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1.
Int J Mol Sci ; 25(9)2024 Apr 25.
Article in English | MEDLINE | ID: mdl-38731902

ABSTRACT

Investigation of chiroptical polymers in the solution phase is paramount for designing supramolecular architectures for photonic or biomedical devices. This work is devoted to the case study of poly(propylene oxide) (PPO) optical activity in several solvents: benzonitrile, carbon disulfide, chloroform, ethyl acetate, and p-dioxane. To attain information on the interactions in these systems, rheological testing was undertaken, showing distinct variations of the rheological parameters as a function of the solvent type. These aspects are also reflected in the refractive index dispersive behavior, from which linear and non-linear optical properties are extracted. To determine the circular birefringence and specific rotation of the PPO solutions, the alternative method of the channeled spectra was employed. The spectral data were correlated with the molecular modeling of the PPO structural unit in the selected solvents. Density functional theory (DFT) computational data indicated that the torsional potential energy-related to the O1-C2-C3-O4 dihedral angle from the polymer repeating unit-was hindered in solvation environments characterized by high polarity and the ability to interact via hydrogen bonding. This was in agreement with the optical characterization of the samples, which indicated a lower circular birefringence and specific rotation for the solutions of PPO in ethyl acetate and p-dioxane. Also, the shape of optical rotatory dispersion curves was slightly modified for PPO in these solvents compared with the other ones.


Subject(s)
Solvents , Solvents/chemistry , Propylene Glycols/chemistry , Polypropylenes/chemistry , Polymers/chemistry , Models, Molecular , Rotation , Hydrogen Bonding , Rheology
2.
J Neuroimmune Pharmacol ; 19(1): 18, 2024 May 11.
Article in English | MEDLINE | ID: mdl-38733535

ABSTRACT

Suppression of immune functions can be elicited by behavioural conditioning using drugs such as cyclosporin A or rapamycin. Nevertheless, little is known about the underlying mechanisms and generalisability of this phenomenon. Against this background, the present study investigated whether the pharmacological properties of fingolimod (FTY720), an immunosuppressive drug widely applied to treat multiple sclerosis, can be conditioned in rats by means of taste-immune associative learning. For this purpose, a conditioned taste avoidance paradigm was used, pairing the presentation of a novel sweet drinking solution (saccharin or sucrose) as conditioned stimulus (CS) with therapeutically effective doses of FTY720 as unconditioned stimulus (US). Subsequent re-exposure to the CS at a later time point revealed that conditioning with FTY720 induced a mild conditioned taste avoidance only when saccharin was employed as CS. However, on an immunological level, neither re-exposure with saccharin nor sucrose altered blood immune cell subsets or splenic cytokine production. Despite the fact that intraperitonally administered FTY720 could be detected in brain regions known to mediate neuro-immune interactions, the present findings show that the physiological action of FTY720 is not inducible by mere taste-immune associative learning. Whether conditioning generalises across all small-molecule drugs with immunosuppressive properties still needs to be investigated with modified paradigms probably using distinct sensory CS. Moreover, these findings emphasize the need to further investigate the underlying mechanisms of conditioned immunomodulation to assess the generalisability and usability of associative learning protocols as supportive therapies in clinical contexts.


Subject(s)
Fingolimod Hydrochloride , Immunosuppressive Agents , Animals , Fingolimod Hydrochloride/pharmacology , Rats , Immunosuppressive Agents/pharmacology , Male , Rats, Wistar , Leukocytes/drug effects , Avoidance Learning/drug effects , Conditioning, Classical/drug effects , Propylene Glycols/pharmacology , Taste/drug effects , Saccharin
3.
ACS Appl Mater Interfaces ; 16(15): 18434-18448, 2024 Apr 17.
Article in English | MEDLINE | ID: mdl-38579182

