Benzocaine Research Articles

Fresh Carrier for an Old Topical Local Anesthetic: Benzocaine in Nanostructured Lipid Carriers.

Nanostructured lipid carriers (NLC) have emerged as innovative drug delivery systems, offering distinct advantages over other lipid-based carriers, such as liposomes and solid lipid nanoparticles. Benzocaine (BZC), the oldest topical local anesthetic in use, undergoes metabolism by pseudocholinesterase, leading to the formation of p-aminobenzoic acid, a causative agent for allergic reactions associated with prolonged BZC usage. In order to mitigate adverse effects and enhance bioavailability, BZC was encapsulated within NLC. Utilizing a 23 factorial design, formulations comprising cetyl palmitate (solid lipid), propylene glycol monocaprylate (liquid lipid), and Pluronic F68 as surfactants were systematically prepared, with variations in the solid/liquid lipid mass ratios (60:40-80:20%), total lipid contents (15-25%), and BZC concentrations (1-3%). The optimized formulation underwent characterization by dynamic light scattering, differential scanning calorimetry, Raman imaging, X-ray diffraction, small-angle neutron scattering, nanotracking analysis, and transmission electron microscopy (TEM)/cryo-TEM, providing insights into the nanoparticle structure and the incorporation of BZC into its lipid matrix. NLCBZC exhibited a noteworthy encapsulation efficiency (%EE = 96%) and a 1 year stability when stored at 25 °C. In vitro kinetic studies and in vivo antinociceptive tests conducted in mice revealed that NLCBZC effectively sustained drug release for over 20 h and prolonged the anesthetic effect of BZC for up to 18 h. We therefore propose the use of NLCBZC to diminish the effective anesthetic concentration of benzocaine (from 20 to 3% or less), thus minimizing allergic reactions that follow the topical administration of this anesthetic and, potentially, paving the way for new routes of BZC administration in pain management.

Studies of spectroanalytical and the biological effectiveness of the Azo compound (J25) prepared from Ethyl p-aminobenzoate

Studies of spectroanalytical and the biological effectiveness of the Azo compound (J25) prepared from Ethyl p-aminobenzoate

Synthesis, characterization and analytical study of new azo ligand driven from benzocaine and its metal complexes

The synthesis and spectrum of of a new azo ligand derived from acetylacetone and benzocaine (Ethyl p-aminobenzoate)). Spectral investigations such as 1H NMR,FT.IR, 13C-NMR and Mass spectra were performed to investigate the azo dye ligand's structure. Several physiochemical approaches, FT-IR, electronic spectra, molar conductivity, atom absorption, and magnetic susceptibility were used to identify new complexes with CO(II), and Zn(II) ions Complexes that are all 1:2 [M:L] were formed using the procedures described, and an tetrahedral geometry with sp3 hybridization. At several pH ranges (2–12), the electronic spectra of these azo dyes have been examined in terms of their acid–base properties, which included determining their isosbestic points and protonation and ionization constants. In the other study, azodye were used as an inductor for acid-base titration.

Novel Microemulsion Containing Benzocaine and Fusidic Acid Simultaneously: Formulation, Characterization, and In Vitro Evaluation for Wound Healing

Modern drug carrier technologies, such as microemulsions with small droplet sizes and high surface areas, improve the ability of low water solubility active ingredients to permeate and localize. The goal of this study was to create microemulsion formulations for wound healing that contained both fusidic acid (FA), an antibacterial agent, and benzocaine (BNZ), a local anesthetic. Studies on characterization were carried out, including viscosity, droplet size, and zeta potential. The drug-loaded microemulsion had a stable structure with –3.014 ± 1.265 mV of zeta potential and 19.388 ± 0.480 nm of droplet size. In both in vitro release and ex vivo permeability studies, the microemulsion was compared with Fucidin cream and oily BNZ solution. According to the drug release studies, BNZ release from the microemulsion and the BNZ solution showed a similar profile (p > 0.05), while FA release from the microemulsion had a higher drug release compared to Fucidin cream (p < 0.001). The microemulsion presented lower drug permeation (p > 0.05) for both active ingredients, on the other hand, provided higher drug accumulation compared to the control preparations. Moreover, according to the results of in vitro wound healing activity, the microemulsion indicated a dose-dependent wound healing potential with the highest wound healing activity at the highest concentrations. To the best of our knowledge, this developed BNZ- and FA-loaded microemulsion would be a promising candidate to create new opportunities for wound healing thanks to present the active ingredients, which have low water solubility, in a single formulation and achieved higher accumulation than control preparations.Graphical

Plant Growth Promotion and Plant Disease Suppression Induced by Bacillus amyloliquefaciens Strain GD4a.

