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BMC Chemistry Nov 2023Recently, green analytical chemistry (GAC) is a key issue towards the idea of sustainability, the analytical community is focused on developing analytical methods that...
Green chromatographic methods for determination of co-formulated lidocaine hydrochloride and miconazole nitrate along with an endocrine disruptor preservative and potential impurity.
Recently, green analytical chemistry (GAC) is a key issue towards the idea of sustainability, the analytical community is focused on developing analytical methods that incorporate green chemistry principles to minimize adverse impacts on the environment and humans. Herein, we present 2 sustainable, selective, and validated chromatographic methods. Initially, lidocaine hydrochloride (LDC) and miconazole nitrate (MIC) with two preservatives; methyl paraben (MTP) and saccharin sodium (SAC) were chromatographed via TLC-densitometric method which employed ethyl acetate: methanol: formic acid (9:1:0.1, by volume) as the mobile phase with UV detection at 220.0 nm, good correlation was obtained in the range of 0.3-3.0 µg/band for MIC and LDC. Following that, RP-HPLC was successfully applied for separating quinary mixture of LDC, MIC, MTP, SAC along with LDC impurity; dimethyl aniline (DMA) using C18 column, and a gradient green mobile phase composed of methanol and phosphate buffer (pH 6.0) in different ratios with a flow rate 1.5 mL/min and UV detection at 210.0 nm, linearity ranges from 1.00 to 100.00 µg/mL for MIC, 2.00-100.00 µg/mL for LDC and 1.00--20.00 µg/mL for MTP and DMA. No records to date regarding the determination of the two drugs, besides MTP and DMA. The proposed methods were validated according to the ICH guidelines and applied successfully to the analysis of the compounds. The methods' results were statistically compared to those obtained by applying the reported one, indicating no significant difference regarding both accuracy and precision. The methods' greenness profiles have been assessed and compared with those of the reported method using different assessment tools.
PubMed: 37941018
DOI: 10.1186/s13065-023-01065-3 -
Oral Diseases Jul 2016Candida-induced denture stomatitis is a common debilitating problem among denture wearers. Previously, we described the fabrication of a new denture material that...
OBJECTIVE
Candida-induced denture stomatitis is a common debilitating problem among denture wearers. Previously, we described the fabrication of a new denture material that released antifungal drugs when immersed in phosphate buffered saline. Here, we use more clinically relevant immersion conditions (human saliva; 37°C) and measure miconazole release and bioactivity.
MATERIALS AND METHODS
Disks were prepared by grafting PNVP [poly(N-vinyl-2-pyrrolidinone)] onto PMMA [poly(methylmethacrylate)] using plasma initiation (PMMA-g-PNVP) and then loaded with miconazole. Drug-loaded disks were immersed in 10-100% human saliva (1-30 days). Miconazole release was measured and then tested for bioactivity vs miconazole-sensitive and miconazole-resistant Candida isolates.
RESULTS
HPLC was used to quantify miconazole levels in saliva. Miconazole-loaded disks released antifungal drug for up to 30 days. Higher drug release was found with higher concentrations of saliva, and, interestingly, miconazole solubility was increased with higher saliva concentrations. The released miconazole retained its anticandidal activity. After immersion, the residual miconazole could be quenched and the disks recharged. Freshly recharged disks displayed the same release kinetics and bioactivity as the original disks. Quenched disks could also be charged with chlorhexidine that displayed anticandidal activity.
CONCLUSIONS
These results suggest that PMMA-g-PNVP is a promising new denture material for long-term management of denture stomatitis.
Topics: Adult; Antifungal Agents; Candida; Chlorhexidine; Delayed-Action Preparations; Dental Materials; Dentures; Dose-Response Relationship, Drug; Drug Carriers; Female; Gentamicins; Humans; Male; Methylmethacrylates; Miconazole; Middle Aged; Polymethyl Methacrylate; Pyrrolidinones; Saliva
PubMed: 26855200
DOI: 10.1111/odi.12456 -
Scientific Reports Dec 2022A green and simple method was proposed for the synthesis of silver nanoparticles (Ag-NPs) using Piper cubeba seed extract as a reducing agent for the first time. The...
Green synthesis, characterization, and antimicrobial applications of silver nanoparticles as fluorescent nanoprobes for the spectrofluorimetric determination of ornidazole and miconazole.
