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The size and morphological characteristics of ketosome and physicochemical characteristics of ketoconazole in ketosomes were determined using dynamic light scattering, differential scanning calorimetry, powder x-ray diffractometer, scanning electron microscopy, and attenuated total reflectance-Fourier transform infrared spectroscopy. According to new study, changes in the cholesterol:surfactants ratio can change the zeta potential from 27. 866 to -12. 153 mV. When the cholesterol levels in the ketosome was high, the most entrapment of ketoconazole was about 87%. In addition, the cell viability assay demonstrated that the ketosome had reduced cytotoxicity in comparison to pure drug. When testing against Candida albicans, the ketosome had a lower MIC value than the pure drug. Conclusion: The results of this research revealed that the optimized ketoconazole-loaded niosome could be used as a potential nanovesicle for ketoconazole drug delivery, potentially opening up new avenues for the treatment of cutaneous candidiasis complaints.
Source link: https://doi.org/10.34172/ps.2022.34
To prevent acute respiratory distress syndrome in critically ill surgical patients, we need to describe the pharmacology of ketoconazole and investigate the use of ketoconazole in critically ill surgical patients. Study Design: Two randomized, controlled, double-blind studies were found that investigated the use of ketoconazole in critically ill surgical patients. Compared to 31% on placebo, one study found a 6% risk of ARDS in patients receiving ketoconazole 200 mg/d versus 31% on placebo. According to another report, there was a 15% risk of ARDs in patients receiving ketoconazole 400 mg/d versus 64% on placebo, with a statistically significant decline in mortality in the ketoconazole group versus placebo. Two studies published in a small population of critically ill surgical patients at risk of ARDs revealed a dramatic decline in the incidence of ARDS in a small population of critically ill surgical patients at risk of ARDS.
Source link: https://doi.org/10.1177/875512259501100511
Abstract One of the key steps in choosing the drug nanoparticle manufacturing processes by supercritical carbon dioxide is determining the solubility of the solid solute. The KTZ solubility in the SC-CO 2 ranged from 1. 70 percent to 8. 02 percent on u2212 4, with cosolvent in the SC-CO 2 ranging from 1. 70 u00d710 5 to 1. 96 u00d710 4 varies, according to 4. 69 u2212 4. This difference demonstrated the pronounced effect of menthol cosolvent on KTZ solubility in the SC-CO 2. Experimental results for the binary system can be more easily correlated for the binary system in comparison to other commonly used models.
Source link: https://doi.org/10.21203/rs.3.rs-139806/v1
An combination of A3K2A3 with benznidazole or ketoconazole produced a good synergism, increasing safety against trypomastigotes or epimastigotes of T. cruzi. In addition, the drug combination of A3K2A3 with benznidazole or ketoconazole on LLCMK2 cells demonstrated an antagonistic effect, resulting in increased cell protection from drug damage. Against T. cruzi, the A3K2A3 might be a promising anti-T. cruzi machine.
Source link: https://doi.org/10.1155/2017/7254193
Following 14 days, only ketoconazole had significantly higher ALT and AST measurements than the control group. The AST values were the highest in the rats treated with ketoconazole, followed by itraconazole, fluconazole, terbinafine, and griseofulvin, respectively. The liver enzyme tests indicated that ketoconazole had the highest risk of liver injury in liver injury, followed by itraconazole, fluconazole, terbinafine, and griseofulvin. Given the poor correlation between liver enzymes and liver injury severity, it is important to identify liver injury by histological examination.
Source link: https://doi.org/10.1155/2017/6746989
A. fumigatus in response to an adjunctive combination, i. e. , Ketoconazole plus EDTA, was the intended outcome of this research. Methods: In the absence and presence of a sublethal dose of EDTA, KTZ, and a mixture of KTZ plus EDTA, A. fumigatus was raised. MALDI-TOF/MS performed the protein analysis by using a proteomic approach, and protein analysis was done by MALDI-TOF/MS. Scanning Electron Microscopy and the harmful effect on erythrocytes by haemolytic assay investigated the morphological effect of the mixture on A. fumigatus. MTT's report: The combination of KTZ and EDTA produced a non-toxic up to 500 u03bcg/ml by MTT assay. These goals can be used for novel drug research as some of them are involved in fungal virulence, and adjunctive combination therapy can be a promising option.
Source link: https://doi.org/10.2174/2211352519666210224095411
Chronic myeloid leukemia is a hematologic disorder characterized by the oncogene BCR-ABL1, which encodes an oncoprotein with tyrosine kinase activity. This research was designed to establish an imatinib-resistant human CML cell line, assess P-gp's role in drug resistance, and determine the ability of ketoconazole to overcome resistance by blocking P-gp. P-gp expression, intracellular accumulation of a P-gp substrate by flow cytometry, and percentage of apoptosis were determined in both cell lines: cell viability after exposure to imatinib and imatinib + ketoconazole, P-gp expression, cell viability, and cell viability. P-gp was overexpressed in the extremely resistant CML cell line obtained, and intracellular doxorubicin was low, suggesting high P-gp activity. P-gp plays a significant role in CML cells' imatinib resistance. Ketoconazole converted CML cell resistance to imatinib by targeting P-gp-related pathways. Patients resistant to imatinib are expected to be helped by ketoconazole's repurposing for CML therapy.
Source link: https://doi.org/10.3390/ijms23147715
In the human promyelocytic cell line HL60, the metabolism of [3 H]25-hydroxyvitamin D 3 in vitro to material with the characteristics of [3 H]24,25-dihydroxyvitamin D 3 has been investigated. For four days, a synthetic D3 of 24,25-Danger D 3 was induced in a dose-dependent manner in cells treated with 0u00b71 n m 1,25-dihydroxyvitamin D 3 in a dose-dependent manner. In a parallel manner, the ability to synthesize [3 H]24,25-D 3 from [3 H]25-D 3 and the expression of NSE activity all responded to the decrease in concentration of 1u03b1,25-2 D 3 in the culture medium. Synthesis of [ 3 H]24,25-2 D3 was linear when the incubation time was between 1 and 8 hrs and the cell number between 1 and 8 h, with the cell number ranging from 1 to 10 cells/incubation.
Source link: https://doi.org/10.1677/jme.0.0030199
Ketoconazole was given orally to sexually mature Wistar rats and testicular function was assessed. Without modifying gonadotrophin levels, a single oral dose of 24 mg ketoconazole/kg body weight lowered plasma testosterone and DHT levels by 83 and 50%, respectively within 2 h, respectively. Treatment for up to 7 days reduced epididvmal sperm number and motility, as well as increased the number of abnormal sperm. Generally, sperm number and motility decreased, increased the number of abnormal sperm, and increased the number of abnormal sperm, but did not affect testicular germ cells.
Source link: https://doi.org/10.1530/acta.0.1110246
In nine previously untreated patients with advanced prostate cancer, we investigated the endocrine effects of ketoconazole. On day four of therapy, no abnormal results were found, but serum testosterone increased gradually. Since sex hormone globulin increased markedly during therapy, the effect of the drug on unbound testosterone was marginally more relevant. In all patients, there was an increase in progesterone and LH. In one patient followed monthly for a period of 12 months, the mean testosterone concentration increased from 69 ng/100 ml to 428 ng/100 ml in another. Between the mean serum concentration of testosterone and the mean concentration of ketoconazole is a good inverse correlation could be established. The change in serum dehydroepiandrosterone sulphate was also related inversely to the mean ketoconazole level, according to the mean ketoconazole level. In 2 patients with mild gynaecomastia, increased oestradiol concentrations were found.
Source link: https://doi.org/10.1530/acta.0.1100276
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