Botrytis cinerea, the causative agent of gray mold disease (GMD), invades plants to obtain nutrients and disseminates through airborne conidia in nature. Bacillus amyloliquefaciens strain GD4a, a beneficial bacterium isolated from switchgrass, shows great potential in managing GMD in plants. However, the precise mechanism by which GD4a confers benefits to plants remains elusive. In this study, an A. thaliana-B. cinerea-B. amyloliquefaciens multiple-scale interaction model was used to explore how beneficial bacteria play essential roles in plant growth promotion, plant pathogen suppression, and plant immunity boosting. Arabidopsis Col-0 wild-type plants served as the testing ground to assess GD4a's efficacy. Additionally, bacterial enzyme activity and targeted metabolite tests were conducted to validate GD4a's potential for enhancing plant growth and suppressing plant pathogens and diseases. GD4a was subjected to co-incubation with various bacterial, fungal, and oomycete pathogens to evaluate its antagonistic effectiveness in vitro. In vivo pathogen inoculation assays were also carried out to investigate GD4a's role in regulating host plant immunity. Bacterial extracellular exudate (BEE) was extracted, purified, and subjected to untargeted metabolomics analysis. Benzocaine (BEN) from the untargeted metabolomics analysis was selected for further study of its function and related mechanisms in enhancing plant immunity through plant mutant analysis and qRT-PCR analysis. Finally, a comprehensive model was formulated to summarize the potential benefits of applying GD4a in agricultural systems. Our study demonstrates the efficacy of GD4a, isolated from switchgrass, in enhancing plant growth, suppressing plant pathogens and diseases, and bolstering host plant immunity. Importantly, GD4a produces a functional bacterial extracellular exudate (BEE) that significantly disrupts the pathogenicity of B. cinerea by inhibiting fungal conidium germination and hypha formation. Additionally, our study identifies benzocaine (BEN) as a novel small molecule that triggers basal defense, ISR, and SAR responses in Arabidopsis plants. Bacillus amyloliquefaciens strain GD4a can effectively promote plant growth, suppress plant disease, and boost plant immunity through functional BEE production and diverse gene expression.

Does the anesthetic tricaine methanesulfonate (MS-222) distort oxidative status parameters in tadpoles?

The effect of anesthesia/euthanasia with ethyl 3-aminobenzoate methanesulfonate (MS-222) on the oxidative status of Hyla arborea tadpoles was examined to determine whether the use of the anesthetic can confound the experimental results of the oxidative stress-based investigation. The experiment was conducted on two groups of tadpoles reared at different temperatures to produce differences in antioxidant capacity between the groups. After development at different temperatures (20 °C and 25 °C), the animals were exposed to different concentrations of MS-222 (0, 0.1, 1, and 5 g/L) for 15 min. The higher temperature decreased catalase activity, glutathione and protein carbonyl levels and increased glutathione reductase activity. The glutathione level and glutathione/thiol-related parameters were significantly changed after MS-222 exposure. However, individuals from the different temperature groups responded differently to the tested anesthetic, pointing to the possible influence of the initial levels of antioxidant capacity. The analysis of the interaction between the factors (temperature and MS-222) confirmed that the anesthetic can confound the results regarding the effects of temperature on the oxidative status parameters. The concentration of 0.1 g/L MS-222 had the lowest influence on the alterations in oxidative status and the results of the effect of temperature. A brief review of the current literature on the use of MS-222 in tadpoles made clear the absence of precise information on anesthetic concentration and exposure time. Similar studies should be repeated and extended to other amphibian species and other factors of interest to provide better guidance on tadpole anesthesia/euthanasia for future experiments that consider oxidative status parameters.

