal activity along with photocatalytic dye degradation in a natural and eco-friendly route.

Breaking the rules: tooth whitening by means of a reducing agent.

OBJECTIVES: It is widely accepted that current tooth whitening treatment effect is based on the oxidizing action of peroxides, even if the mechanism of action remains still unclear. Treatments are claimed to be safe, but several secondary effects have been described, since long application times and high concentrations are needed. A faster whitening ingredient which permits the use of lower concentrations and shorter application times could potentially overcome this problem. In this work, a different approach based on a reducing agent, sodium metabisulfite (MBS), is explored. MATERIALS AND METHODS: The reaction between tannic acid (TA) with carbamide peroxide (CP), MBS, and potassium persulfate (PS), as an oxidizing agent, was monitored for 48 hours by measuring its absorbance, comparing their different whitening effects. The reduction process between TA and MBS was confirmed by cyclic voltammetry. An in vitro test was used to observe if MBS whitens also stained teeth. RESULTS: It is shown that MBS bleaching effect is faster and higher than CP's effect over time. PS produced a darkening effect after the 3rd hour because of the strong absorbance of the oxidation metabolite. Cyclic voltammetry showed a progressive increase in the intensity of the TA anodic peak when MBS was present, demonstrating that a reduction is taking place. In vitro, MBS showed a faster whitening performance than CP, using lower concentrations. CONCLUSIONS: Using a TA solution as a staining model, it was possible to show that MBS has a visible bleaching effect through a reduction reaction, faster than CP, both in solution and in vitro. Low concentrations of MBS are effective in whitening. CLINICAL SIGNIFICANCE: This work shows MBS as a promising candidate to develop novel whitening treatments, which is acting by reducing mechanism instead of oxidation.

Effect of Reducing Agent on Solution Synthesis of Li3V2(PO4)3 Cathode Material for Lithium Ion Batteries.

In this study, Li3V2(PO4)3 (LVP) powders are prepared by a solution synthesis method. The effects of two reducing agents on crystal structure and morphology and electrochemical properties are investigated. Preliminary studies on reducing agents such as oxalic acid and citric acid, are used to reduce the vanadium (V) precursor. The oxalic acid-assisted synthesis induces smaller particles (30 nm) compared with the citric acid-assisted synthesis (70 nm). The LVP powders obtained by the oxalic acid exhibit a higher specific capacity (124 mAh g-1 at 1C) and better cycling performance (122 mAh g-1 following 50 cycles at 1C rate) than those for the citric acid. This is due to their higher electronic conductivity caused by carbon coating and downsizing the particles. The charge-discharge plateaus obtained from cyclic voltammetry are in good agreement with galvanostatic cycling profiles.

Identification of recombinant AtPYL2, an abscisic acid receptor, in E. coli using a substrate-derived bioactive small molecule, a biotin linker with alkyne and amino groups, and a protein cross-linker.

Target protein identification of bioactive small molecules is one of the most important research in forward chemical genetics. The affinity chromatography technique to use a resin bound with a small molecule is often used for identification of a target protein of a bioactive small molecule. Here we report a new method to isolate a protein targeted with a bioactive small molecule using a biotin linker with alkyne and amino groups, protein cross-linker containing disulfide bond, and a bioactive small molecule with an azido group (azido probe). After an azido probe is associated with a target protein, the complex of a target protein and azido probe is covalently bound through the biotin linker by azide-alkyne Huisgen cycloaddition and protein cross-linker containing disulfide bond. This ternary complex is immobilized on an affinity matrix with streptavidin, and then the target protein is selectively eluted with a buffer containing a reducing agent for cleavage of disulfide bonds. This method uses a probe having an azido group, which a small functional group, and has the possibility to be a solution strategy to overcome the hindrance of a functional group introduced into the probe that reduces association a target protein. The effectiveness of the method in this study was shown using linker 1, 3'-azidoabscisic acid 3, and protein cross-linker containing a disulfide bond (DTSSP 5).

In-situ microscale spectrophotometric determination of phenytoin by using branched gold nanoparticles.

A rapid method for the sensitive detection of phenytoin (PHT) by branched gold nanoparticles (B-AuNPs) is described. These nanoparticles were synthesized by adding methanol as the reducing agent and poly(ethylene glycol) as the stabilizer at 70 °C. The B-AuNPs are red in color with an absorption maximum at 540 nm when prepared in situ. However, the color becomes increasingly weaker when PHT is present in increasing concentrations. This method can determine PHT over the 67-670 ng·mL-1 concentration range, with detection limit of 21 ng·mL-1. The relative standard deviation for five replicate measurements at 68 and 530 ng·mL-1 of PHT was 3.2% and 1.2%, respectively. The method was applied to the determination of PHT in plasma samples of epileptic patients, and the results were in agreement with those obtained by a standard official method. Graphical abstract Branched gold nanoparticles (AuNPs) prepared in situ have a red color with an absorption maximum at 540 nm. The color becomes increasingly weaker with decreasing the intensity of the characteristic SPR band when PHT is present in increasing concentration. The current assay is capable of determining PHT over the 67-670 ng·mL-1 concentration range with a limit of detection of 21 ng·mL-1.