ABSTRACT

The poor solubility of clotrimazole in the aqueous medium and the uncontrolled removal of the drug-loaded suppository content limit its effectiveness in the treatment of vulvovaginal candidiasis. We present here the aqueous formulations of clotrimazole in the form of non-Newtonian structured fluids, i.e., Bingham plastic or pseudoplastic fluids constructed of hyperbranched polyglycidol, HbPGL, with a hydrophobized core with aryl groups such as phenyl or biphenyl. The amphiphilic constructs were obtained by the modification of linear units containing monohydroxyl groups with benzoyl chloride, phenyl isocyanate, and biphenyl isocyanate, while the terminal 1,2-diol groups in the shell were protected during the modification step, followed by their deprotection. The encapsulation of clotrimazole within internally hydrophobized HbPGLs using a solvent evaporation method followed by water addition resulted in structured fluids formation. Detailed Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) analyses performed for aryl-HbPGLs with clotrimazole revealed the difference in drug compatibility among polymers. Clotrimazole in biphenyl-enriched HbPGL, unlike phenyl derivatives, was molecularly distributed in both the dry and the hydrated states, resulting in transparent formulations. The shear-thinning properties of the obtained fluid formulations make them injectable and thus suitable for the intravaginal application. Permeability tests performed with the usage of the Franz diffusion cell showed a 5-fold increase in the permeability constant of clotrimazole compared to drugs loaded in a commercially available disposable tablet and a 50-fold increase of permeability in comparison to the aqueous suspension of clotrimazole. Furthermore, the biphenyl-modified HbPGL-based drug liquid showed enhanced antifungal activity against both Candida albicans and Candida glabrata that was retained for up to 7 days, in contrast to the phenyl-HbPGL derivatives and the tablet. With their simple formulation, convenient clotrimazole/biphenyl-HbPGL formulation strategy, rheological properties, and enhanced antifungal properties, these systems are potential antifungal therapeutics for gynecological applications. This study points in the synthetic direction of improving the solubility of poorly water-soluble aryl-enriched pharmaceuticals.


Subject(s)
Antifungal Agents , Biphenyl Compounds , Clotrimazole , Propylene Glycols , Clotrimazole/chemistry , Antifungal Agents/chemistry , Biological Availability , Solubility , Water , Tablets
4.
Food Chem ; 449: 139206, 2024 Aug 15.
Article in English | MEDLINE | ID: mdl-38579658

ABSTRACT

Novel aqueous biphasic systems (ABSs) developed with benzyl-based quaternary ammonium salts-deep eutectic solvents (DESs) and polypropylene glycol (PPG) were herein proposed. The liquid-liquid equilibrium and the partitioning behavior of pigments in the systems were addressed. The results suggested that the shorter the carbon chain length of the DES, the easier to form two phases. The analysis of mixed samples showed that the selective separation was achieved in the ABSs, including 99.47% of tartrazine in the DES-rich phase and 98.47% of sudan III in the PPG-rich phase. Additionally, the systems were successfully applied to the extraction of pigments from the actual beverage samples with recoveries ranging from 93.43% to 102.15%. Furthermore, the study on the separation mechanism indicated that the hydrogen bonding played a significant role in the separation process. All the above results highlight the proposed DES/polymer-based ABSs have great advantages in selective and high-performance separation of pigments from beverages.


Subject(s)
Azo Compounds , Beverages , Deep Eutectic Solvents , Polymers , Beverages/analysis , Polymers/chemistry , Deep Eutectic Solvents/chemistry , Propylene Glycols/chemistry , Propylene Glycols/isolation & purification , Coloring Agents/chemistry , Coloring Agents/isolation & purification , Solvents/chemistry , Quaternary Ammonium Compounds/chemistry
5.
Enzyme Microb Technol ; 177: 110438, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38518554