Mesophase analysis, DFT calculation and microbial activity of a novel mesomorphic homologous series with ethyl 4-aminobenzoate

A novel homologous series of cinnamoyl ester comprising of elven (C1 to C16) homologues liquid crystal (LC) samples have been synthesized and characterized using instrumental methods (spectral and thermal) of analysis and DFT approach. As results, middle ordered melting type of series with exhibition of nematic mesophase were observed. The observed mesogenic properties and transition temperature are affected by the size of alkyl chains that shows mesomorphism is susceptible to molecular structure. The prepared LCs of cinnamoyl ester derivatives were further examined for their biological activities and the obtained results indicates a good biological potential for the studied LC materials.

Comparative characteristics of different methods for electrophoretic determination of mono- and disaccarides using derivatization

The following variants of electrophoretic determination of sugars with prior derivatization are considered in the article: reductive amination using p-aminobenzoic acid ethyl ester (ABEE) and condensation with 1-phenyl-3-methyl-5-pyrazolone (PMP). Derivatization products were separated using capillary electrophoresis in both zone and micellar modes, and comparative estimate characteristics were obtained. The best efficiency (ca. 650 thousand theoretical plates), selectivity (2.1–2.4), and LOD (0.8–2.9 μg/mL) was observed for the separation of reductive amination products using micellar electrokinetic chromatography (MEKC). Optimization of derivatization conditions was performed for the reductive amination using the central composite experiment design. Additionally, LOD was lowered by the sample intracapillary concentration in sweeping mode, and sample enhancement factors (SEF) of 13–19 were achieved. A proof-of-concept possibility of the intracapillary reductive amination ensuring electrophoretic mobility of the derivatization reagent using detergent micelles as carrying agents was demonstrated. Both derivatization methods were applied for the analysis of baby food.

Transcaruncular double injection technique for peribulbar anesthesia in vitreoretinal surgery.

Local anesthesia is commonly adopted in vitreoretinal surgery to reach painless and akinesia surgical condition. Currently, peribulbar anesthesia (PBA) and subtenonian injection (STN) are the most widely used methods. We propose a transcaruncular double injection peribulbar technique (TRS) and aim to compare it with both standard PBA and STN injections. A total of 105 patients underwent either TRS or PBA or STN. Numerical Rating Scale (NRS) was used to assess pre, post and intraoperative pain. Best akinesia score, onset and duration of akinesia were evaluated by two independent graders. The need for supplementary injection was also registered. TRS group was characterized by a lower intraoperative NRS variation and absolute NRS score both at the beginning of surgery (p 0.046), after 30 minutes (p 0.032) and at the end of surgery (p 0.002) compared to the other groups. TRS group also showed better akinesia score (p 0.004), fastest onset (p 0.002) and longer duration (p 0.042) compared to both PBA ad STN. No injection related complications were reported in the 3 groups. the newly proposed transcaruncular PBA provided superior pain control and akinesia level with no additional adverse events.

Sensitive electrochemical detection of benzocaine based on hollow carbon nanobowl modified electrode

Benzocaine (BZC) is a widely used anaesthetic drug coupled with multiple undesirable side effects, thus developing sensitive method for its detection is of great importance; meanwhile, hollow carbon nanospheres (HCS) have received intense interests in electroanalysis resulted from its unique merits, but the related close structures restrain the availability factor of the internal surfaces, hence suppressing their analytical performance. In this work, a novel nanomaterial with open structure, hollow carbon nanobowl (HCB) was prepared and adopted as the electrode material for fabricating a highly sensitive electrochemical sensor of BZC. The obtained results revealed the as-prepared HCB can display more superior sensing performance than conventional HCS. After optimizing various experimental conditions including the modified amount of HCB, accumulation time and the buffer pH value, the detection of BZC was performed at HCB modified electrode, and a considerably low detection limit (4.0 nM) coupled with high sensitivity (2.1527 μA μM−1) was obtained. In addition, the further experiments demonstrated that the HCB modified electrode possesses superior capability in repeatability, stability, selectivity and practical application. It’s thus expected that the as-designed HCB-based sensing platform has important application for BZC and other targets detection.