A novel structured nanosized CaO on nanosilica surface as an alternative solid reducing agent for hydrogen fluoride removal from industrial waste water.

In the semiconductor industry, perfluorinated compound removal is a major concern owing to the formation of highly toxic and hazardous hydrogen fluoride (HF) as a by-product. Calcium oxide (CaO) can be considered a promising material for HF sorption reaction process. However, the easier reaction between CaO and H2O results in the formation of Ca(OH)2, which ultimately limits the usefulness of CaO. The objective of the research work is preparation of CaO nanoparticles on hydrophobic silica (SiO2) to use as a alternative solid reducing catalyst for efficient HF removal process. High-resolution transmission electron microscopy micrographs confirmed that the as-prepared CaO particles are <5 nm in size and the smaller sized CaO nanoparticles are homogeneously anchored on the entire surface of ∼100 nm spherical SiO2 nanoparticles. The reaction-enhanced regenerative catalytic system (RE-RCS) was used to measure the HF removal efficiency. HF is removed more efficiently using CaO on SiO2 than using CaO alone. At the outlet of the RE-RCS, the obtained HF concentrations are 2811.4 and 2166.1 ppm after a 3 h reaction using CaO and CaO on SiO2 as the sorbent, respectively. The lower concentration of HF at the outlet of the system using CaO on SiO2 indicates that HF sorption is remarkably enhanced using CaO on SiO2 inside the RE-RCS. In addition, the presence of a hydrophobic region in the catalyst sorbent prevents the reaction between CaO and water, which leads to avoiding the formation of Ca(OH)2. These phenomena significantly enhance the HF removal efficiency and CaF2 formation process.

A discovery and development roadmap for new endectocidal transmission-blocking agents in malaria.

Reaching the overall goal of eliminating malaria requires halting disease transmission. One approach to blocking transmission is to prevent passage of the parasite to a mosquito, by preventing formation or transmission of gametocytes. An alternative approach, pioneered in the veterinary field, is to use endectocides, which are molecules that render vertebrate blood meals toxic for the mosquito vector, also killing the parasite. Field studies and modelling suggest that reducing the lifespan of the mosquito may significantly reduce transmission, given the lengthy maturation process of the parasite. To guide the development of new endectocides, or the reformulation of existing molecules, it is important to construct a framework of the required attributes, commonly called the target candidate profile. Here, using a combination of insights from current endectocides, mathematical models of the malaria transmission dynamics, and known impacts of vector control, a target candidate profile (TCP-6) and a regulatory strategy are proposed for a transmission reducing agent. The parameters chosen can be used to assess the potential of a new medicine, independent of whether it has classical endectocide activity, reduces the insect and parasite lifespan or any combination of all three, thereby constituting an 'endectocidal transmission blocking' paradigm.

Quantification of the catalytic performance of C1-cellulose-specific lytic polysaccharide monooxygenases.

Lytic polysaccharide monooxygenases (LPMOs) have recently been shown to significantly enhance the degradation of recalcitrant polysaccharides and are of interest for the production of biochemicals and bioethanol from plant biomass. The copper-containing LPMOs utilize electrons, provided by reducing agents, to oxidatively cleave polysaccharides. Here, we report the development of a ß-glucosidase-assisted method to quantify the release of C1-oxidized gluco-oligosaccharides from cellulose by two C1-oxidizing LPMOs from Myceliophthora thermophila C1. Based on this quantification method, we demonstrate that the catalytic performance of both MtLPMOs is strongly dependent on pH and temperature. The obtained results indicate that the catalytic performance of LPMOs depends on the interaction of multiple factors, which are affected by both pH and temperature.

Improved detection of biomarkers in cervico-vaginal mucus (CVM) from postpartum cattle.

BACKGROUND: In the postpartum cow, early diagnosis of uterine disease is currently problematic due to the lack of reliable, non-invasive diagnostic methods. Cervico-vaginal mucus (CVM) is an easy to collect potentially informative source of biomarkers for the diagnosis and prognosis of uterine disease in cows. Here, we report an improved method for processing CVM from postpartum dairy cows for the measurement of immune biomarkers. CVM samples were collected from the vagina using gloved hand during the first two weeks postpartum and processed with buffer alone or buffer containing different concentrations of the reducing agents recommended in standard protocols: Dithiothriotol (DTT) or N-Acetyl-L-Cysteine (NAC). Total protein was measured using the bicinchoninic acid (BCA) assay; interleukin 6 (IL-6), IL-8 and α1-acid glycoprotein (AGP) were measured by ELISA. RESULTS: We found that use of reducing agents to liquefy CVM affects protein yield and the accuracy of biomarker detection. Our improved protocol results in lower protein yields but improved detection of cytokines and chemokines. Using our modified method to measure AGP in CVM we found raised levels of AGP at seven days postpartum in CVM from cows that went on to develop endometritis. CONCLUSION: We conclude that processing CVM without reducing agents improves detection of biomarkers that reflect uterine health in cattle. We propose that measurement of AGP in CVM during the first week postpartum may identify cows at risk of developing clinical endometritis.