ABSTRACT

Klebsiella pneumoniae can use glucose or glycerol as carbon sources to produce 1,3-propanediol or 2,3-butanediol, respectively. In the metabolism of Klebsiella pneumoniae, hydrogenase-3 is responsible for H2 production from formic acid, but it is not directly related to the synthesis pathways for 1,3-propanediol and 2,3-butanediol. In the first part of this research, hycEFG, which encodes subunits of the enzyme hydrogenase-3, was knocked out, so K. pneumoniae ΔhycEFG lost the ability to produce H2 during cultivation using glycerol as a carbon source. As a consequence, the concentration of 1,3-propanediol increased and the substrate (glycerol) conversion ratio reached 0.587 mol/mol. Then, K. pneumoniae ΔldhAΔhycEFG was constructed to erase lactic acid synthesis which led to the further increase of 1,3-propanediol concentration. A substrate (glycerol) conversion ratio of 0.628 mol/mol in batch conditions was achieved, which was higher compared to the wild type strain (0.545 mol/mol). Furthermore, since adhE encodes an alcohol dehydrogenase that catalyzes ethanol production from acetaldehyde, K. pneumoniae ΔldhAΔadhEΔhycEFG was constructed to prevent ethanol production. Contrary to expectations, this did not lead to a further increase, but to a decrease in 1,3-propanediol production. In the second part of this research, glucose was used as the carbon source to produce 2,3-butanediol. Knocking out hycEFG had distinct positive effect on 2,3-butanediol production. Especially in K. pneumoniae ΔldhAΔadhEΔhycEFG, a substrate (glucose) conversion ratio of 0.730 mol/mol was reached, which is higher compared to wild type strain (0.504 mol/mol). This work suggests that the inactivation of hydrogenase-3 may have a global effect on the metabolic regulation of K. pneumoniae, leading to the improvement of the production of two industrially important bulk chemicals, 1,3-propanediol and 2,3-butanediol.


Subject(s)
Bacterial Proteins , Butylene Glycols , Fermentation , Glycerol , Hydrogenase , Klebsiella pneumoniae , Propylene Glycols , Butylene Glycols/metabolism , Klebsiella pneumoniae/enzymology , Klebsiella pneumoniae/metabolism , Klebsiella pneumoniae/genetics , Propylene Glycols/metabolism , Glycerol/metabolism , Bacterial Proteins/metabolism , Bacterial Proteins/genetics , Hydrogenase/metabolism , Hydrogenase/genetics , Glucose/metabolism , Hydrogen/metabolism , Lactic Acid/metabolism , Lactic Acid/biosynthesis
6.
Article in English | MEDLINE | ID: mdl-38422382

ABSTRACT

Glycidyl esters (GEs) and 3-monochloropropanediol esters (3-MCPDEs) are process contaminants commonly found in refined edible oils which are often added to infant formulas. The Taiwan Food and Drug Administration (TFDA) launched regulations for GEs in infant formulas that went into effect on 1 July 2021. To investigate levels of GEs and 3-MCPDEs in infant formula powder, 45 products were sampled and analysed during 2020-2021. The contents of GEs and 3-MCPDEs in formulas of different brands significantly varied, but their concentrations in all of the formulas complied with European Union (EU) regulations. Infant formulas containing palm oil had significantly higher 3-MCPDE levels in both extracted oils and milk powder than those without palm oil. Concentrations of GEs and 3-MCPDEs in infant formula powder and extracted oils were significantly lower in products from Europe than those from Australia and New Zealand. Infants aged 0-1 years in Taiwan who consumed only infant formula showed a margin of exposure (MoE) exceeding 25,000. Mean consumer exposures to 3-MCPDEs stayed below the tolerable daily intake (TDI), while high exposures at the 95th percentile (P95) exceeded the TDI by 1.7-fold. Herein, we present the changing trends in the risk assessment results of infant formula across various countries in the decade. Implementation of regulations and mitigation strategy effectively reduced the risk of infants being exposed to GEs and 3-MCPDEs through infant formula.


Subject(s)
Infant Formula , Propylene Glycols , alpha-Chlorohydrin , Infant , Humans , Palm Oil , Infant Formula/analysis , alpha-Chlorohydrin/analysis , Esters/analysis , Powders , Taiwan , Food Contamination/analysis , Risk Assessment , Plant Oils/analysis
7.
Microb Cell Fact ; 23(1): 62, 2024 Feb 24.
Article in English | MEDLINE | ID: mdl-38402147

