High Ee Research Articles

Manipulation of Lipid Nanocapsules as an Efficient Intranasal Platform for Brain Deposition of Clozapine as an Antipsychotic Drug

Background/objectives: The blood–brain barrier (BBB) significantly limits the treatment of central nervous system disorders, such as schizophrenia, by restricting drug delivery to the brain. This study explores the potential of intranasal clozapine-loaded lipid nanocapsules (IN LNCsClo) as a targeted and effective delivery system to the brain. Methods: LNCsClo were prepared using the phase inversion technique and characterized in terms of size, zeta potential, entrapment efficiency (EE%), and in vitro drug release. The pharmacokinetic, safety, and pharmacodynamic effects of LNCsClo were then evaluated in a rat model through intranasal (IN) administration and compared with those of oral and intravenous (IV) Clo solutions. Results: LNCsClo were prepared using a phase inversion technique, resulting in a nanocarrier with a particle size of 28.6 ± 3.6 nm, homogenous dispersion, and high EE% (84.66 ± 5.66%). Pharmacokinetic analysis demonstrated that IN LNCsClo provided enhanced Clo brain bioavailability, rapid CNS targeting, and prolonged drug retention compared to oral and intravenous routes. Notably, the area under the curve (AUC) for brain concentration showed more than two-fold and eight-fold increases with LNCsClo, compared to IV and oral solutions, respectively, indicating improved brain-targeting efficiency. Safety assessments indicated that LNCsClo administration mitigated Clo-associated metabolic side effects, such as hyperglycemia, insulin imbalance, and liver enzyme alterations. Additionally, pharmacodynamic studies showed that LNCsClo significantly improved antipsychotic efficacy and reduced schizophrenia-induced hyperactivity, while preserving motor function. Conclusions: These results highlight the potential of IN LNCsClo as a novel drug delivery system, offering improved therapeutic efficacy, reduced systemic side effects, and better patient compliance in the treatment of schizophrenia and potentially other CNS disorders.

Fabrication and Evaluation of Polyacrylate Nanocomposites Embedded With Metal Oxides as Enhanced Multipurpose Nanocarriers for Long‐Term Anti‐Inflammatory and Amazing Antimicrobial Properties

ABSTRACTThe design of super‐antimicrobially active multipurpose nanocarriers as polymeric nanocomposites embedded with metal oxides with sustained drug release is beneficial in medical treatment for controlling inflammation and targeting a wide range of pathogenic microorganisms. Brilliant metal oxide nanoparticles (MOx) involving selenium dioxide, titanium dioxide, and vanadium pentoxide were well prepared in good yields, and their morphologies and structures were specified. Then they were embedded in copolymeric nanocomposites through in situ microemulsion polymerization of (E)‐2‐cyano‐N‐cyclohexyl‐3‐(dimethylamino)acrylamide (CHAA) with methyl methacrylate (MMA), dimethylaminoethyl methacrylate (DMAEMA), and acrylic acid (AA). In addition, ibuprofen was then loaded into the synthesized polymers and their nanocomposites to achieve high drug entrapment efficiency EE%, and its release behavior was studied in various simulated fluids. The produced drug‐loaded polymers and their nanocomposites were characterized using Fourier‐transform infrared spectroscopy (FT‐IR), transmission electron microscope (TEM), X‐ray diffraction (XRD), and thermogravimetric analysis (TG). Well‐defined nanospheres of polymeric‐metal oxide nanocomposites were generated in a size range of 50 nm, with ibuprofen loaded at a high encapsulation efficiency of approximately 97%. In vitro drug release was inspected for the polymer and its nanocomposites revealing that the presence of metal oxide nanoparticles resulted in prolonged and sustained release behavior for wound dressing. The antimicrobial study based on the zone of inhibition against various pathogenic microorganisms showed excellent activity against Bacillus cereus, Staphylococcus aureus, Escherichia coli, Helicobacter pylori, and Candida albicans. These findings validate the potential of these nanocomposites to serve as a viable upcoming antimicrobial agent for the treatment of human ailments.