A green and simple method was proposed for the synthesis of silver nanoparticles (Ag-NPs) using Piper cubeba seed extract as a reducing agent for the first time. The prepared Ag-NPs were characterized using different spectroscopic and microscopic techniques. The obtained Ag-NPs showed an emission band at 320 nm when excited at 280 nm and exhibited strong green fluorescence under UV-light. The produced Ag-NPs were used as fluorescent nanosensors for the spectrofluorimetric determination of ornidazole (ONZ) and miconazole nitrate (MIZ) based on their quantitative quenching of Ag-NPs native fluorescence. The current study introduces the first spectrofluorimetric method for the determination of the studied drugs using Ag-NPs without the need for any pre-derivatization steps. Since the studied drugs don't exhibit native fluorescent properties, the importance of the proposed study is magnified. The proposed method displayed a linear relationship between the fluorescence quenching and the concentrations of the studied drugs over the range of 5.0-80.0 µM and 20.0-100.0 µM with limits of detection (LOD) of 0.35 µM and 1.43 µM for ONZ and MIZ, respectively. The proposed method was applied for the determination of ONZ and MIZ in different dosage forms and human plasma samples with high % recoveries and low % RSD values. The developed method was validated according to ICH guidelines. Moreover, the synthesized Ag-NPs demonstrated significant antimicrobial activities against three different bacterial strains and one candida species. Therefore, the proposed method may hold potential applications in the antimicrobial therapy and related mechanism research.
Topics: Humans; Silver; Metal Nanoparticles; Microbial Sensitivity Tests; Ornidazole; Miconazole; Anti-Infective Agents; Plant Extracts; Anti-Bacterial Agents
PubMed: 36496441
DOI: 10.1038/s41598-022-25830-x -
International Journal of Nanomedicine 2016Miconazole is a broad-spectrum antifungal drug that has poor aqueous solubility (<1 µg/mL); as a result, a reduction in its therapeutic efficacy has been reported. The...
BACKGROUND AND OBJECTIVE
Miconazole is a broad-spectrum antifungal drug that has poor aqueous solubility (<1 µg/mL); as a result, a reduction in its therapeutic efficacy has been reported. The aim of this study was to formulate and evaluate miconazole-loaded solid lipid nanoparticles (MN-SLNs) for oral administration to find an innovative way to alleviate the disadvantages associated with commercially available capsules.
METHODS
MN-SLNs were prepared by hot homogenization/ultrasonication. The solubility of miconazole in different solid lipids was measured. The effect of process variables, such as surfactant types, homogenization and ultrasonication times, and the charge-inducing agent on the particle size, zeta potential, and encapsulation efficiency were determined. Furthermore, in vitro drug release, antifungal activity against Candida albicans, and in vivo pharmacokinetics were studied in rabbits.
RESULTS
The MN-SLN, consisting of 1.5% miconazole, 2% Precirol ATO5, 2.5% Cremophor RH40, 0.5% Lecinol, and 0.1% Dicetylphosphate, had an average diameter of 23 nm with a 90.2% entrapment efficiency. Furthermore, the formulation of MN-SLNs enhanced the antifungal activity compared with miconazole capsules. An in vivo pharmacokinetic study revealed that the bioavailability was enhanced by >2.5-fold.
CONCLUSION
MN-SLN was more efficient in the treatment of candidiasis with enhanced oral bioavailability and could be a promising carrier for the oral delivery of miconazole.
Topics: Administration, Oral; Animals; Antifungal Agents; Biological Availability; Candida albicans; Candidiasis; Chemistry, Pharmaceutical; Drug Carriers; Lipids; Male; Miconazole; Nanoparticles; Particle Size; Rabbits; Solubility
PubMed: 26869787
DOI: 10.2147/IJN.S100625 -
Molecules (Basel, Switzerland) Jul 2018This study aims to develop new antifungal dermal films based on their mechanical properties (elongation, adhesion, behaviour towards vapour moisture) and the in vitro... (Comparative Study)
Comparative Study
This study aims to develop new antifungal dermal films based on their mechanical properties (elongation, adhesion, behaviour towards vapour moisture) and the in vitro availability of miconazole nitrate, used as a pharmaceutical active ingredient in various concentrations. The three polymeric films prepared were translucent or shiny, with the surface of 63.585 cm², 0.20⁻0.30 mm thickness, and content of miconazole nitrate of 3.931 or 15.726 mg·cm². The mechanical resistance and elongation tests demonstrated that the two films based on hydroxyethyl cellulose (HEC) polymer were more elastic than the one prepared with hydroxypropyl methylcellulose (HPMC). The vapour water absorption and vapour water loss capacity of the films revealed that the HPMC film did not dry very well in the process of preparation by the evaporation of the solvent technique, unlike the HEC films that jellified more evenly in water and had higher drying capacity at 40 °C. The in vitro availability of miconazole nitrate from dermal films was evaluated using the Franz diffusion cell method, through a synthetic membrane (Ø 25 mm × 0.45 µm) and acceptor media with pH 7.4 (phosphate buffer and sodium lauryl sulphate 0.045%), resulting a release rate of up to 70%.