Hollow-architected Co3O4 for enhancing Oxone activation to eliminate an anesthetic, benzocaine, from water: A structure-property investigation with degradation pathway and eco-toxicity

BackgroundAs the most widely-used oral anesthetic, benzocaine (BZC), is increasingly detected in municipal wastewater and regarded as an emerging contaminant. Thus, it would be highly imperative to develop useful methods to eliminate BZC from water. However, very few studies have been ever reported, and only photocatalysis of BZC was attempted. Therefore, this present study aims to be the first study of developing the sulfate-radical-based chemical oxidation technology (SR-COT) for degrading BZC. MethodsFor establishing a useful SR-COT, the oxidant, Oxone, is then adopted and a facile nanostructured Co3O4 is then developed for maximizing catalytic activities of Oxone activation by creating a hollow fluffy Co3O4 nanostructure using CoMOF as a template, followed by a carving-architected treatment to afford the hollow fluffy Co3O4 (HFCC). Significant findingsIn comparison to the solid (non-hollow) Co3O4 (SCC), HFCC possesses not only the excellent textural properties, but also superior electrochemical properties and highly reactive surfaces, making HFCC exhibit the significantly higher catalytic activity than SCC as well as traditional Co3O4 nanoparticle in activating Oxone to degrade BZC. The density function theory calculation is performed to investigate the degradation pathway, and the corresponding eco-toxicity is also studied to realize the degradation implication of BZC by HFCC-activated Oxone.

Atlantic Salmon Gill Epithelial Cell Line (ASG-10) as a Suitable Model for Xenobiotic Biotransformation.

Fish are exposed to xenobiotics in the water. Uptake occurs mainly through the gills, which function as an exchange point with the environment. The gills' ability to detoxify harmful compounds by biotransformation is an essential protection mechanism. The enormous numbers of waterborne xenobiotics requiring ecotoxicological assessment makes it necessary to replace in vivo fish studies with predictive in vitro models. Here, we have characterized the metabolic capacity of the ASG-10 gill epithelial cell line from Atlantic salmon. Inducible CYP1A expression was confirmed by enzymatic assays and immunoblotting. The activities of important cytochrome P450 (CYP) and uridine 5'-diphospho-glucuronosyltransferase (UGT) enzymes were established using specific substrates and metabolite analysis by liquid chromatography (LC) triple quadrupole mass spectrometry (TQMS). Metabolism of the fish anesthetic benzocaine (BZ) in ASG-10 confirmed esterase and acetyl transferase activities through the production of N-acetylbenzocaine (AcBZ), p-aminobenzoic acid (PABA) and p-acetaminobenzoic acid (AcPABA). Moreover, we were able to determine hydroxylamine benzocaine (BZOH), benzocaine glucuronide (BZGlcA) and hydroxylamine benzocaine glucuronide (BZ(O)GlcA) by LC high-resolution tandem mass spectrometry (HRMS/MS) fragment pattern analysis for the first time. Comparison to metabolite profiles in hepatic fractions, and in plasma of BZ-euthanized salmon, confirmed the suitability of the ASG-10 cell line for investigating biotransformation in gills.

A new pyrazine carboxyl derivative and its two d10 metal coordination polymers: Syntheses, characterization, DFT and property

A new pyridazine carboxyl derivative, 1-(3-carboxyphenyl)-5-methyl-4-oxo-1,4-dihydropyrida zine-3-carboxylic acid (C13H10N2O5, Mr = 274.06, abbreviate as H2(3-PDCA)) has been synthesized by ethyl 3-aminobenzoate, its structure was determined by 1H NMR, 13C NMR, FT-IR and X-ray single crystal analysis. According to density functional theory, the reaction sites of title molecule were visualized in molecular electrostatic potential maps plot. Meanwhile, two d10 metal coordination polymers had been constructed by title molecule under solvothermal conditions: [Cd(H2O)(3-PDCA)·2H2O]n (SNUT-10) and {[Zn3(H2O)10(3-PDCA)2][Zn(H2O)2(3-PDCA)2]·8H2O}n (SNUT-11). Single crystal X-ray analysis demonstrates that SNUT-10 features a 2D structure with ligands and metal atoms alternated. SNUT-11 exhibits an 2D unusual double layer architecture. In addition, the fluorescence properties of coordination polymers in the solid state were also investigated at room temperature.

