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Powder bed fusion–laser beam (PBF-LB) three-dimensional (3D) printing: Influence of laser hatching distance on the properties of zolpidem tartrate tablets
Get PDFLaser sintering, known as powder bed fusion–laser beam (PBF-LB), offers promising potential for the fabrication of patient-specific drugs. The aim of this study was to provide an insight into the PBF-LB process with regard to the process parameters, in particular the laser hatching distance, and its influence on the properties of zolpidem tartrate (ZT) tablets. PHARMACOAT® 603 was used as the polymer, while Candurin® Gold Sheen and AEROSIL® 200 were added to facilitate 3D printing. The particle size distribution of the powder blend showed that the layer height should be set to 100 µm, while the laser hatching distance was varied in five different steps (50, 100, 150, 200 and 250 µm), keeping the temperature and laser scanning speed constant. Increasing the laser hatching distance and decreasing the laser energy input led to a decrease in the colour intensity, mass, density and hardness of the ZT tablets, while the disintegration and dissolution rate were faster due to the more fragile bonds between the particles. The laser hatching distance also influenced the ZT dosage, indicating the importance of this process parameter in the production of presonalized drugs. The absence of drug-polymer interactions and the amorphization of the ZT were confirmed
Estimation of passive gastrointestinal absorption of new dual DNA gyrase and topoisomerase IV inhibitors using PAMPA and biopartitioning micellar chromatography and quantitative structure-retention relationship analysis
No full textDNA gyrase and topoisomerase IV play significant role in maintaining the correct structure of DNA during replication and they have been identified as validated targets in antibacterial drug discovery. Inadequate pharmacokinetic properties are responsible for many failures during drug discovery and their estimation in the early phase of this process maximizes the chance of getting useful drug candidates. Passive gastrointestinal absorption of a selected group of thirteen dual DNA gyrase and topoisomerase IV inhibitors was estimated using two in vitro tests – parallel artificial membrane permeability assay (PAMPA) and biopartitioning micellar chromatography (BMC). Due to good correlation between obtained results, passive gastrointestinal absorption of remaining ten compounds was estimated using only BMC. With this experimental setup, it was possible to identify compounds with high values of retention factors (k) and highest expected passive gastrointestinal absorption, and compounds with low values of k for which low passive gastrointestinal absorption is predicted. Quantitative structure-retention relationship (QSRR) modelling was performed by creating multiple linear regression (MLR), partial least squares (PLS) and support vector machines (SVM) models. Descriptors with the highest influence on retention factor were identified and their interpretation can be used for the design of new compounds with improved passive gastrointestinal absorption
Vaccinium myrtillus L. Leaf Waste as a Source of Biologically Potent Compounds: Optimization of Polyphenol Extractions, Chemical Profile, and Biological Properties of the Extracts
Get PDFThe aims of the present research include (1) optimization of extraction from Vaccinium myrtillus leaf waste via investigation of plant material:medium ratio, extraction medium, and extraction period, employing extractions at room and high temperatures, or using ultrasound and microwaves (M, HAE, UAE, and MAE, respectively), (2) physicochemical characterization, and (3) investigation of extract biological potential. The statistical analysis revealed that optimal levels of parameters for the greatest polyphenolic yield were a proportion of 1:30 g/mL, ethyl alcohol 50% (v/v) during 2 min of microwave irradiation. By LC-MS analysis, 29 phenolic components were detected; HAE showed the highest richness of almost all determined polyphenols, while chlorogenic acid and quercetin 3-O-glucuronide were dominant. All extracts showed a high inhibition of Staphylococcus aureus growth. The effect of different parameters on extracts’ antioxidant capacity depended on the used tests. The extracts also showed a stimulative influence on keratinocyte viability and anti-inflammatory activity (proven in cell-based ELISA and erythrocyte stabilization assays). The extraction procedure significantly affected the extraction yield (MAE ≥ maceration ≥ UAE ≥ HAE), whereas conductivity, density, surface tension, and viscosity varied in a narrow range. The presented research provides evidence on the optimal extraction conditions and technique, chemical composition, and antioxidant, antimicrobial, anti-inflammatory, and keratinocyte viability properties of bilberry extracts for potential applications in pharmacy and cosmetics
Introduction to the Monitoring of Medicinal and Aromatic Plants in the "Stara Planina" Nature Park on the Territory of the Knjaževac Municipality
No full textТеренским истраживањем ПП „Стара
планина” на територији општине Књажевац регистровано је 159 лековитих и ароматичних врста биљака сврстаних у 54 фамилије од којих су
Lamiaceae Rosaceae и Asteraceae са највећим бројем
представника. За све регистроване врсте је наведен орган који се сакупља и начин употребе према
званичној и народној медицини. Статус заштите
према националној легислативи такође je приказан за све врсте. За одабране, најзаступљеније комерцијално значајне врсте презентоване су карте
распрострањења. Образложени су најзначајнији
фактори угрожавања и истакнут је значај познавања и примена принципа одрживог сакупљања
ради заштите и очувања популација самониклих
лековитих биљака.The field research conducted within
the "Stara Planina" Nature Park, in the territory of
Knjaževac municipality, registered 159 medicinal and
aromatic plant species classified into 54 families, with
Lamiaceae, Rosaceae and Asteraceae being the families with the highest number of medicinal representa-
tives. For all recorded species, the part of the plant that
is harvested and its use according to official and traditional medicine is indicated. The conservation status according to national legislation is also provided
for all species. For selected commercially significant
and most represented species, distribution maps are
presented. The most significant threatening factors are
discussed, and the importance of understanding and
applying sustainable harvesting principles to ensure
the protection and conservation of wild medicinal
plant populations is highlighted
In silico analysis of positive and negative effects of isothiocyanates in breast cancer
No full textBreast cancer is the most common cancer in women, with a constant
trend of increasing incidence, poor prognosis and high death rate.