ABSTRACT

BACKGROUND: 1,2-propanediol (1,2-PDO) is widely used in the cosmetic, food, and drug industries with a worldwide consumption of over 1.5 million metric tons per year. Although efforts have been made to engineer microbial hosts such as Corynebacterium glutamicum to produce 1,2-PDO from renewable resources, the performance of such strains is still improvable to be competitive with existing petrochemical production routes. RESULTS: In this study, we enabled 1,2-PDO production in the genome-reduced strain C. glutamicum PC2 by introducing previously described modifications. The resulting strain showed reduced product formation but secreted 50 ± 1 mM D-lactate as byproduct. C. glutamicum PC2 lacks the D-lactate dehydrogenase which pointed to a yet unknown pathway relevant for 1,2-PDO production. Further analysis indicated that in C. glutamicum methylglyoxal, the precursor for 1,2-PDO synthesis, is detoxified with the antioxidant native mycothiol (MSH) by a glyoxalase-like system to lactoylmycothiol and converted to D-lactate which is rerouted into the central carbon metabolism at the level of pyruvate. Metabolomics of cell extracts of the empty vector-carrying wildtype, a 1,2-PDO producer and its derivative with inactive D-lactate dehydrogenase identified major mass peaks characteristic for lactoylmycothiol and its precursors MSH and glucosaminyl-myo-inositol, whereas the respective mass peaks were absent in a production strain with inactivated MSH synthesis. Deletion of mshA, encoding MSH synthase, in the 1,2-PDO producing strain C. glutamicum ΔhdpAΔldh(pEKEx3-mgsA-yqhD-gldA) improved the product yield by 56% to 0.53 ± 0.01 mM1,2-PDO mMglucose-1 which is the highest value for C. glutamicum reported so far. CONCLUSIONS: Genome reduced-strains are a useful basis to unravel metabolic constraints for strain engineering and disclosed in this study the pathway to detoxify methylglyoxal which represents a precursor for 1,2-PDO production. Subsequent inactivation of the competing pathway significantly improved the 1,2-PDO yield.


Subject(s)
Corynebacterium glutamicum , Propylene Glycol , Propylene Glycols , Propylene Glycol/metabolism , Corynebacterium glutamicum/genetics , Corynebacterium glutamicum/metabolism , Pyruvaldehyde/metabolism , Lactates/metabolism , Metabolic Engineering
8.
Spectrochim Acta A Mol Biomol Spectrosc ; 312: 124060, 2024 May 05.
Article in English | MEDLINE | ID: mdl-38402704

ABSTRACT

A green, rapid and sensitive fluorimetric method to quantify levodropropizine (LVP) in human plasma was exploited for the first time. The proposed method adopts LVP's intrinsic fluorescence in distilled water at a detecting emission of 345 nm following excitation at 240 nm. LVP displayed linearity across concentrations ranging from 50 to 1000 ng mL-1, with a detection limit of 0.77 ng mL-1 and a quantification limit of 2.33 ng mL-1. Thorough validation confirmed its reliability, successfully determining LVP in tablets with an average recovery of 98.64 ± 1.07 %. Furthermore, the method's applicability extended to estimate the studied drug in spiked human plasma with excellent obtained percentage recoveries (98.68 ± 1.28-100.14 ± 1.23).


Subject(s)
Plasma , Propylene Glycols , Humans , Spectrometry, Fluorescence/methods , Reproducibility of Results , Fluorometry , Tablets
9.
Perspect Med Educ ; 13(1): 33-43, 2024.
Article in English | MEDLINE | ID: mdl-38343553

ABSTRACT

Coaching is an increasingly popular means to provide individualized, learner-centered, developmental guidance to trainees in competency based medical education (CBME) curricula. Aligned with CBME's core components, coaching can assist in leveraging the full potential of this educational approach. With its focus on growth and improvement, coaching helps trainees develop clinical acumen and self-regulated learning skills. Developing a shared mental model for coaching in the medical education context is crucial to facilitate integration and subsequent evaluation of success. This paper describes the Royal College of Physicians and Surgeons of Canada's coaching model, one that is theory based, evidence informed, principle driven and iteratively and developed by a multidisciplinary team. The coaching model was specifically designed, fit for purpose to the postgraduate medical education (PGME) context and implemented as part of Competence by Design (CBD), a new competency based PGME program. This coaching model differentiates two coaching roles, which reflect different contexts in which postgraduate trainees learn and develop skills. Both roles are supported by the RX-OCR process: developing Relationship/Rapport, setting eXpectations, Observing, a Coaching conversation, and Recording/Reflecting. The CBD Coaching Model and its associated RX-OCR faculty development tool support the implementation of coaching in CBME. Coaching in the moment and coaching over time offer important mechanisms by which CBD brings value to trainees. For sustained change to occur and for learners and coaches to experience the model's intended benefits, ongoing professional development efforts are needed. Early post implementation reflections and lessons learned are provided.