MP44-16 NON-INFECTIOUS ADVERSE EVENTS OF TRANSPERINEAL PROSTATE BIOPSIES PERFORMED UNDER LOCAL ANESTHESIA IN AN OUTPATIENT SETTING: RESULTS FROM THE NORAPP STUDY

You have accessJournal of UrologyCME1 Apr 2023MP44-16 NON-INFECTIOUS ADVERSE EVENTS OF TRANSPERINEAL PROSTATE BIOPSIES PERFORMED UNDER LOCAL ANESTHESIA IN AN OUTPATIENT SETTING: RESULTS FROM THE NORAPP STUDY Maciej Jacewicz, Erik Rud, and Eduard Baco Maciej JacewiczMaciej Jacewicz More articles by this author , Erik RudErik Rud More articles by this author , and Eduard BacoEduard Baco More articles by this author View All Author Informationhttps://doi.org/10.1097/JU.0000000000003290.16AboutPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissionsReprints ShareFacebookLinked InTwitterEmail Abstract INTRODUCTION AND OBJECTIVE: The aim of our study was to examine the feasibility and adverse events of transperineal prostate biopsies (TPBx) performed under local anesthesia (LA) in an outpatient setting. METHODS: Patients with suspicion of prostate cancer were included in this randomized clinical trial. Primary endpoint was examining the role of antibiotic prophylaxis in TPBx. Secondary endpoints were pain during and after the procedure (VAS), hematuria, hematospermia and acute urinary retention (AUR). Patients with a high risk of infection were excluded. Free-hand MRI-TRUS fusion TPBx, using the Koelis Trinity device, were performed in an outpatient setting under LA. 40 ml of 1% Lidocaine and 4 ml Sodium Bicarbonate was injected in the perineal skin, under the prostatic apex, in levator ani bilaterally and along the path of the needle under TRUS guidance. Target biopsies were performed in patients with PIRADS ≥3 on MRI, systematic biopsies were performed in biopsy naïve and MRI negative patients. VAS was reported immediately after biopsy, followup regarding non-infectious adverse events was after 2 weeks and 2 months. Correlation was analyzed using Pearson coefficient. RESULTS: We included 402 patients. Median age was 69 years (IQR 63-74, range: 38-86), PSA 7.0 ng/ml (IQR 4.5-11) and prostate volume (PV) 40 ml (IQR 27-58). Median number of cores was 8 (IQR 6-10). Response rate to the questionnaire was 100% (401/402). Median VAS during the placement of LA was 1 (IQR: 1-2, range 0-8) and VAS during biopsy 1 (IQR:1-2, range: 0-8). Additional LA was required by 10% (40/401). There was a weak correlation between age and VAS during placement of LA (r: -0.293, p: <0.001), age and VAS during biopsy (r: -0.243 p:<0.001) and number of cores and VAS during biopsy (r:0.137, p=0.006). There was no correlation between VAS and PV. Median post-procedural VAS was 0 (IQR: 0-0, range 0-5), 2% (9/401) used analgesics after the procedure. Hematuria was present in 64% (258/401), median duration was 3 days (IQR:2-7, range 1-35). There was a weak correlation between number of cores and hematuria (r:0.180, p:<0.001. Hematospermia was present in 54% (197/366) of patients, median duration was 14 days (IQR:7-21, range 1-49). AUR occurred in two patients (0.5%, 95% CI:0.1-1.8). One suffered a clot retention resolved by single time catheterization, the other was treated with a permanent catheter for a week. CONCLUSIONS: Transperineal prostate biopsies under LA can safely be performed in an outpatient setting with limited discomfort to the patient and few non-infectious adverse events. Source of Funding: Oslo University Hospital © 2023 by American Urological Association Education and Research, Inc.FiguresReferencesRelatedDetails Volume 209Issue Supplement 4April 2023Page: e618 Advertisement Copyright & Permissions© 2023 by American Urological Association Education and Research, Inc.MetricsAuthor Information Maciej Jacewicz More articles by this author Erik Rud More articles by this author Eduard Baco More articles by this author Expand All Advertisement PDF downloadLoading ...

OPIOID FREE GENERAL ANESTHESIA IN CLINICAL PRACTICE - A REVIEW ARTICLE.

