-
Prevalence and drug susceptibility of clinical species in nasopharyngeal cancer patients in Vietnam.One Health (Amsterdam, Netherlands) Jun 2024In the nature, species are normal inhabitants and can be observed in a wide variety of vertebrates. In humans, especially for cancer patients who fall prey to...
In the nature, species are normal inhabitants and can be observed in a wide variety of vertebrates. In humans, especially for cancer patients who fall prey to opportunistic pathogens, this group of susceptible multi-drug resistant and biofilm-forming yeasts, are among the commonest ones. In this study, species in 76 oral lesion samples from Vietnamese nasopharyngeal-cancer patients were isolated, morphologically identified using CHROMagar™, germ tube formation, and chlamydospore formation tests, and molecularly confirmed by PCR-RFLP. The drug susceptibility of these isolates was then tested, and the gene was DNA sequenced to investigate the mechanism of resistance. The results showed that remained the most prevalent species (63.16% of the cases), followed by , , and . The rates of resistance of for tested drugs were 85.71%, 53.57%, and 57.14% to fluconazole, clotrimazole, and miconazole, respectively. Although the drug-resistance rate of was lower than that of , it was higher than expected, suggesting an emerging drug-resistance phenomenon. Furthermore, DNA sequencing revealed different mutations (especially K128T), implying the presence of multiple resistance mechanisms. Altogether, the results indicate an alarming drug-resistance situation in species in Vietnamese cancer patients and emphasize the importance of species identification and their drug susceptibility prior to treatment.
PubMed: 38179314
DOI: 10.1016/j.onehlt.2023.100659 -
Journal of Advanced Pharmaceutical... 2023The reason for conducting this study is to prolong release of miconazole in the ocular site of action by ocular-based gels (OBGs) formulations. The formulation factors...
The reason for conducting this study is to prolong release of miconazole in the ocular site of action by ocular-based gels (OBGs) formulations. The formulation factors affecting on the release from OBG should be studied using various gelling agents in various concentrations to achieve the improvement in retention and residence time in response to prolonged release. In this study, the formulations were prepared using carbopol 940, pectin, sodium alginate, poloxamer 407, and poly(methacrylic acid) at 0.5%, 1%, and 1.5% w/v, respectively. Hydroxypropyl methylcellulose E5 (HPMC E5) 1% was added as thickening agent/viscosity builder. The formulation containing carbopol 940, pectin and sodium alginate at 1.5% w/v, displayed a noticable improvement in viscosity, gelling capacity, and extended release for 7 h in comparison with the reference drug. Overall, the release showed that the sodium alginate with HPMC E5 form gel which had longer time of release reach to 12 h compared with other polymers. the release of miconazole from the OBGs affected significantly by two factors includes gelling capacity and viscosity builder. The novelty of this study is supporting the delivery of ocular drugs through a cornea as an important key of the eye instead of dependence on an internal blood supply using an oral or a parental administration.
PubMed: 38107457
DOI: 10.4103/japtr.japtr_91_23 -
Journal of Medicinal Chemistry Dec 2023Developing drugs for brain infection by is an unmet medical need. We used a combination of cheminformatics, target-, and phenotypic-based drug discovery methods to...
Developing drugs for brain infection by is an unmet medical need. We used a combination of cheminformatics, target-, and phenotypic-based drug discovery methods to identify inhibitors that target an essential enzyme, sterol 14-demethylase (NfCYP51). A total of 124 compounds preselected were tested against . Nine primary hits with EC ≤ 10 μM were phenotypically identified. Cocrystallization with NfCYP51 focused attention on one primary hit, miconazole-like compound . The -enantiomer of produced a 1.74 Å cocrystal structure. A set of analogues was then synthesized and evaluated to confirm the superiority of the -configuration over the -configuration and the advantage of an ether linkage over an ester linkage. The two compounds, - and -, had an improved EC and compared to . Importantly, both were readily taken up into the brain. The brain-to-plasma distribution coefficient of - was 1.02 ± 0.12, suggesting further evaluation as a lead for primary amoebic meningoencephalitis.