Relationship between emotional eating and nutritional intake in adult women with overweight and obesity: a cross-sectional study

BackgroundEmotional eating (EE) is particularly prevalent in overweight or obese women, who may turn to food as a way to cope with stress, sadness, or anxiety. Limited research has been conducted on the association between EE and nutritional intake. Therefore, present study was designed to explore this association in adult women with overweight and obesity.MethodsIn this cross-sectional study, the relationship between EE and nutritional intake in 303 overweight and obese women (aged 18–50 years) was examined. The researchers used the validated semi-quantitative Food Frequency Questionnaire (FFQ) to assess participants’ nutritional intake and the Dutch Eating Behavior Questionnaire (DEBQ) to evaluate their eating behavior. To determine the association between EE and nutritional intake, we employed the multiple linear regression analysis.ResultsThe frequency of high intensity EE was 64.4% among the study participants and the mean total score of EE subscale of DBEQ was 2.32 ± 0.81. The total score of EE was positively associated with the energy intake (β = 0.396, P = 0.007), even after adjusting for age and BMI. In addition, a significant inverse association was found between the score of EE and the daily intake of calcium (β= -0.219, P = 0.026), riboflavin (β= -0.166, P = 0.043), and vitamin B12 (β= -0.271, P = 0.035), independent from energy and age. Also the results showed a significant positive association between the score of EE and the frequency of daily intake of cracker, muffin, cake, cream cake, pastry, candy, ice cream, pickles, melon, hydrogenated vegetable oil, peanut, salted and roasted seeds, and corn-cheese puff snack.ConclusionThis study found that overweight or obese women with higher intensity of EE might have a higher intake of energy and a lower intake of dietary calcium, riboflavin and vitamin B12. Integrating a balanced diet with psychotherapy is suggested to help individuals with EE reducing the urge to eat in response to emotions.

Asymmetric Synthesis of Benzofuranones with a C3 Quaternary Center via an Addition/Cyclization Cascade Using Noncovalent N-Heterocyclic Carbene Catalysis.

An asymmetric addition/cyclization cascade of amidoesters and iminoquinones is developed using noncovalent N-heterocyclic carbene (NHC) catalysis. The process enables access to various functionalized benzofuranones with an all-carbon quaternary stereocenter with high yields and ee values. The reaction displays a broad substrate scope. Via product modifications, enantioenriched synthesis of biologically relevant spirocyclic lactones and lactams is achieved. Substrate activation via noncovalent interaction with NHC is suggested for the process.

A highly efficient chemoenzymatic process to produce (R)-6,7-dihydroxygeraniol

The efficient asymmetric dihydroxylation of 6,7-epoxygeraniol was performed using a chemoenzymatic process employing a yeast epoxide hydrolase (EH) resolution stereoinversion step, followed by stereoretentive chemical hydrolysis of the remaining epoxide to produce (6 R)-6,7-dihydroxygeraniol at unprecedented high enantiometic excess (ee) (>97.5%) and high isolated yield (72 mol % overall yield over 5 steps from commercially available geraniol). The enzymatic process was completed within 2 h at 250 g/L substrate loading reaching > 49.5 mass % conversion of the racemic epoxide. The reaction was self-limiting and furnished both the homochiral (6 R)-triol and the residual (6 R)-epoxide at > 99% ee, due to enantio-inversion of the (6S)-epoxide. The (6 R)-epoxide was subsequently chemically hydrolysed, without first needing to separate the epoxide and triol products, to afford the desired (6 R)-triol product in >97.5% ee, at multigram scale. This chemoenzymatic procedure offers an excellent alternative to chemical asymmetric epoxidation or dihydroxylation for the production of enantiopure 6,7-dihydroxygeranyl and 6,7-epoxygeranyl type compounds in general. It exemplifies the benefits of using greener EH bioprocesses to produce such compounds in high ee’s and high isolated yields.