Subject(s)
Education, Medical , Mentoring , Propylene Glycols , Surgeons , Humans , Curriculum
10.
Int J Biol Macromol ; 260(Pt 1): 129497, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38232884

ABSTRACT

A new synergistic flame retardant named Bisiminopropyl trimethoxysilane-1,3,5-triazine-O-bicyclic pentaerythritol phosphate (BTPODE) was synthesized, which is a type of Si/P/N flame retardant. This was accomplished by grafting aminopropyl trimethoxysilane and bicyclic pentaerythritol phosphate onto a triazine ring structure, serving as an intermediate. The structure of BTPODE was determined using nuclear magnetic resonance (1H NMR, 13C NMR, and 31P NMR) and Fourier transform infrared spectroscopy (FT-IR). SEM was used to detect the surface morphology of cotton fabrics, which suggested that BTPODE had been resoundingly stick to cotton fabrics. The flame retardant properties of cotton fabrics were evaluated by measuring the limiting oxygen index (LOI) and conducting vertical flammability experiments. Cotton fabrics with a weight gain of 20.73 % achieved an LOI value of 32.5 %. Thermogravimetric (TG) experiments demonstrated the samples' good thermostability. Furthermore, under nitrogen conditions, the char residue of cotton fabric with a weight gain of 20.73 % was 36.85 %. The cone calorimetry test (CONE) showed a significant reduction in the TSP value, indicating a certain level of smoke suppression performance. Finally, based on the obtained experimental results, the fire-retardant mechanism principle of the flame retardant was deduced.


Subject(s)
Flame Retardants , Propylene Glycols , Silanes , Humans , Triazines/chemistry , Spectroscopy, Fourier Transform Infrared , Phosphates , Weight Gain
11.
Hum Psychopharmacol ; 39(2): e2892, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38193849

ABSTRACT

OBJECTIVE: Fasedienol (PH94B) is a pherine compound formulated as a nasal spray that is hypothesized to regulate olfactory-amygdala circuits of fear and anxiety. Fasedienol's effect on the local electrogram of nasal chemosensory neurons (EGNR) and autonomic nervous system (ANS) responses versus steroidal hormones and controls in healthy adults is reported. METHODS: Eight males and 8 females randomly received aerosolized control (propylene glycol) and study drugs (fasedienol, 17ß-estradiol, progesterone, cortisol, and testosterone, 0.4 µg each in propylene glycol) onto the nasal septum mucosal lining at 30-min intervals over 2 sessions. EGNR was continuously monitored; autonomic parameters were recorded before and after administration. RESULTS: Fasedienol significantly increased EGNR amplitude (males: 5.0 vs. 0.6 mV, p < 0.001; females:5.7 vs. 0.6 mV, p < 0.001), and rapidly reduced respiratory rate (p < 0.05), heart rate (p < 0.01), and electrodermal activity (p < 0.05) versus control. EGNR and ANS responses after steroidal hormone administration were similar to control. 81% reported feeling less tense/more relaxed after receiving fasedienol, but not after receiving either control or steroidal hormones. CONCLUSIONS: Intranasal fasedienol, but not control or steroidal hormones, activated EGNR and rapidly reduced ANS responses, consistent with sympatholytic effects. Combined with subjective reports, results suggest fasedienol may provide acute relief in anxiety conditions.


Subject(s)
Autonomic Nervous System , Nasal Sprays , Adult , Female , Humans , Male , Autonomic Nervous System/physiology , Estradiol , Healthy Volunteers , Propylene Glycols
12.
BMJ Case Rep ; 17(1)2024 Jan 03.
Article in English | MEDLINE | ID: mdl-38171639