Structural basis of the substrate specificity and instability in solution of a glycosidase from Lactobacillus plantarum.

Statistics from structural genomics initiatives reveal that around 50-55% of the expressed, non-membrane proteins cannot be purified and therefore structurally characterized due to solubility problems, which emphasized protein solubility as one of the most serious concerns in structural biology projects. Lactobacillus plantarum CECT 748T produces an aggregation-prone glycosidase (LpBgl) that we crystallized previously. However, this result could not be reproduced due to protein instability and therefore further high-resolution structural analyses of LpBgl were impeded. The obtained crystals of LpBgl diffracted up to 2.48Å resolution and permitted to solve the structure of the enzyme. Analysis of the active site revealed a pocket for phosphate-binding with an uncommon architecture, where a phosphate molecule is tightly bound suggesting the recognition of 6-phosphoryl sugars. In agreement with this observation, we showed that LpBgl exhibited 6-phospho-ß-glucosidase activity. Combination of structural and mass spectrometry results revealed the formation of dimethyl arsenic adducts on the solvent exposed cysteine residues Cys211 and Cys292. Remarkably, the double mutant Cys211Ser/Cys292Ser resulted stable in solution at high concentrations indicating that the marginal solubility of LpBgl can be ascribed specifically to these two cysteine residues. The 2.30Å crystal structure of this double mutant showed no disorder around the newly incorporated serine residues and also loop rearrangements within the phosphate-binding site. Notably, LpBgl could be prepared at high yield by proteolytic digestion of the fusion protein LSLt-LpBgl, which raises important questions about potential hysteretic processes upon its initial production as an enzyme fused to a solubility enhancer.

Biorelevant Dissolution Models for a Weak Base To Facilitate Formulation Development and Overcome Reduced Bioavailability Caused by Hypochlordyria or Achlorhydria.

In this study, two dissolution models were developed to achieve in vitro-in vivo relationship for immediate release formulations of Compound-A, a poorly soluble weak base with pH-dependent solubility and low bioavailability in hypochlorhydric and achlorhydric patients. The dissolution models were designed to approximate the hypo-/achlorhydric and normal fasted stomach conditions after a glass of water was ingested with the drug. The dissolution data from the two models were predictive of the relative in vivo bioavailability of various formulations under the same gastric condition, hypo-/achlorhydric or normal. Furthermore, the dissolution data were able to estimate the relative performance under hypo-/achlorhydric and normal fasted conditions for the same formulation. Together, these biorelevant dissolution models facilitated formulation development for Compound-A by identifying the right type and amount of key excipient to enhance bioavailability and mitigate the negative effect of hypo-/achlorhydria due to drug-drug interaction with acid-reducing agents. The dissolution models use readily available USP apparatus 2, and their broader utility can be evaluated on other BCS 2B compounds with reduced bioavailability caused by hypo-/achlorhydria.

Increasing the Bile Acid Sequestration Performance of Cationic Hydrogels by Using an Advanced/Controlled Polymerization Technique.

PURPOSE: To investigate the influence of the polymerization technique and the content of hydroxyl groups on the performance of new bile acid sequestrants based on PAMPMTA-co-PHEA (PAMPTMA: poly((3-acrylamidopropyl)trimethylammonium chloride); PHEA: poly(2-hydroxyethyl acrylate)) hydrogels. METHODS: PAMPMTA-co-PHEA hydrogels were prepared using either free radical polymerization or supplemental activator and reducing agent atom transfer radical polymerization. The chemical structure and composition of the hydrogels was confirmed by both FTIR and ssNMR. The binding of sodium cholate as the model bile salt was evaluated in simulated intestinal fluid using HPLC. The degradation of the polymers was evaluated in vitro in solutions mimicking the gastrointestinal tract environment. RESULTS: The binding showed that an increase of the amount of HEA in the hydrogel lead to a decrease of the binding capacity. In addition, it was demonstrated for the first time that the hydrogels produced by SARA ATRP presented a higher binding capacity than similar ones produced by FRP. Finally, it was observed that copolymers of PAMPTMA-co-PHEA showed no sign of degradation in solutions mimicking both the stomach and the intestine environment. CONCLUSIONS: The use of an advanced polymerization technique, such as the SARA ATRP, could be beneficial for the preparation of BAS with enhanced performance.