Newer studied show that the application of phytochemicals, such as
sulforaphane (SFN) and phenylethyl isothicyanate (PEITC), has a chemoprotective effect, but also that the safety of their application has not
been sufficiently tested. Therefore, the aim of this research was to
investigate the positive and negative effects of SFN and PEITC on breast
cancer using in silico methods, i.e., detailed analysis of available toxicogenomic data, with doxorubicin serving as a control molecule. The
Gene Expression Omnibus, GEO (https://www.ncbi.nlm.nih.gov/geo/), a publicly available database, was utilized to procure gene profiles
from both malignant and healthy tissues. These profiles were subsequently analyzed using the GEO2R tool (https://www.ncbi.nlm.nih.
gov/geo/geo2r/), which identifies genes differentially expressed between tumor and healthy tissue. To assess genes interacting with doxorubicin (as a control), sulforaphane (SFN), and phenethyl isothiocyanate (PEITC), the Comparative Toxicogenomic Database (CTD, http://
ctdbase.org/) was used. Interactivenn tool (http://www.interactivenn.
net/) helped with obtaining sets of common genes interacting with
doxorubicin, SFN, and PEITC, respectively, and which are dysregulated in breast cancer. Toppgene tool (https://toppgene.cchmc.org/) Toppfun function was used to investigate the role of the selected genes in
gene ontology processes that could affect cancer progression, while
GeneMania (https://genemania.org/) determined genes related to the
set of genes and the type of interaction between all of them. A total of
103 genes have altered expression in breast cancer. After analyzing the
gene network, it was determined that doxorubicin interacts with 41
genes altered in breast cancer (21 upregulated and 20 downregulated),
sulforaphane with 13 genes (6 upregulated and 7 downregulated), and
phenylethyl isocyanate with 3 genes (1 upregulated and 2 downregulated). The dominant type of interaction between upregulated and
downregulated genes and doxorubicin was co-expression (42.9% and
70.05%), co-expression of upregulated genes and sulforaphane
(68.44%), colocalization of downregulated genes and sulforaphane
(68.38%), and physical interactions between PEITC and upregulated
and downregulated genes (77.64%). Up-regulated genes associated
with sulforaphane are involved in the metabolism of amino acids and
their derivatives, while down-regulated genes are associated with gluconeogenesis and glycolysis. In a conclusion, doxorubicin and isothiocyanates show a positive chemoprotective effect, however, they also
cause negative effects, which affects the safety of application. Doxorubicin exhibits cardiotoxic properties, and sulforaphane can lead to
disturbances in glucose metabolism or be associated with metabolic
epileptic disorders.Abstracts of the 58th Congress of the European Societies of Toxicology (EUROTOX 2024), "Toxicology – A Quest for safe Chemicals and Medicines.", 8-11 September 2024 • Copenhagen, Denmar
Animal models to study cognitive impairment of chronic kidney disease
No full textMild cognitive impairment (MCI) is common in people with chronic kidney disease (CKD), and its prevalence increases with progressive loss of kidney function. MCI is characterized by a decline in cognitive performance greater than expected for an individual age and education level but with minimal impairment of instrumental activities of daily living. Deterioration can affect one or several cognitive domains (attention, memory, executive functions, language, and perceptual motor or social cognition). Given the increasing prevalence of kidney disease, more and more people with CKD will also develop MCI causing an enormous disease burden for these individuals, their relatives, and society. However, the underlying pathomechanisms are poorly understood, and current therapies mostly aim at supporting patients in their daily lives. This illustrates the urgent need to elucidate the pathogenesis and potential therapeutic targets and test novel therapies in appropriate preclinical models. Here, we will outline the necessary criteria for experimental modeling of cognitive disorders in CKD. We discuss the use of mice, rats, and zebrafish as model systems and present valuable techniques through which kidney function and cognitive impairment can be assessed in this setting. Our objective is to enable researchers to overcome hurdles and accelerate preclinical research aimed at improving the therapy of people with CKD and MCI
Vaccination health literacy: cultural validation and pilot testing of the HLS19-VAC instrument
No full textIntroduction
Vaccinаtion health literacy (VHL) is considered an extremely important aspect of health literacy. HLS19-VAC questionnaire is a 14-item ‘subjective’ perception-based instrument used for measuring VHL in the M-POHL Health Literacy Survey 2019-2021, which Serbia was not part of.