Currently, enhanced recovery after surgery (ERAS) protocols are multimodal perioperative care pathways with the goal to achieve early patient recovery after surgery with minimal postoperative complications. According to studies, opioid free general anesthesia has many perioperative benefits and should be part of the ERAS protocols in specific surgical and patient indications. Opioid free general anesthesia is a multimodal balanced technique that is based on the concept that opioids are not used preoperatively or intraoperatively until the patient has aroused. The basic concept of opioid free general anesthesia is intravenous administration of several nonopioid drugs that operate at different pharmacological sites blocking surgical stress and sympathetic activation response. Moreover, current studies have shown that opioid free anesthesia is a technique which satisfactorily controls postoperative pain as the fifth vital sign, and has minimal side effects and better patient recovery with the same surgical conditions as general multimodal balanced anesthesia. However, further research is needed.

Exposure to airborne PM&lt;sub&gt;2.5&lt;/sub&gt; chemical exposome increases heart rate of middle- and old-aged populations

&lt;p&gt;Previous studies have rarely focused on the effects of industrial chemicals on heart rate. There is also a lack of epidemiological investigations to elucidate the mixture effects of complex components of fine particulate matter (PM&lt;sub&gt;2.5&lt;/sub&gt;) on cardiovascular health and identify the key toxic components. Here, a population health-oriented methodology is established to quantify mixed effects of airborne PM&lt;sub&gt;2.5&lt;/sub&gt; chemical exposome and identify key components. This methodology was applied to a cross-sectional study to elucidate the mixture effect of industrial chemical components of PM&lt;sub&gt;2.5&lt;/sub&gt; on the heart rate of middle- and old-aged populations (including 373 people from seven Chinese cities) and further identify key chemical components for the effect. Exposure to seven groups of industrial chemicals, including phthalate esters (PAEs), adipate esters (AEs), benzothiazoles and benzotriazoles (BTHs &amp; BTRs), benzophenones and benzoates (BZPs &amp; BZAs), bisphenols (BPs), alkyl organophosphate esters (alkyl-OPEs) and aryl organophosphate esters (aryl-OPEs), was observed to significantly increase the heart rate of study participants. Seven chemicals, including dimethyl isophthalate (DMiP), di-iso-nonyl adipate (DiNA), 2-(2H-benzotriazol-2-yl)-4,6-di-tert-pentylphenol (UV-328), ethyl-4-aminobenzoate (EAB), bisphenol F (BPF), triethyl phosphate (TEP) and tricresyl phosphate (TCrP), were identified as the key components driving the adverse effect on heart rate. Our study highlights the cardiovascular hazards of airborne PM&lt;sub&gt;2.5&lt;/sub&gt; chemical exposome.&lt;/p&gt;

Supramolecular assembly of benzocaine bearing cyclodextrin cavity via host-guest complexes on polyacrylonitrile as an electrospun nanofiber

Nanofibers (NFs) can be encapsulated with cyclodextrins (CDs) based host-guest complexes (HCs) in order to enable many biological applications. Here, benzocaine (BNZ) forms HCs with β-cyclodextrin (β-CD) that are co-precipitated and further added to polyacrylonitrile (PAN) solution for making BNZ:β-CD-HCs/PAN NFs material with the aid of electrospinning technique. The marginal increase in absorbance and fluorescence intensity along with the shift in spectral maxima of BNZ in the presence of β-CD suggested the host-guest interaction between BNZ and β-CD. NFs showed a uniform and clean morphology in SEM images and interestingly, the ICs revealed that significantly thinner in terms of average fiber diameter (AFD) than those of free BNZ on PAN medium. BNZ molecule is completely included in the PAN surface as the result of NFs and thus, the original sharp peaks for the BNZ have vanished and the peaks are much broader for the BNZ and BNZ:β-CD-HCs. BNZ is also found to be a good candidate for anti-inflammatory, anti-oxidant, and anti-diabetic. The results showed an improved activity when it is in the form of HCs on a PAN medium. Making HCs of drugs could be significant in biological applications.

