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Search results for: drugs dosage
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Determination of MDPBP in postmortem blood samples by gas chromatography coupled with mass spectrometry
PublicationMDPBP (1-(3,4-methylenedioxyphenyl)-2-(1-pyrrolidinyl)-1-butanone) is a new psychoactive substance sold on the black market. It has been a controlled drug of abuse in Poland and China since 2015 as some toxic and fatal cases connected with use of synthetic cathinone derivatives were observed. The fatal case outlined here concerns a 19 year-old man, who was found dead with an envelope containing white powder lying nearby the cadaver....
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New Peptide Based Fluconazole Conjugates with Expanded Molecular Targets
PublicationInfections of Candida spp. etiology are frequently treated with azole drugs. Among azoles, the most widely used in the clinical scenario remains fluconazole (FLC). Promising results in treatment of dangerous, systemic Candida infections demonstrate the advantages of combined therapies carried out with combinations of at least two different antifungal agents. Here, we report five conjugates composed of covalently linked FLC and...
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Mission impossible for cellular internalization: When porphyrin alliance with UiO-66-NH2 MOF gives the cell lines a ride
PublicationIs it possible to accelerate cell internalization by hybridization of nanomaterials? Herein we support the realization of using metal-organic frameworks (MOFs) with the assistance of rigid porphyrin structure (H2TMP) aimed at drug loading, drug release, relative cell viability, and targeted in vitro drug delivery. There are several MOFs, i.e., UiO-66-NH2 (125 ± 12.5 nm), UiO-66-NH2 @H2TMP (160 ± 14 nm), UiO-66-NH2 @H2TMP@DOX, and...
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Optimization of adsorption of methyl orange from aqueous solution by magnetic CoFe2O4/ZnAl-layered double hydroxide composite using response surface methodology
PublicationThe CoFe2O4/ZnAl-layered double hydroxide (LDH) composite was successfully developed through a facile co-precipitation method, characterized, and applied as an effective adsorbent for the removal of methyl orange (MO) dye from aqueous solutions. The central composite design (CCD) of the response surface methodology (RSM) was employed to estimate and optimize process variables such as initial MO concentrations, solution pH, adsorbent...
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Effects of Addictive Substances During Pregnancy and Infancy and Their Analysis in Biological Materials
PublicationThe use of addictive substances during pregnancy is a serious social problem, not only because of effects on the health of the woman and child, but also because drug or alcohol dependency it detracts from childcare and enhances the prospect of child neglect and family breakdown. Developing additive substance abuse treatment programs for pregnant women is socially important and can help ensure the health of babies, prevent subsequent...
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Degradation kinetics and mechanism of pentoxifylline by ultraviolet activated peroxydisulfate
PublicationDegradation of pentoxifylline (PTX) by sodium peroxydisulfate (SPDS) assisted by UV irradiation has been investigated in deionized water. The treatment was more favorable over direct photolysis or peroxydisulfate oxidation alone. The effects of various parameters, including different dosage of oxidant agent, PTX concentration, initial solution pH levels, and the presence of inorganic ions like chloride, nitrate and carbonate have...
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Silver nanoparticles induce premutagenic DNA oxidation that can be prevented by phytochemicals from Gentiana asclepiadea
PublicationAmong nanomaterials, silver nanoparticles (AgNPs) have the broadest and most commercial applications due to their antibacterial properties, highlighting the need for exploring their potential toxicity and underlying mechanisms of action. Our main aim was to investigate whether AgNPs exert toxicity by inducing oxidative damage to DNA in human kidney HEK 293 cells. In addition, we tested whether this damage could be counteracted...
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Selection of effective cocrystals former for dissolution rate improvement of active pharmaceutical ingredients based on lipoaffinity index
PublicationNew theoretical screening procedure was proposed for appropriate selection of potential cocrystal formers possessing the ability of enhancing dissolution rates of drugs. The procedure relies on the training set comprising 102 positive and 17 negative cases of cocrystals found in the literature. Despite the fact that the only available data were of qualitative character, performed statistical analysis using binary classification...