ABSTRACT

Fingolimod is a sphingosine-1-phosphate receptor modulator approved as a disease-modifying therapy (DMT) for relapsing-remitting multiple sclerosis (MS). A woman in her 30s was treated with fingolimod for relapsing-remitting MS. After 7 years of treatment, she presented with non-productive cough, night sweats, breathlessness and unintentional weight loss. She had a negative interferon-gamma release assay (IGRA). A high-resolution CT thorax showed innumerable miliary opacities in both lungs. Bronchoalveolar lavage was positive for Mycobacterium tuberculosis complex PCR. An MRI head showed multiple small punctate contrast-enhancing lesions most typical for tuberculomas. We describe the first reported case of disseminated tuberculosis (TB) associated with fingolimod treatment. Patients who are receiving DMT must be closely observed for the development of opportunistic infections, and IGRA results should be interpreted with caution. Screening for latent TB prior to commencing fingolimod should be considered on an individual basis. The management of TB in MS patients on DMT requires an interdisciplinary approach.


Subject(s)
Multiple Sclerosis, Relapsing-Remitting , Multiple Sclerosis , Tuberculosis , Female , Humans , Fingolimod Hydrochloride/adverse effects , Multiple Sclerosis/drug therapy , Immunosuppressive Agents/adverse effects , Propylene Glycols , Sphingosine , Multiple Sclerosis, Relapsing-Remitting/drug therapy
13.
Sci Rep ; 14(1): 1942, 2024 01 23.
Article in English | MEDLINE | ID: mdl-38253598

ABSTRACT

Despite concerns over their safety, e-cigarettes (e-cigs) remain a popular tobacco product. Although nicotine and flavors found in e-cig liquids (e-liquids) can cause harm in the airways, whether the delivery vehicles propylene glycol (PG) and vegetable glycerin (VG) are innocuous when inhaled remains unclear. Here, we investigated the effects of e-cig aerosols generated from e-liquid containing only PG/VG on airway inflammation and mucociliary function in primary human bronchial epithelial cells (HBEC) and sheep. Primary HBEC were cultured at the air-liquid interface (ALI) and exposed to e-cig aerosols of 50%/50% v/v PG/VG. Ion channel conductance, ciliary beat frequency, and the expression of inflammatory markers, cell type-specific markers, and the major mucins MUC5AC and MUC5B were evaluated after seven days of exposure. Sheep were exposed to e-cig aerosols of PG/VG for five days and mucus concentration and matrix metalloproteinase-9 (MMP-9) activity were measured from airway secretions. Seven-day exposure of HBEC to e-cig aerosols of PG/VG caused a significant reduction in the activities of apical ion channels important for mucus hydration, including the cystic fibrosis transmembrane conductance regulator (CFTR) and large conductance, Ca2+-activated, and voltage-dependent K+ (BK) channels. PG/VG aerosols significantly increased the mRNA expression of the inflammatory markers interleukin-6 (IL6), IL8, and MMP9, as well as MUC5AC. The increase in MUC5AC mRNA expression correlated with increased immunostaining of MUC5AC protein in PG/VG-exposed HBEC. On the other hand, PG/VG aerosols reduced MUC5B expression leading overall to higher MUC5AC/MUC5B ratios in exposed HBEC. Other cell type-specific markers, including forkhead box protein J1 (FOXJ1), keratin 5 (KRT5), and secretoglobin family 1A member 1 (SCGB1A1) mRNAs, as well as overall ciliation, were significantly reduced by PG/VG exposure. Finally, PG/VG aerosols increased MMP-9 activity and caused mucus hyperconcentration in sheep in vivo. E-cig aerosols of PG/VG induce airway inflammation, increase MUC5AC expression, and cause dysfunction of ion channels important for mucus hydration in HBEC in vitro. Furthermore, PG/VG aerosols increase MMP-9 activity and mucus concentration in sheep in vivo. Collectively, these data show that e-cig aerosols containing PG/VG are likely to be harmful in the airways.