Preparation of curcumin-loaded chitosan/lecithin nanoparticles with increased anti-oxidant activity and in vivo bioavailability

As a natural polyphenol, curcumin (Cur) has exhibited a range of bioactive properties, including anti-inflammatory, anti-oxidant, and anti-infection properties. However, the chemical instability and low water solubility of Cur hinder its wide application. Herein, Cur-loaded chitosan/lecithin nanoparticles (CCL NPs) were prepared by the electrostatic self-assembly method. The prepared CCL NPs showed a small particle size (122.86 ± 1.53 nm) with homogeneous distribution (PDI = 0.17 ± 0.01). The high EE (79.34 ± 2.93 %) and LC (9.33 ± 0.34 %) indicated that most of Cur was encapsulated in CCL NPs. Meanwhile, the Cur was released from CCL NPs in a quick and sustained way after being exposed to simulated gastrointestinal fluids. The CCL NPs displayed superior anti-oxidant activity than that of free Cur. Moreover, the in vivo pharmacokinetic studies showed that the CCL NPs could lead to a ~ 2.64-fold increase in oral bioavailability compared with that of free Cur. All these findings indicated that the formation of CCL NPs would be a promising platform to deliver Cur in the food industry.

Visible-light-driven photobiocatalytic synthesis of chiral sulfoxides over immobilized chloroperoxidase on magnetic yolk–shell Fe3O4@Cu-H-TiO2 photocatalyst

Chloroperoxidase (CPO) is promising for the asymmetric synthesis of sulfoxides from sulfides, owing to its high enantioselectivity under mild reaction conditions. However, suffering from the stability and recyclability issue, the application of free CPO is heavily restricted in current stage. In this work, an integrated photobiocatalyst was designed and fabricated by immobilizing CPO on a magnetically recyclable photocatalyst, Fe3O4@Cu-H-TiO2, which can supply H2O2 for CPO in situ continuously and suppress the destruction of CPO caused by excess H2O2. The obtained CPO@Fe3O4@Cu-H-TiO2 can catalyze the synthesis of enantiopure (R)-sulfoxides from sulfides with high yield up to 88% and high ee value up to >99% over this TiO2-based photobiocatalyst. The enhanced performance of the integrated photobiocatalyst is attributed to the controllable supply of H2O2, the improved stability of immobilized CPO and the enhanced proximity effect between photo- and bio- catalytic modules.

Asymmetric Intermolecular Conjugate Addition of 3-Substituted 2-Benzofuranones to Maleimides via Noncovalent NHC Catalysis

AbstractAn efficient N-heterocyclic carbene (NHC)-catalyzed asymmetric conjugate addition reaction to afford synthetically challenging benzofuranone derivatives having vicinal all-carbon quaternary and tertiary stereocenters is presented. The reaction operates solely through noncovalent interaction between a newly designed NHC and the substrates, providing access to a series of functionalized benzofuranones in good yields and with high ee values. The protocol applies to preparative-scale synthesis. A catalytic cycle involving a noncovalent substrate–NHC interaction is implicated in the process, based on a mechanistic control study.

Formulation and Evaluation of Acyclovir Loaded Transferosomal Gel for Transdermal Drug Delivery

Background: A carrying structure for targeted transdermal drug delivery is a transferosome. These unique liposomes are made of an edge activator and phosphatidylcholine. The most common antiviral drug is acyclovir, a synthetic nucleotide nucleoside analog derived from guanine. It works well to cure the varicella-zoster virus and the virus that causes herpes simplex (HSV), primarily HSV-1 and HSV-2. But its skin permeability is minimal. Therefore, this work aimed to use transferosomes to prepare acyclovir so that it could pass through the skin's barrier function. Objective: This study uses a 32-factorial factorial design to develop a transferosomal gel containing acyclovir through thin-film hydration method for painless acyclovir delivery services for skin disease treatment. Material and Methods: The independent variables are the amount of phospholipid (X1) and tween 80 (X2), while the dependent variables are particle size (Y1) and percentage entrapment efficiency (Y2). To create an ideal formulation, the produced transferosomes were assessed for particle size, in vitro drug release amount, and entrapment efficiency (EE%). A Carbopol 934 gel basis was prepared using the optimized acyclovir transferosome formulation, and its drug concentration, pH, spreadability, viscosity, and stability were assessed. Results: With small particles ranging from 176.6 to 324.4 nm, the produced acyclovir transferosomes had a high EE% range from 66.34 to 76.42 %. According to the in vitro release study, there is a negative correlation between in vitro release and EE%. The formulation TF5, including 1%w/w of carbopol 940, provides a superior profile of drug absorption in vitro. Consequently, acyclovir can enter the skin as transferosomes and cross the stratum corneum barrier. Conclusion: Acyclovir can be transformed into a transfersomal gel, which will improve antiviral efficacy, get over the skin's protective layer, prevent adverse oral reactions, and eventually improve patient adherence. Keywords: Transferosome, Transdermal drug delivery system, Acyclovir, 32 Fractional factorial design, Carbopol 934