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Detoxification of the tricyclic antidepressant opipramol and its analog – IS-noh by UGT enzymes before and after activation by phase I enzymes in rat liver microsomes
PublicationThe present studies were carried out to evaluate the simultaneous one-pot metabolism of opipramol (IS-opi) and analog (IS-noh) by phase I and phase II enzymes present in rat liver microsomes (RLM) as an alternative to separate testing with recombinant enzymes. This approach allows for more time-saving and cost-effective screening of the metabolism of newly discovered drugs. We also considered that the lack of results for phase...
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Badanie znaczenia atrybutów bazy wiedzy.
PublicationW pracy przedstawiono dwie metody umożliwiające wyznaczanie miary znaczenia wybranych atrybutów bazy wiedzy. W pierwszej metodzie wykorzystano teorię zbiorów przybliżonych i podano definicje miary znaczenia atrybutów oparte na liczbie reguł sprzecznych. Druga metoda wykorzystująca teorię zbiorów rozmytych pozawala na zdefiniowanie dwóch sposobów oceny miary znaczenia. Pierwsza miara opiera się na liczbie reguł sprzecznych,...
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Voltammetric and biological studies of folate-targeted non-lamellar lipid mesophases
PublicationFolate-targeted lipid nanostructures are promising strategies for the development of biocompatible drug delivery systems. The objective of this study was to evaluate the efficacy of drug delivery to cancer cells by folate-targeted lipid mesophases, cubosomes (CUB) and hexosomes (HEX), loaded with doxorubicin (DOX). Three cancer-derived cell lines (KB, HeLa, T98G) exhibiting different expressional levels of folate receptor protein...
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The relationship between standard reduction potentials of catechins and biological activities involved in redox control
PublicationRedox homeostasis involves factors that ensure proper function of cells. The excess reactive oxygen species (ROS) leads to oxidative stress and increased risk of oxidative damage to cellular components. In contrast, upon reductive stress, insufficient ROS abundance may result in faulty cell signalling. It may be expected that dietary antioxidants, depending on their standard reduction potentials (E°), will affect both scenarios....
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Topical delivery of pharmaceutical and cosmetic macromolecules using microemulsion systems
PublicationMicroemulsions are transparent, thermodynamically stable colloidal systems. Over the recent years, they have been increasingly investigated due to their potential as skin delivery vehicles for a wide range of drug molecules. The nanoscale particle size and the specificity of microemulsion components are the main features determining the skin permeation process. However, in order to effectively cross the skin barrier, the active...
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High-dose chemotherapy with autologous stem cell transplantation is an effective treatment of primary refractory Hodgkin's disease. Retrospective study of the Polish Lymphoma Research Group
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Fabrication methods of smart composite coatings - review
PublicationPostoperative bacterial infections are one of the main reasons for unsuccessful implantation of long-term implants. The development of bacterial infection requires antibiotic therapy, in extreme cases a reimplantation procedure is necessary. In order to provide materials for implants with antibacterial properties, they are subjected to modifications to create a coating that will release the drug substance, when the inflammation...
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Opioid Growth Factor and its Derivatives as Potential Non-toxic Multifunctional Anticancer and Analgesic Compounds
PublicationIn this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin and its analogues are interesting candidates for the...
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Biological and mechanical properties of bone cement with nanoparticles - in vivo and in vitro research
PublicationDespite antibiotics preventive treatment, before and after an implant implementation, risk of infection are real. These infections at the implant surface develop in a few months after applying them into the body. To prevent the development of bacteria and to reduce the risk of infection, implants coated with nanoparticles come into use. The Mechanical Department of the Technical University of Gdańsk carried out a research with...
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Examination of selected failure criteria with asymmetric shear stresses in the collapse analysis of laminated shells
PublicationThe paper is concerned with failure analysis of composite shells performed with the usage of the nonlinear 6‐parameter shell theory with drilling rotation degree of freedom. This special theory embodies naturally unlim-ited translations and rotations and is suitable for analysis of irregular shells for instance with various, partic-ularly orthogonal, intersections. The presence of the drilling rotation is inherently accompanied...
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Analiza wrażliwości pierwszego i drugiego rzędu w problemach statyki prętów cienkościennych
PublicationAnaliza wrażliwości pierwszego rzędu jest wykorzystywana w wielu zagadnieniach teorii konstrukcji. Pomimo tego, że analiza wrażliwości drugiego rzędu pozwala na znaczną poprawę dokładności uzyskiwanych wyników, jest ona mniej popularna niż analiza pierwszego rzędu. W pracy wyznaczono drugą wariację zmiennych stanu zachowania się konstrukcji. Przyjęto klasyczne założenia teorii prętów cienkościennych. W przykładzie numerycznym wyznaczono...