Subject(s)
Electronic Nicotine Delivery Systems , Tobacco Products , Humans , Animals , Sheep , Glycerol , Matrix Metalloproteinase 9/genetics , Vegetables , Mucus , Aerosols , RNA, Messenger , Propylene Glycols
14.
Eur J Pharm Biopharm ; 196: 114182, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38224756

ABSTRACT

Glycols stand out as one of the most commonly employed safe and effective excipients for pharmaceutical and cosmeceutical products. Their widespread adoption can be attributed to their exceptional solvency characteristics and their ability to interact effectively with skin lipids and keratin for permeation enhancement. Notably, propylene glycol enjoys significant popularity in this regard. Ongoing research endeavours have been dedicated to scrutinising the impact of glycols on dermal drug delivery and shedding light on the intricate mechanisms by which glycols enhance skin permeation. This review aims to mitigate the discordance within the existing literature, assemble a holistic understanding of the impact of glycols on the percutaneous absorption of active compounds and furnish the reader with a profound comprehension of the foundational facets pertaining to their skin permeation enhancement mechanisms, while simultaneously delving deeper into the intricacies of these processes.


Subject(s)
Glycols , Skin , Solvents/pharmacology , Administration, Cutaneous , Glycols/metabolism , Glycols/pharmacology , Skin/metabolism , Skin Absorption , Propylene Glycol , Propylene Glycols
15.
Spectrochim Acta A Mol Biomol Spectrosc ; 309: 123823, 2024 Mar 15.
Article in English | MEDLINE | ID: mdl-38181621

ABSTRACT

In this work, a green, fast, and simple synchronous spectrofluorimetric approach has been developed to simultaneously determine favipiravir, levodropropizine, and moxifloxacin hydrochloride as co-administered medications for COVID-19 treatment in pure form and spiked human plasma. The synchronous fluorescence spectroscopy technique to analyze the studied drugs at Δλ = 110 nm enabled the determination of levodropropizine at 360 nm. Then, applying Fourier Self-Deconvolution to each spectra to measure favipiravir and moxifloxacin hydrochloride at peak amplitudes of 431 nm and 479 nm, respectively, without any interference. Favipiravir, levodropropizine, and moxifloxacin hydrochloride could be sensitively determined using the described approach over concentration ranges of 20-300 ng/mL, 10-600 ng/mL, and 50-500 ng/mL, respectively. The method's validation was carried out effectively in accordance with guidelines recommended by the ICH. Finally, the Eco-scale and Green Analytical Procedure Index (GAPI) techniques have been used to evaluate the greenness of the proposed method.


Subject(s)
Amides , COVID-19 Drug Treatment , COVID-19 , Propylene Glycols , Pyrazines , Humans , Moxifloxacin , Spectrometry, Fluorescence
16.
J Colloid Interface Sci ; 660: 1030-1038, 2024 Apr 15.
Article in English | MEDLINE | ID: mdl-38220494

ABSTRACT

HYPOTHESIS: Triblock copolymers of poly(ethylene oxide) and poly(propylene oxide)-based matrices, such as Poloxamer 407 (P407) or Pluronic® F127, are extensively utilized in drug delivery and permeation systems due to their FDA approval and listing in the US and European Pharmacopoeias. The study hypothesizes that incorporating 2-hydroxypropyl-ß-cyclodextrin (HP-ß-CD) and the celecoxib-HP-ß-CD inclusion complex into a 16 wt% P407 and chitosan blend in an aqueous acetic acid solution will affect the system's rheological and structural properties. EXPERIMENTS: Rheological, small-angle X-ray scattering (SAXS), and dynamic light scattering (DLS) experiments were conducted to assess the impact of acetic acid and chitosan on the 16 wt% P407 and chitosan blend. Additionally, in vitro drug release studies were performed to monitor the drug release profile over time. FINDINGS: The addition of HP-ß-CD was found to inhibit gel formation in the 16 wt% P407 and chitosan blend. However, the presence of the celecoxib-HP-ß-CD inclusion complex showed no significant structural effects compared to P407 blended with chitosan alone. Rheological and SAXS analyses demonstrated that acetic acid led to the formation of a lamellar phase due to the lower pH, facilitating injectability. The presence of chitosan in acetic acid resulted in the detection of a hexagonal phase, affecting the release of celecoxib.