Topics: Miconazole; 14-alpha Demethylase Inhibitors; Naegleria fowleri; Drug Discovery
PubMed: 38085955
DOI: 10.1021/acs.jmedchem.3c01898 -
BMC Chemistry Dec 2023Two accurate, sensitive, and selective methods for simultaneous determination of miconazole nitrate (MIC), nystatin (NYS), and metronidazole (MET) in pure state or drug...
Two accurate, sensitive, and selective methods for simultaneous determination of miconazole nitrate (MIC), nystatin (NYS), and metronidazole (MET) in pure state or drug product were established and verified. First, RP-HPLC-DAD was designed. Separation was accomplished using a ZOBRAX Eclipse Plus RP-C column that was running under an isocratic elution of methanol: 0.05% aqueous solution of sodium dodecyl sulphate (40: 60 v/v), with a flow rate that was regulated at 0.8 mL/min. The column temperature was adjusted at 25 °C and diode array detector was monitored at 220 nm. The linearity range of the proposed method was achieved at the concentration of 5-50, 4-50, and 4-40 µg/mL and the attained retention time for the studied drugs was 2.52, 3.52 and 4.99 min for MIC, NYS, and MET, correspondingly. Second, a TLC-densitometric approach was used to resolve the three compounds. Resolution of the three cited drugs was carried out using TLC aluminum plates pre-coated with 0.25 mm silica gel 60 F. A developing solvent comprised ethyl acetate: toluene: methanol: triethyl amine: formic acid (3: 1: 7: 0.3: 0.1 by volume) (pH = 5.5) was utilized and scanning of the resolved bands at 215 nm. Linearity of the developed TLC method was evaluated and evident to be 0.4-2, 0.4-2.2, and 0.4-2 μg/band for MIC, NYS, and MET, in that order. The suggested chromatographic methods were verified according to ICH directives. The findings of the developed chromatographic procedures were statistically compared with the results of the reported ones using student's t-test and F-test. Furthermore, two green assessment tools evaluated the indicated methods' level of greenness (GAPI and AGREE).
PubMed: 38041191
DOI: 10.1186/s13065-023-01083-1 -
HIV/AIDS (Auckland, N.Z.) 2023Oral candidiasis is the most prevalent opportunistic infection in patients with human immunodeficiency virus (HIV) or acquired immunodeficiency syndrome (AIDS),...
INTRODUCTION
Oral candidiasis is the most prevalent opportunistic infection in patients with human immunodeficiency virus (HIV) or acquired immunodeficiency syndrome (AIDS), impacting their quality of life. This report aims to emphasize the importance of clinical assessment and management of HIV/AIDS patients with oral candidiasis to improve their quality of life.
CASE
Five male patients, aged between 32 and 71 years, came to the HIV clinic and complained of white plaques in their mouths and painful swallowing. The World Health Organization's (WHO) clinical staging of all patients was 4. Three patients had not yet received antiretroviral therapy (ART), and their total lymphocyte counts (TLC) of <1.170 cells/mm. Two patients had dropped out of ART with CD4 counts were <40 cells/mm. The body mass index of two patients was underweight, while the others were normal. The oral hygiene index simplified (OHI-S) of the patients was fair to poor. The quality of life assessment using the oral health impact profile 14 (OHIP-14) questionnaires before therapy showed values from 6-20. Clinical examination defined the diagnosis as oral candidiasis, exfoliative cheilitis, oral hairy leukoplakia, and a cytomegalovirus-related ulcer.
CASE MANAGEMENT
The patients were treated with fluconazole, 0.2% chlorhexidine gluconate mouthwash, 2% miconazole cream, diphenhydramine, and multivitamins. The oral lesions were improved within 14 days to a month of treatment, and OHIP-14 scores were significantly reduced (0-3).
CONCLUSION
Clinical assessment is important in managing HIV/AIDS patients with oral candidiasis, which improves the patient's quality of life. Therefore, routine clinical assessment and management of HIV/AIDS patients are strongly recommended.
PubMed: 38028189
DOI: 10.2147/HIV.S434175 -
Clinical Case Reports Nov 2023A simple culturing method for available at a clinical laboratory is a key for making timely diagnosis and starting treatment with topical 0.02% chlorhexidine gluconate...