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Examination of epigenetic inhibitor zebularine in treatment of skin wounds in healthy and diabetic mice
PublicationDNA methyltransferase inhibitor zebularine was proven to induce regeneration in the ear pinna in mice. We utilized a dorsal skin wound model to further evaluate this epigenetic inhibitor in wound healing. Full-thickness excisional wounds were made on the dorsum of 2 and 10-month-old healthy BALB/c and 3 and 8-month-old diabetic (db/db) mice, followed by topical or intraperitoneal zebularine delivery. Depending on the strain, age,...
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Role of miR-15b/16–2 cluster network in endometrial cancer: An in silico pathway and prognostic analysis
PublicationEndometrial cancer (EC) is the second most common cancer in women. A large number of human cancers exhibit dysregulation of microRNA expression including EC. MiR-15b/16–2 is one of the best-known miRNA clusters that is expressed in many types of cancer tissues. Herein, we analyzed the expression of individual miR-15b/16–2 cluster members, its paralogues, and their target network analysis, as well as their prognostic significance...
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Novel fused pyran derivatives induce apoptosis and target cell cycle progression in anticancer efficacy against multiple cell lines.
PublicationNitrogen-based heterocycles such as pyrazole, imidazole, 1,2,4-triazole, benzimidazole, and benzotriazole substituted fused pyran derivatives (6a–e, 8a–e, 10a–e, 12a–e,&14a–e) have been synthesized and tested for their in vitro anticancer efficacies against MCF7, A549, and HCT116 cancer cell lines. Among the compounds, 6e, 14b, and 8c were identified as the most potent against MCF7, A549, and HCT116, with IC50 values of 12.46 2.72...
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TU‐FF‐A2‐04: New High‐Resolution Method to Measure the 3D Dose Distribution Around Brachytherapy Seeds Using BANG3‐Pro Gel Dosimetry
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Attitudes toward Receiving COVID-19 Booster Dose in the Middle East and North Africa (MENA) Region: A Cross-Sectional Study of 3041 Fully Vaccinated Participants
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Attitudes toward Receiving COVID-19 Booster Dose in the Middle East and North Africa (MENA) Region: A Cross-Sectional Study of 3041 Fully Vaccinated Participants
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Structural and dynamic changes adopted by EmrE, multidrug transporter protein—Studies by molecular dynamics simulation
PublicationEmrE protein transports positively charged aromatic drugs (xenobiotics) in exchange for two protons and thus provides bacteria resistance to variety of drugs. In order to understand how this protein may recognize ligands, the monomer and asymmetric apo-form of the EmrE dimer embedded in a heterogeneous phospholipid (POPE + POPG) membrane were studied by molecular dynamics simulations. Dimer is regarded as a functional form of the...
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Biological and mechanical properties of bone cement with nanoarticles - in vitro and in vivo research
PublicationDespite antibiotic preventive treatment both before and after implant implementation, the risks of infection are real. These infections develop at the implant surface a few months after inserting them into the body. To prevent the development of bacteria and reduce the risk of infection, implants coated with nanoparticles are used. The Mechanical Department of the Technical University of Gdansk carries out research into using bone...
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Functionalized Peptide Fibrils as a Scaffold for Active Substances in Wound Healing
PublicationTechnological developments in the field of biologically active peptide applications in medicine have increased the need for new methods for peptide delivery. The disadvantage of peptides as drugs is their low biological stability. Recently, great attention has been paid to self-assembling peptides that can form fibrils. Such a formulation makes bioactive peptides more resistant to enzymatic degradation and druggable. Peptide fibrils...
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Improvement of opipramol base solubility by complexation with β-cyclodextrin
PublicationOpipramol (OPI), a tricyclic antidepressant and anxiolytic compound, is administered orally in the form of a dihydrochloride. Salt form of the drug has a higher solubility in water and hence bioavailability and stability. A similar effect can be achieved by closing the hydrophobic part of the drug molecule in the cyclodextrin cavity. The paper presents opipramol inclusion complexes with beta-cyclodextrin (β-CD) in 1:1 molar ratio....