Variables Affecting the Preparation and Characterization of Axitinib as Oral Niosmoes

Axitinib is anticancer drug act on different solid tumors by inhibtion protein kinase enzyme which is responsible for support the tumors with blood demand. Due to its low solubility, it has low bioavailability when given orally also it is affected by liver metabolism. Axitinib formulated as non-ionic vesicles (niosomes) for the first time to study the effect of different variables on the in vitro behaviour of vesicles in a hope to improve drug oral bioavailability. Niosomal dispersion formulas were formulated by diverse techniques via multiple kinds of surface-active agent (tween also span), cholesterol and dicetyl phosphate then evaluated for visual appearance, efficiency of drug entrapment (EE%), size of the vesicles, poly dispersity index, zetapotential, viscosity, invitro drug release and study the vesicles morphology by FE-SEM. Many variables effect on EE% were studied such as effect of surfactant amount and type, effect of surfactant combination, impact of various ratios of cholesterol, impact of DCP in various amount , effect of preparation method and effect of sonication time. The results showed that the EE% between (50.97%-98.24%), the particle size was found within the range (64.5 nm - 530.79 nm), zeta potential which was between ( -16.6 to -31 mV), polydispersity index (PDI) <1 and viscosity between (584 – 889.6) centipoise. The niosomal dispersion F1 which contained 1:1 weight ratio (span60: cholesterol) was found with high EE% (96.5±0.16%), smallest particle size (64.5±0.5 nm), highest drug release (100%) of drug released at the end of 4 hours and FE-SEM photograph showed that niosomes were spherical with no aggregation and had a smooth surface. The results showed that thin film hydration method with sonication for four minutes was the best method for preparation of axitinib niosomes, the type and amount of surfactants used, cholesterol ratio, stabilizer and the time of sonication had a substantial effect on EE%, the size of the vesicles as well as drug release; which were investigated so as to optimize the niosomal dispersion of anti-tumour drug reaching to an optimum formula that may improve drug bioavailability. Key words: Axitinib, Anticancer, Vesicles, Surfactants, Invitro behaviour, Entrapment efficiency.

Fluidized spanlastics for intranasal brain delivery of lacosamide aiming to control Status Epilepticus: Design, Characterization, Ex-vivo permeation, Radioiodination and In-vivo biodistribution studies

Status Epilepticus (SE) is a neurological condition characterized by anomalous brain activity, causing repetitive seizures lasting for more than 5 min or periods of unusual behavior without returning to a normal level of consciousness between episodes. Chitosan has shown various pharmaceutical benefits, particularly in intranasal administration. In the current manuscript, novel ultra-deformable vesicles (fluidized spanlastics) loaded with lacosamide (LCM), a model anti-epileptic drug, were formulated and compared with their chitosan containing counterparts. The formed vesicles were assessed for their particle size (PS), zeta potential (ZP), entrapment efficiency (EE%) and storage stability. Surface morphology, pH and viscosity measurements, in-vitro release study and release kinetics, and ex-vivo permeation across nasal sheep mucosa were carried out on the optimized formulations. The bio-distribution and pharmacokinetic studies were performed using the radioiodinated-LCM (131I-LCM) utilizing different routes of administration to assess the in-vivo performance of intravenous solutions (IVs), intranasal solutions (INs) and the intranasal administered optimized formula (INFS). LCM-vesicles showed PS ranging from 109.90 to 418.4 nm, negative ZP values ranging from −28.00 to −48.30 mV in case of regular vesicles and shifted to +16.70 to +18.72 mV in case of chitosan coated vesicles, high EE% values having a range of 65.76–97.25 % and good storage stability properties. The optimized formulation showed spherical shape and enhanced ex-vivo permeation approximately 4-fold higher compared to LCM solution. The results of the in-vivo study demonstrated that the brain/blood ratio (B/B) of INs was 3.3-fold higher than IVs and INs of 131I-LCM in the first 5 min. Accordingly, the prepared system has been shown to possess a promising potential for brain diagnosis and/or therapy.