Synthesis, Characterization and Antioxidant Evaluation of Some Tetrazole Derivatives

The present study introduces the synthesis of two series of tetrazole derivatives. Firstly, monosubstituted S1 was prepared by the reaction of ethyl 4-aminobenzoate with an amount of sodium azide and triethyl orthoformate in hot glacial acetic acid. Then, ethyl 4-(1H-tetrazol-1-yl) benzoate S1 was treated with a solution of hydrazine hydrate to prepare acetohydrazide S2. After that, tetrazole derivatives S3-S4 were prepared via the reaction of acetohydrazide S2 with various aromatic aldehydes. Secondly, compound 1,5-disubstituted tetrazole S5 was prepared from the reaction of aryl isothiocyanate with sodium azide in water presence. Then alkylation to compound S5 was made with ethyl chloroacetate to produce S6. In the next step, S6 was reacted with hydrazine hydrate to get acetohydrazide S7. Moreover, the produced S7 was reacted with some aromatic aldehydes for the synthesis of S8-S10. The structures of synthesized compounds were confirmed by the different available spectral methods, i.e., FTIR, 1H-NMR and 13C-NMR spectroscopy. The antioxidant activity of the synthesized compounds was evaluated by the use of 2,2-diphenyl-1-picrylhydrazyl. The results showed that compound S10 has the highest value as radical scavenging among the synthesized compounds.

Hydrogen-bond based charge bridge in a heterojunction system for the synergistic degradation and detoxification of two PPCPs

The use of photocatalysis to remove pharmaceuticals and personal care products (PPCPs) is emerging as a promising method, but few studies have investigated the simultaneous degradation of multiple PPCPs. Here, we constructed a hydrogen-bonded bridged MIL-101(Cr)–NH2/BiOCl-OH (MCN/BOCH) system to degrade sulfamethoxazole and ethyl p-aminobenzoate alone or in combination. The MCN/BOCH system effectively removed two PPCPs under visible light and exerted a synergistic effect on degrading the combined pollutants. Meanwhile, the degradation products of the mixture changed significantly compared with that of a single pollutant, and the toxicity of the composite pollutants was significantly reduced through the combined effect of synergistic degradation. The bridging of hydrogen bonds effectively accelerated charge transfer at the heterojunction interface under visible light. Moreover, the separated redox side of the MCN/BOCH heterojunction system and the electron donor and acceptor effect of the two PPCPs significantly enhanced the synergistic photocatalytic degradation performance. This work might be useful for controllable designs of hydrogen-bonded photocatalysts for the treatment of complex PPCP pollution.

Evaluating Novel Agarose-Based Buccal Gels Scaffold: Mucoadhesive and Pharmacokinetic Profiling in Healthy Volunteers.

Agarose (AG) forms hydrocolloid in hot water and possesses a noteworthy gel strength. However, no reasonable scientific work on investigating the mucoadhesive character of AG has been reported. Therefore, the current study was designed to develop AG and carbopol (CP) based buccal gel scaffold for simultaneous release of benzocaine (BZN) and tibezonium iodide (TIB). Gels’ scaffold formulations (F1–F12) were prepared with varied concentrations (0.5–1.25% w/v) of AG and CP alone or their blends (AG-CP) using homogenization technique. The prepared formulations were characterized for solid-state, physicochemical, in vitro, ex vivo, and in vivo mucoadhesive studies in healthy volunteers. The results showed that mucoadhesive property of AG was concentration dependent but improved by incorporating CP in the scaffolds. The ex vivo mucoadhesive time reached >36 h when AG was used alone or blended with CP at 1% w/v concentration or above. The optimized formulation (F10) depicted >98% drugs release within 8 h and was also storage stable up to six months. The salivary concentration of BZN and TIB from formulation F10 yielded a Cmax value of 9.97 and 8.69 µg/mL at 2 and 6 h (tmax), respectively. In addition, the FTIR, PXRD, and DSC results confirmed the presence of no unwanted interaction among the ingredients. Importantly, the mucoadhesive study performed on healthy volunteers did not provoke any signs of inflammation, pain, or swelling. Clearly, it was found from the results that AG-CP scaffold provided better mucoadhesive properties in comparison to pure AG or CP. Conclusively, the developed AG based mucoadhesive drug delivery system could be considered a potential alternative for delivering drugs through the mucoadhesive buccal route.