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Synthesis of green benzamide-decorated UiO-66-NH2 for biomedical applications
PublicationMetal-organic frameworks (MOFs) biocompatible systems can host enzymes/bacteria/viruses. Herein we synthesized a series of fatty acid amide hydrolase (FAAH)-decorated UiO-66-NH2 based on Citrus tangerine leaf extract for drug delivery and biosensor applications. Five chemically manipulated FAAH-like benzamides were localized on the UiO-66-NH2 surface with physical interactions. Comprehensive cellular and molecular analyses were...
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Determination of antibiotic residues in honey
PublicationHoney produced by honeybees is a valuable food product. The presence of xenobiotics in honey may harm its quality and constitute a danger to human health. Antibiotics are commonly applied by beekeepers to eliminate disease among honeybees. Moreover, ubiquitous administration of antibiotics may cause bacteria to become resistant to many drugs and spread antibioticresistant strains of bacteria. Appropriate sample preparation and...
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Pharmaceuticals wastewater treatment via different advanced oxidation processes: Reaction mechanism, operational factors, toxicities, and cost evaluation – A review
PublicationPharmaceuticals comprises different drugs used for treating different infections in human being and animals. The huge quantities of pharmaceuticals used are found to discharge into different water resources and cause different health and environmental problems. The continuous and large-scale discharge of pharmaceuticals increases their persistency which can consequently make them more toxic. The different advanced oxidation processes...
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Epidemiologia udaru mózgu
PublicationUdar mózgu i choroba wieńcowa to główne przyczyny zgonu i niepełnosprawności. Choroby naczyń mózgowych są drugą przyczyną śmierci naświecie i trzecią przyczyną śmiertelności w krajach Europy Zachodniej.
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Quantifying the effective mobilized RAP content during hot in-place recycling techniques
PublicationThe utilization of in-place recycling techniques is capable of consuming 100% reclaimed asphalt pavement (RAP). Hot in-place recycling (HIR) is one of the promising techniques to rehabilitate the pavements suffering from minor cracking issues through heat scarification, additive injecting, mechanical mixing, and compacting. However, the main concern of using 100% RAP in HIR remains as how much RAP can be activated and mobilized...
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Protective Effect of Black Tea Against Ethanol-Induced Oxidative Modifications of Liver Proteins and Lipids
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Pregabalin for the treatment of social anxiety disorder
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SU‐GG‐T‐286: Performance of An Improved Optical Computed Tomography Polymer Gel Dosimeter System for 3‐D Dose Verification of Static and Dynamic Phantom Deliveries
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AOP173 key event associated pathway predictor – online application for the prediction of benchmark dose lower bound (BMDLs) of a transcriptomic pathway involved in MWCNTs-induced lung fibrosis
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Common methods for the chiral determination of amphetamine and related compounds I. Gas, liquid and thin-layer chromatography
PublicationThis article reviews the most common, useful methods for the chiral determination of amphetamine (AM) and AM-deriveddesigner drugs in different of matrix, including blood, hair, urine, medicaments or standard solutions, taking into considerationarticles published in the past 15 years. We consider chromatographic methods (e.g., gas, liquid, high-performance liquid, and thinlayer). We describe several types of chiral derivatization...
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Targeting of FLT3-ITD kinase contributes to high selectivity of imidazoacridinone C-1311 against FLT3-activated leukemia cells
PublicationDrugs targeting receptor tyrosine kinase FLT3 are of particular interest since activating FLT3-internal tandem duplication (ITD) mutations abundantly occur in fatal acute myeloid leukemias (AMLs). Imidazoacridinone C-1311, a DNA-reactive inhibitor of topoisomerase II, has been previously shown to be a potent and selective inhibitor of recombinant FLT3. Here, we expand those findings by studying its effect on leukemia cells with...
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Mass spectrometry based identification of geometric isomers during metabolic stability study of a new cytotoxic sulfonamide derivatives supported by quantitative structure-retention relationships
PublicationA set of 15 new sulphonamide derivatives, presenting antitumor activity have been subjected to a metabolic stability study. The results showed that besides products of biotransformation, some additional peaks occurred in chromatograms. Tandem mass spectrometry revealed the same mass and fragmentation pathway, suggesting that geometric isomerization occurred. Thus, to support this hypothesis, quantitative structure-retention relationships...