High durable SPEEK/TiO2 nanopaper composite membrane for vanadium redox flow battery

Sulfonated poly (ether ether ketone) (SPEEK) ion exchange membranes for VRFB are promising alternatives to Nafion, but require improved mechanical and chemical stability for long-term operation. Here, we have fabricated composite membranes using SPEEK as proton conductive medium and TiO2 nanopapers as reinforcing framework to improve the mechanical and chemical stabilities of SPEEK membranes. The SPEEK/TiO2 nanopaper composite membranes exhibited almost twice the tensile strength and only one-third the vanadium ion permeability compared to pristine SPEEK (DS=60 %). Due to the excellent cell performance such as high EE, slow capacity degradation and long-term lifetime, these high durable composite membranes could be found their potential use as ion exchange membranes for commercial VRFBs.

Back to Nature: Development and Optimization of Bioinspired Nanocarriers for Potential Breast Cancer Treatment

This study focuses on the preparation and optimization of caffeic acid (CA)-loaded casein nanoparticles (CS NPs) via the Box–Behnken design (BBD) for potential applications in cancer treatment. CS NPs were loaded with CA as a promising anti-cancer molecule. Non-hazardous green materials were exploited for nanoparticle fabrication. The BBD was used, followed by a desirability function to select the optimum formulation. The BBD was adopted as it avoids the runs implemented in extreme conditions, hence making it suitable for proteins. CS NPs were characterized regarding particle size (PS), size distribution (PDI), zeta potential (ZP), drug entrapment, morphology using TEM, differential scanning calorimetry, molecular docking, in vitro release, and cytotoxicity studies. PS, PDI, and ZP had significant responses, while EE% was insignificant. The suggested models were quadratic with high fitting. Optimized NPs showed PS = 110.31 ± 1.02 nm, PDI = 0.331 ± 0.029, ZP = −23.94 ± 1.64 mV, and EE% = 95.4 ± 2.56%. Molecular modeling indicated hydrophobic and electrostatic interactions between CA and CS, accounting for the high EE%. Almost spherical particles were realized with a sustained CA release pattern. Optimized NPs effectively suppressed the growth of MCF-7 cell lines by scoring the lowest IC50 = 78.45 ± 1.7 µg/mL. A novel combination of bioinspired-derived materials was developed for use in breast cancer treatment.

Green and Enantioselective Synthesis via Cascade Biotransformations: From Simple Racemic Substrates to High-Value Chiral Chemicals.

Asymmetric synthesis of chiral chemicals in high enantiomeric excess (ee) is pivotal to the pharmaceutical industry, but classic chemistry usually requires multi-step reactions, harsh conditions, and expensive chiral ligands, and sometimes suffers from unsatisfactory enantioselectivity. Enzymatic catalysis is a much greener and more enantioselective alternative, and cascade biotransformations with multi-step reactions can be performed in one pot to avoid costly intermediate isolation and minimise waste generation. One of the most attractive applications of enzymatic cascade transformations is to convert easily available simple racemic substrates into valuable functionalised chiral chemicals in high yields and ee. Here, we review the three general strategies to build up such cascade biotransformations, including enantioconvergent reaction, dynamic kinetic resolution, and destruction-and-reinstallation of chirality. Examples of cascade transformations using racemic substrates such as racemic epoxides, alcohols, hydroxy acids, etc. to produce the chiral amino alcohols, hydroxy acids, amines, and amino acids are given. The product concentration, ee, and yield, scalability, and substrate scope of these enzymatic cascades are critically reviewed. To further improve the efficiency and practical applicability of the cascades, enzyme engineering to enhance catalytic activities of the key enzymes using the latest microfluidics-based ultrahigh-throughput screening and artificial intelligence-guided directed evolution could be a useful approach.