Aim
Translation and cultural validation of the HLS19-VAC questionnaire and using the validated Serbian version (HLS19-VAC_RS) for pilot study research.
Materials and methods
The English version of HLS19-VAC was translated using a systematic approach; three forward and one back-translations were synthesized and compared by an expert committee. Thereafter, cognitive interviews with 11 participants produced a version that was culturally validated by an expert panel. We conducted a cross-sectional pilot study using a HLS19-VAC_RS, on a convenient sample of the general population in Serbia. VHL was assessed by calculating the score for 4 out of 14 questions. Additional data were collected through a general questionnaire with 30 questions. Descriptive and inferential statistics were used.
Results
Cognitive interviews showed some problems in wording, and cultural adaptation resulted in minor refinements to eight out of 14 items. The instrument was pretested by 11 experts who adjusted it accordingly to produce culturally validated HLS19 -VAC_RS. Of 439 respondents in a pilot study, 15% had problematic VHL, while the levels of sufficient and excellent VHL were nearly the same (38.5% and 35.1%, respectively). There was difficulty in deciding whether to receive the flu vaccine (15.0%) and to find information about recommended vaccines (12.3%). There was a significant statistical difference in responses to VHL and monthly income and alcohol consumption. Most of the respondents contacted pharmacists as primary sources of information about medication (42.7%).
Conclusions
HLS19 -VAC_RS could be implemented in a local context as culturally appropriate. Further testing on a population level is needed.17th European Public Health Conference 2024 Sailing the Waves of European Public Health: Exploring a Sea of Innovation Lisbon, Portugal 12–15 November 202
Low-energy nanoemulsions with ibuprofen – interfacial interplay of oils, surfactants and cosolvents
No full textThe aim of this work was to elucidate how oils and stabilizers of different
properties affect the phase behavior of low-energy nanoemulsions while serving as carriers
for active pharmaceutical ingredients (API) with both lipophilic and hydrophilic
characteristics (ibuprofen as the model drug).Poster: [https://farfar.pharmacy.bg.ac.rs/handle/123456789/5871
Subacute cutaneous lupus erythematosus induced by biological therapy of psoriasis: a literature review
No full textIntroduction & Objectives:
Due to the increasing availability and use of biological therapy, adverse reactions to these medications are being
carefully monitored and studied. Cytokine and immune imbalance caused by certain biologics can trigger
autoimmune diseases, including lupus-like syndrome, specifically one of its cutaneous forms – subacute cutaneous
lupus erythematosus (SCLE). This literature review aimed to identify and analyze SCLE cases associated with
biological therapy of psoriasis reported to date. ...Abstract: [https://farfar.pharmacy.bg.ac.rs/handle/123456789/5870
The role of dendritic cells in tertiary lymphoid structures: implications in cancer and autoimmune diseases
No full textTertiary Lymphoid Structures (TLS) are organized aggregates of immune cells such as T cells, B cells, and Dendritic Cells (DCs), as well as fibroblasts, formed postnatally in response to signals from cytokines and chemokines. Central to the function of TLS are DCs, professional antigen-presenting cells (APCs) that coordinate the adaptive immune response, and which can be classified into different subsets, with specific functions, and markers. In this article, we review current data on the contribution of different DC subsets to TLS function in cancer and autoimmunity, two opposite sides of the immune response. Different DC subsets can be found in different tumor types, correlating with cancer prognosis. Moreover, DCs are also present in TLS found in autoimmune and inflammatory conditions, contributing to disease development. Broadly, the presence of DCs in TLS appears to be associated with favorable clinical outcomes in cancer while in autoimmune pathologies these cells are associated with unfavorable prognosis. Therefore, it is important to analyze the complex functions of DCs within TLS in order to enhance our fundamental understanding of immune regulation but also as a possible route to create innovative clinical interventions designed for the specific needs of patients with diverse pathological diseases.This article has been corrected. Link to the correction: [https://farfar.pharmacy.bg.ac.rs/handle/123456789/5999