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Prenatal exposure to substance of abuse: A worldwide problem
PublicationSubstance abuse during pregnancy is an important public health issue affecting the mother and the growing infant. Preterm labor, miscarriage, abruption and postpartum hemorrhage are obstetric complications which have been associated with women who are dependent on abused substances. Moreover, women are also at an increased risk of medical problems such as poor nutrition, anemia, urinary tract infections as well as sexually transmitted...
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Enzymes of the lysine biosynthetic pathway as targets for antifungals ?
PublicationSystemic infections caused by human pathogenic fungi in immunocompromized patients continue to be one of the important clinical problems. Limited availability of safe and efficacious antifungal chemotherapeutics and emerging resistance to existing drugs stimulates search for novel molecular targets for antifungals. The α-aminoadipate pathway (AAP) of L-lysine biosynthesis is unique in fungi and thus has been so far considered...
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Phospholipids as potential prevention factor in carcinogenesis
PublicationPhospholipids are a group of complex lipids, which can be used in cancer chemoprevention. Glicerophospholipids are composed of fatty acids esterified to a glycerol backbone, a phosphate group and a hydrophilic residue such as: cho- line, ethanoloamine, serine or inositol. In the sn-2 position of glicerophospholipid usually there are unsaturated fatty acids, i.e. linolenic acid, while in the sn-1 position more typi- cal are saturated...
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Cztery algorytmy które wstrząsnęły światem. Część II: Od czasu wykładniczego do wielomianowego
PublicationDrugi odcinek cyklu poświęcono problemowi programowania liniowego, który wywarł ogromny wpływ na życie milionów ludzi oraz badaniu liczb pierwszych, a więc problemowi ściśle związanemu z bezpieczeństwem naszych pieniędzy zdeponowanych w bankach.
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublicationRational drug design and in vitro pharmacology profiling constitute the gold standard in drug development pipelines. Problems arise, however, because this process is often dicult due to limited information regarding the complete identification of a molecule’s biological activities. The increasing aordability of genome-wide next-generation technologies now provides an excellent opportunity to understand a compound’s diverse eects...
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TRF1 and TRF2: pioneering targets in telomere-based cancer therapy
PublicationThis article presents an in-depth exploration of the roles of Telomere Repeat-binding Factors 1 and 2 (TRF1 and TRF2), and the shelterin complex, in the context of cancer biology. It emphasizes their emerging significance as potential biomarkers and targets for therapeutic intervention. Central to the shelterin complex, TRF1 and TRF2 are crucial in maintaining telomere integrity and genomic stability, their dysregulation often...
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Influence of the electrosynthesis conditions on the spontaneous release of anti-inflammatory salicylate during degradation of polypyrrole coated iron for biodegradable cardiovascular stent
PublicationIn this work, the spontaneous release of anti-inflammatory salicylate from polypyrrole (PPy) coated iron has been studied during degradation of the material in phosphate buffer saline at 37 C. The sodium salicylate was incorporated into PPy in a one-step electropolymerization process. The influence of the synthesis conditions such as sodium salicylate concentration, pyrrole concentration and deposition charge on drug release profile...
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Antibacterial Porous Systems Based on Polylactide Loaded with Amikacin
PublicationThree porous matrices based on poly(lactic acid) are proposed herein for the controlled release of amikacin. The materials were fabricated by the method of spraying a surface liquid. Description is given as to the possibility of employing a modifier, such as a silica nanocarrier, for prolonging the release of amikacin, in addition to using chitosan to improve the properties of the materials, e.g., stability and sorption capacity....
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Ocena odporności powłok na bazie DLC na doraźne uszkodzenie w warunkach tarcia ślizgowego ze smarowaniem wodą i solą fizjologiczną = Evaluation of DLC based coatings resistance to instanteneous damage under sliding friction conditions with distilated water or saline lubrication
PublicationWykonano serię testów w celu wyznaczenia granicznych warunków wymuszenia, zdefiniowaego jako średnie naciski powierzchniowe oraz prędkość ślizgania, po przekroczeniu których następuje gwałtowne zniszczenie powłoki. Na podstawie wyników pomiarów opracowano aproksymowane charakterystyki granicznych wymuszeń w układzie p - v oraz pokrewnych dla badanych materiałów, smarów i zakresu parametrów wymuszenia.