(Invited) Introducing Selectivity into Electrochemical Reactions: From Solution to Surfaces

Induction of asymmetry into electrosynthetic reactions has taken off in recent years for the electrochemical community. As of late most transformations have focused on either simple electrochemical oxidations or reductions, such as the reduction of various ketones to chiral alcohol feedstock molecules, or transition metal cross coupling reactions. At the same time, there has been little effort to introduce asymmetry into cyclization reactions that capitalize on highly reactive radical ion intermediates to accomplish umpolung-type transformations or to fully take advantage of electrode surfaces for manipulating the selectivity of synthetically more complex transformations like transition metal cross coupling reactions. In the case more complex electrochemical transformations, many of the reactions studied have led to either high ee and low yield or low ee and high yield. With this in mind, we are looking new approaches for introducing selectivity into electrochemical transformations by taking advantage of high yielding cathodic cyclization reactions and the Heck reaction. The influence of chiral electrolytes, chiral catalysts and mediators, and modified electrode surfaces on these transformations is being explored with a particular emphasis on both the induction of asymmetry into the reactions and the use of remote functionality in the molecules as a control element. This presentation to be given will detail our progress in these areas.

Capecitabine-loaded NLC for Breast Cancer Treatment: Preparation, Characterization, and In vitro Evaluation.

Cancer treatment often involves the use of potent antineoplastic drugs like Capecitabine [CAP], which can lead to serious toxicities. There is a need for dosage forms to manage these toxicities that can deliver the medication effectively to the target site while maintaining therapeutic efficacy at lower doses. To achieve the aforesaid objective, NLC containing capecitabine [NANOBIN] was prepared and evaluated. Different formulations of NANOBIN, denoted as CaTS, CaT1S, CaT2S, CaTS1, and CaTS2, were designed and evaluated to improve drug delivery and therapeutic outcomes. The NANOBIN formulations were prepared using the hot homogenization method. The characterization of these formulations was conducted based on various parameters such as particle size, Polydispersity Index [PDI], Zeta Potential [ZP], Transmission Electron Microscopy [TEM] imaging, and Encapsulation Efficiency [EE]. In vitro evaluations included stability testing, release studies to assess drug release kinetics, and a cytotoxicity assay [MTT assay] to evaluate the efficacy of these formulations against human breast cancer cells [MCF-7]. The characterization results revealed that all NANOBIN formulations exhibited particle sizes ranging from 65 to 193 nm, PDI values within the range of 0.26-0.37, ZP values between 46.47 to 61.87 mV [-ve], and high EE percentages ranging from 94.121% to 96.64%. Furthermore, all NANOBIN formulations demonstrated sustained and slow-release profiles of CAP. The MTT assay showed that the NANOBINs exhibited significantly enhanced cytotoxic efficacy, approximately 10 times greater than free CAP when tested on MCF-7 cells. These findings indicate the potential of NANOBINs to deliver CAP effectively to the target site, enabling prolonged drug availability and enhanced therapeutic effects at lower doses. The study demonstrates that NANOBINs can effectively deliver CAP to target sites, prolonging drug exposure and enhancing therapeutic efficacy while reducing the required dose. Further studies are necessary to validate these findings and establish NANOBINs as a preferred treatment option for cancer therapy.

Candidaantarctica Lipase B mediated kinetic resolution: A sustainable method for chiral synthesis of antiproliferative β-lactams

Biocatalysis is a valuable industrial approach in active pharmaceutical ingredient (API) manufacturing for asymmetric induction and synthesis of chiral APIs. Herein, we investigated synthesis of a panel of microtubule-destabilising antiproliferative β-lactam enantiomers employing a commercially available immobilised Candida antarctica lipase B enzyme together with methanol and MTBE. The β-lactam ring remained intact during chiral kinetic resolution reactions, plausibly due to a bulky N-1 phenyl substituent on the β-lactam ring substrate. The predominant reaction mediated by CAL-B was methanol catalysed conversion of the β-lactam 3-acetoxy substituent to a 3-hydroxyl group, with preferential methanolysis of the 3S, 4S enantiomer. The unreacted substrate underwent progressive enantioenrichment to the 3R, 4R enantiomer. Substitution patterns on the B ring C3 meta position of the β-lactam scaffold greatly affected the rate of reaction. Halo substituents (fluoro-, chloro- and bromo-) reduced the rate of conversion compared to unsubstituted analogues, which in turn increased enantiomeric excess (ee). Ee values up to 86 % for the 3S, 4S 3-hydroxyl enantiomer were achieved. A double resolution approach for unreacted substrate yielded high ee values (>99 %) for the 3R, 4R 3-acetoxy enantiomer. CAL-B mediated methanolysis is a more sustainable method for resolution of racemic antiproliferative β-lactams compared to a previous technique of chiral diastereomeric resolution. Yields of β-lactams obtained using CAL-B are far superior than previously described, which will facilitate progression toward pre-clinical and clinical development. Biocatalysis is a useful tool in the toolbox of the medicinal chemist.