Subject(s)
Chitosan , Polyethylene Glycols , Propylene Glycols , 2-Hydroxypropyl-beta-cyclodextrin , Chitosan/chemistry , Celecoxib , Drug Liberation , Scattering, Small Angle , X-Ray Diffraction , Poloxamer/chemistry , Acetates
17.
Environ Sci Pollut Res Int ; 31(5): 8046-8060, 2024 Jan.
Article in English | MEDLINE | ID: mdl-38175516

ABSTRACT

Earth pressure balance (EPB) shield is increasingly employed in metro tunnel construction, and causes a series of environmental, safety, and resource waste problems due to the disposal of a considerable amount of muck. In situ recycling of EPB shield muck is an effective solution, whereas the foam is generated by residual foaming agents used as the muck conditioning material during tunnelling, which often adsorbs clay particles and overflows the flocculation tank. To achieve defoaming and antifoaming during the reuse of muck, this study prepared novel eco-friendly silicone oil-polyether defoamers by condensation, compounding, and shear emulsification. Defoaming and antifoaming performances of different defoamers were tested using a modified Ross-Miles method and a scale model of field flocculation systems. The results indicated that a high efficiency in defoam and antifoam was characterized by chemical grafting of nano-SiO2 from silicone oils, uniform distribution and large size of grains, low viscosity, and surface tension. The defoamer dosage of 0.002-0.004 wt% near critical micelle concentration (CMC) for each defoamer is reasonable. Overall, the prepared hydroxyl silicone oil-glycerol polyoxypropylene ether (H-G) defoamer compared with other silicone oil-polyether defoamers and commercial defoamers presents the highest defoaming and antifoaming efficiency. Considering the effects of EPB shield muck, the H-G defoamer is least affected by the compound materials and increasing concentration of the commercial foaming agent. Nevertheless, the stability of the H-G emulsion system is weaker than that of the dimethyl silicone oil-glycerol polyoxypropylene ether (D-G) emulsion system after 1 month of sealed storage.


Subject(s)
Antifoaming Agents , Polymers , Propylene Glycols , Silicone Oils , Antifoaming Agents/chemistry , Antifoaming Agents/pharmacology , Silicone Oils/chemistry , Emulsions/chemistry , Glycerol , Surface-Active Agents , Ethers
18.
Chem Commun (Camb) ; 60(10): 1257-1260, 2024 Jan 30.
Article in English | MEDLINE | ID: mdl-38175608

ABSTRACT

Homopurine strands are known to form antiparallel triplexes stabilized by G*G and A*A Hoogsteen pairs, which have two hydrogen bonds. But there has been no report on the parallel triplex formation of homopurine involving both adenosine and guanosine to the duplex. In this paper, we first report parallel triplex formation between a homopurine serinol nucleic acid (SNA) strand and an RNA/SNA duplex. Melting profiles revealed that the parallel SNA:RNA*SNA triplex was remarkably stable, even though the A*A pair has a single hydrogen bond. An L-acyclic threoninol nucleic acid (L-aTNA) homopurine strand also formed a stable parallel triplex with an L-aTNA/RNA duplex.


Subject(s)
Butylene Glycols , Nucleic Acids , Propanolamines , Propylene Glycols , Nucleic Acids/chemistry , RNA/chemistry , Amino Alcohols/chemistry , Nucleic Acid Conformation
20.
Macromol Rapid Commun ; 45(2): e2300452, 2024 Jan.
Article in English | MEDLINE | ID: mdl-37838916

ABSTRACT

Polymers are of great interest for medical and cosmeceutical applications. The current trend is to combine materials of natural and synthetic origin in order to obtain products with appropriate mechanical strength and good biocompatibility, additionally biodegradable and bioresorbable. Citric acid, being an important metabolite, is an interesting substance for the synthesis of materials for biomedical applications. Due to the high functionality of the molecule, it is commonly used in biomaterials chemistry as a crosslinking agent. Among citric acid-based biopolyesters, poly(1,8-octanediol citrate) is the best known. It shows application potential in soft tissue engineering. This work focuses on a much less studied polyester, poly(1,3-propanediol citrate). Porous and non-porous materials based on the synthesized polyesters are prepared and characterized, including mechanical, thermal, and surface properties, morphology, and degradation. The main focus is on assessing the biocompatibility and antimicrobial properties of the materials.


Subject(s)
Anti-Infective Agents , Citric Acid , Propylene Glycols , Citric Acid/chemistry , Citrates/chemistry , Biocompatible Materials/chemistry , Polyesters/chemistry , Tissue Engineering , Propylene Glycol , Anti-Infective Agents/pharmacology
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