Topics: Administration, Cutaneous; Antifungal Agents; Biological Availability; Biomechanical Phenomena; Cellulose; Chemistry, Pharmaceutical; Elasticity; Hypromellose Derivatives; Miconazole
PubMed: 29976876
DOI: 10.3390/molecules23071640 -
Saudi Pharmaceutical Journal : SPJ :... Apr 2023Miconazole is a synthetic derivative of imidazole, a medication with a broad-spectrum antifungal agent that is used to treat localized vaginal, skin, and nail...
Miconazole is a synthetic derivative of imidazole, a medication with a broad-spectrum antifungal agent that is used to treat localized vaginal, skin, and nail infections. The aim of the study was to develop an innovative technique to improve the permeability and efficacy of topical miconazole nitrate. A nanoemulgel of miconazole nitrate was formulated by the incorporation of a nanoemulsion and a hydrogel. The nanoemulsion was first optimized using a self-emulsifying technique, and the drug was then loaded into the optimum formulation and evaluated prior to mixing with the hydrogel. Miconazole nitrate nanoemulgel formulations were evaluated for their physical characteristics and antifungal activity. Based on the results, the formulation with 0.4 % Carbopol showed the highest release profile (41.8 mg/ml after 2 h); thus, it was chosen as the optimum formulation. A cell diffusion test was performed to examine the ability of the Miconazole nitrate nanoemulgel to penetrate the skin and reach the bloodstream. Percentage cumulative drug releases of 29.67 % and 23.79 % after 6 h were achieved for the MNZ nanoemulgel and the commercial cream, Daktazol, respectively. The antifungal activity of the novel MNZ nanoemulgel formulation was tested against and compared to Daktazol cream and almond oil; the results were: 40.9 ± 2.3 mm, 25.4 ± 2.7 mm and 18 ± 1.9 mm, respectively. In conclusion, a novel MNZ nanoemulgel showing superior antifungal activity compared to that of the commercial product has been developed. This nanotechnology technique is a step toward making pharmaceutical dosage forms that has a lot of promise.
PubMed: 37063448
DOI: 10.1016/j.jsps.2023.02.005 -
The Pan African Medical Journal 2021Candidiasis is an acute or subacute fungal infection caused by fungi that belongs to candida genus, with Candida albicansbeing the most frequent causative agent. Candida...
Candidiasis is an acute or subacute fungal infection caused by fungi that belongs to candida genus, with Candida albicansbeing the most frequent causative agent. Candida kefyr is a rare cause of candidiasis which has been reported in systemic candidiasis and deep infections. However, to date, it has never been reported as a cause in dermatophytosis. We report a case of candidiasis caused by Candida kefyr in a 72-year-old woman with a chief complaint of pruritic erythematous rash on the back from one day prior to admission. Diagnosis was established based on clinical features, direct microscopic examination with 10% potassium hydroxide solution, gram staining. The fungal species was determined by carbohydrate fermentation test which showed a positive result for Candida kefyr. The patient was treated with miconazole cream and fusidic cream and showed significant clinical improvement.
Topics: Aged; Antifungal Agents; Candidiasis, Cutaneous; Erythema; Female; Fusidic Acid; Humans; Kluyveromyces; Miconazole; Pruritus; Treatment Outcome
PubMed: 33995784
DOI: 10.11604/pamj.2021.38.178.28054 -
Indian Journal of Otolaryngology and... Mar 2015To evaluate the efficacy of clotrimazole, miconazole and fluconazole in empirical treatment of otomycosis in our tertiary care hospital and to appraise possible better...
To evaluate the efficacy of clotrimazole, miconazole and fluconazole in empirical treatment of otomycosis in our tertiary care hospital and to appraise possible better outcome in otomycosis. Two hundred and ninety five patients who presented with clinical otomycosis at our Melmaruvathur Adiparasakthi Institute of medical sciences were incorporated in this study. Two hundred and fourteen patients who satisfied our criteria were recognized and they were randomly alienated into three groups A, B, C. Group A patients were advised to instill clotrimazole ear drops by themselves. Miconazole cream instillation were done by our trained personal in group B patients. Group C patients were advised to use fluconazole ear drops. Patients were educated to keep ear dry and instructed to come for evaluation in first and second week after initial visit. A randomized double blinded prospective study. In the first week, clotrimazole had a good response than miconazole and fluconazole in our patients and in the second week, our patients showed a drastic response in patients instilling flucanozole ear drops compared to those using micanozole and clotrimazole. This better outcome doesn't show statistical significance since p value is 0.882. Clotrimazole drops, miconazole cream and Fluconazole drops showed almost same therapeutic efficacy in Otomycosis.