Eating behavior and dietary practices are associated with age, sex, body mass index, and body fat in individuals with type 2 diabetes and/or hypertension in Brazil

Type 2 diabetes (T2DM), hypertension, and obesity are major contributors to global mortality. This study aimed to evaluate eating behavior and dietary practices among individuals with T2DM and/or hypertension, examining their associations with sociodemographic and anthropometric characteristics. We hypothesized that these factors may contribute to body mass index (BMI) and body fat (BF) levels in these individuals. In a cross-sectional study, adults/older individuals diagnosed with T2DM and/or hypertension were included. Eating behavior was evaluated via Three-factor Eating Questionnaire-R21. Dietary practices were assessed using the Dietary Guidelines for the Brazilian Population (DGBP) questionnaire. Poisson regression examined associations between eating behaviors, dietary practices, and sociodemographic factors. Linear regressions were employed to analyze relationships between eating behavior, dietary practices, BMI, and BF. The study included 275 primarily female (70.5%) participants under 60 years old (54.2%). Male and older participants had a lower prevalence of high scores in the 'emotional eating' (EE; PR: 0.40 [0.25;0.63]) and 'uncontrolled eating' (UE; PR: 0.68 [0.50;0.92]) domains. In contrast, older patients had a higher prevalence of adherence to the DGBP recommendations (PR:1.53 [1.20;1.94]). A positive association was observed between high EE (β:3.71 [1.98;5.44]) and UE (β:2.85 [1.15;4.55]) scores and BMI, whereas higher dietary practice scores (β:-2.19 [-3.88;-0.50]) were negatively associated with BMI. High EE (β:2.20 [0.38;4.02]) and UE (β:1.92 [0.17;3.67]) scores were positively associated with BF regardless of the confounding factors included. Higher scores on the dietary practices were inversely associated with BF (β:-1.94 [-3.67;-0.21]). Understanding dietary behaviors and practices can facilitate a more comprehensive and effective treatment approach.

Screening, characterization and mechanism of a potential stabiliser for nisin nanoliposomes with high encapsulation efficiency

The encapsulation efficiency (EE%) reflects the amount of bioactive components that can be loaded into nanoliposomes. Obtaining a suitable nanoliposome stabiliser may be the key to improving their EE%. In this study, three polyphenols were screened as stabilisers of nanoliposomes with high nisin EE%, with curcumin nanoliposomes (Cu-NLs) exhibiting the best performance (EE% = 95.94%). Characterizations of particle size, PDI and zeta potential indicate that the Cu-NLs had good uniformity and stability. TEM found that nisin accumulated at the edges of the Cu-NLs' phospholipid layer. DSC and FT-IR revealed that curcumin was involved in the formation of the phospholipid layer and altered its structure. FT-IR and molecular docking simulations indicate that the interactions between curcumin and nisin are mainly hydrogen bonding and hydrophobic. In whole milk, Cu-NLs effectively protected nisin activity. This study provides an effective strategy for improving the EE% of nanoliposomes loaded with nisin and other bacteriocins.

α-Amino Acid Synthesis by 1,3-Nitrogen Migration: An Update

AbstractAn improved practical and efficient procedure for the synthesis of non-racemic unnatural α-amino acids through a stereocontrolled rearrangement is reported. Carboxylic acids are converted into azanyl esters RCO2NHBoc followed by an iron-catalyzed 1,3-nitrogen migration to provide non-racemic α-amino acids in an asymmetric (α-monosubstituted α-amino acids) or enantioconvergent fashion (α,α-disubstituted α-amino acids). Under optimized conditions using a fluorinated chiral iron catalyst and 2,2,6,6-tetramethylpiperidine as the base in a solvent mixture of 1,2-dichlorobenzene and CHCl3, enantioselectivities of up to 98% ee were obtained. Such high ee values are important for practical purposes, allowing the direct use of many of the obtained N-Boc-protected α-amino acids for subsequent applications.