PubMed: 25621236
DOI: 10.1007/s12070-014-0780-9 -
Current Medical Mycology Mar 2015Otomycosis is an acute, subacute or chronic fungal infection of the pinna, the external auditory meatus and the ear canal caused mainly by several species of saprophytic...
BACKGROUND AND PURPOSE
Otomycosis is an acute, subacute or chronic fungal infection of the pinna, the external auditory meatus and the ear canal caused mainly by several species of saprophytic fungi. Lamisil (Terbinafine) is an allylamine antifungal agent, that is used both in the topical and oral administration for the treatment of dermatophytosis, cutaneous candidiasis, and the pityriasis versicolor. We investigated the activity of clotrimazole, miconazole, nystatin, and Lamisil against the agents of otomycosis.
MATERIALS AND METHODS
Fifteen clinically obtained isolates from otomycosis ( species; n=13, and species, n=2) and 8 environmental isolates of were tested. The disk diffusion method was employed to detect susceptibility. In the present study, the activity of the terbinafine with clotrimazole, miconazole, and nystatin against several isolates of and with different sources were compared.
RESULTS
Out of 23 isolates of , 4(17.4%) and 1(4.4%) were resistant to nystatin and miconazole, respectively. In addition, all tested organisms were sensitive to clotrimazole and terbinafine. Statistical analysis has shown that there are no significant differences on the effects of clotrimazole, miconazole and, terbinafine on saprophytic (environmental) and pathogenic isolates of , , and (P value= 0.85). In addition, all tested organisms were found to be highly susceptible to terbinafine (P< 0.04).
CONCLUSION
This is a new approach for the possible use of Lamisil for the treatment of otomycosis
PubMed: 28680976
DOI: 10.18869/acadpub.cmm.1.1.18 -
Journal of Clinical Laboratory Analysis Dec 2021Metabolic abnormalities in patients with gastric adenocarcinoma lead to drug resistance and poor prognosis. Therefore, this study aimed to explore biomarkers that can...
BACKGROUND
Metabolic abnormalities in patients with gastric adenocarcinoma lead to drug resistance and poor prognosis. Therefore, this study aimed to explore biomarkers that can predict the prognostic risk of gastric adenocarcinoma by analyzing drug metabolism-related genes.
METHODS
The RNA-seq and clinical information on gastric adenocarcinoma were downloaded from the UCSC and gene expression omnibus databases. Univariate and least absolute shrinkage and selection operator regression analyses were used to identify the prognostic gene signature of gastric adenocarcinoma. The relationships between gastric adenocarcinoma prognostic risk and tumor microenvironment were assessed using CIBERSORT, EPIC, QUANTISEQ, MCPCounter, xCell, and TIMER algorithms. The potential drugs that could target the gene signatures were predicted in WebGestalt, and molecular docking analysis verified their binding stabilities.
RESULTS
Combined with clinical information, an eight-gene signature, including GPX3, ABCA1, NNMT, NOS3, SLCO4A1, ADH4, DHRS7, and TAP1, was identified from the drug metabolism-related gene set. Based on their expressions, risk scores were calculated, and patients were divided into high- and low-risk groups, which had significant differences in survival status and immune infiltrations. Risk group was also identified as an independent prognostic factor of gastric adenocarcinoma, and the established prognostic and nomogram models exhibited excellent capacities for predicting prognosis. Finally, miconazole and niacin were predicted as potential therapeutic drugs for gastric adenocarcinoma that bond stably with NOS3 and NNMT through hydrogen interactions.
CONCLUSIONS
This study proposed a drug metabolism-related eight-gene signature as a potential biomarker to predict the gastric adenocarcinoma prognosis risks.
Topics: Adenocarcinoma; Adult; Aged; Biomarkers, Tumor; Glyburide; Humans; Inactivation, Metabolic; Miconazole; Middle Aged; Molecular Docking Simulation; Nomograms; Prognosis; Protein Interaction Maps; Proteins; Reproducibility of Results; Risk Factors; Stomach Neoplasms; Tumor Microenvironment
PubMed: 34773716
DOI: 10.1002/jcla.24085