KEY CLINICAL MESSAGE
A simple culturing method for available at a clinical laboratory is a key for making timely diagnosis and starting treatment with topical 0.02% chlorhexidine gluconate eye drops, together with 0.1% miconazole or fluconazole eye drops.
ABSTRACT
A 19-year-old woman with pain and injection in the right eye showed spotty corneal infiltration and radiating linear opacity. Suspicious of keratitis, corneal scraping, and the soft contact lens were sent to in-house clinical laboratory to culture successfully on Sabouraud dextrose agar plate painted with heat-treated dead bacilli.
PubMed: 38028087
DOI: 10.1002/ccr3.8248 -
Pharmaceutics Oct 2023Miconazole nitrate (MCNR) is a BCS class II antifungal drug with poor water solubility. Although numerous attempts have been made to increase its solubility, formulation...
Miconazole nitrate (MCNR) is a BCS class II antifungal drug with poor water solubility. Although numerous attempts have been made to increase its solubility, formulation researchers struggle with this significant issue. Transethosomes are promising novel nanocarriers for improving the solubility and penetration of drugs that are inadequately soluble and permeable. Thus, the objective of this study was to develop MCNR-loaded transethosomal gel in order to enhance skin permeation and antifungal activity. MCNR-loaded transethosomes (MCNR-TEs) were generated using the thin film hydration method and evaluated for their zeta potential, particle size, polydispersity index, and entrapment efficiency (EE%). SEM, FTIR, and DSC analyses were also done to characterize the optimized formulation of MCNR-TEs (MT-8). The optimized formulation of MCNR-TEs was incorporated into a carbopol 934 gel base to form transethosomal gel (MNTG) that was subjected to ex vivo permeation and drug release studies. In vitro antifungal activity was carried out against through the cup plate technique. An in vivo skin irritation test was also performed on Wistar albino rats. MT-8 displayed smooth spherical transethosomal nanoparticles with the highest EE% (89.93 ± 1.32%), lowest particle size (139.3 ± 1.14 nm), polydispersity index (0.188 ± 0.05), and zeta potential (-18.1 ± 0.10 mV). The release profile of MT-8 displayed an initial burst followed by sustained release, and the release data were best fitted with the Korsmeyer-Peppas model. MCNR-loaded transethosomal gel was stable and showed a non-Newtonian flow. It was found that ex vivo drug permeation of MNTG was 48.76%, which was significantly higher than that of MNPG (plain gel) ( ≤ 0.05) following a 24-h permeation study. The prepared MCNR transethosomal gel exhibited increased antifungal activity, and its safety was proven by the results of an in vivo skin irritation test. Therefore, the developed transethosomal gel can be a proficient drug delivery system via a topical route with enhanced antifungal activity and skin permeability.
PubMed: 38004517
DOI: 10.3390/pharmaceutics15112537 -
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 -
Resurgence and Repurposing of Antifungal Azoles by Transition Metal Coordination for Drug Discovery.Pharmaceutics Sep 2023Coordination compounds featuring one or more antifungal azole (AA) ligands constitute an interesting family of candidate molecules, given their medicinal polyvalence and... (Review)
Review
Coordination compounds featuring one or more antifungal azole (AA) ligands constitute an interesting family of candidate molecules, given their medicinal polyvalence and the viability of drug complexation as a strategy to improve and repurpose available medications. This review reports the work performed in the field of coordination derivatives of AAs synthesized for medical purposes by discussing the corresponding publications and emphasizing the most promising compounds discovered so far. The resulting overview highlights the efficiency of AAs and their metallic species, as well as the potential still lying in this research area.
PubMed: 37896159
DOI: 10.3390/pharmaceutics15102398 -
BMC Oral Health Oct 2023To evaluate the clinical efficacy of photodynamic therapy (PDT) as an adjunct or alternative to traditional antifungal drugs in the treatment of oral candidiasis, and to... (Meta-Analysis)
Meta-Analysis
OBJECTIVE
To evaluate the clinical efficacy of photodynamic therapy (PDT) as an adjunct or alternative to traditional antifungal drugs in the treatment of oral candidiasis, and to provide evidence-based medical evidence for its use in the treatment of oral candidiasis.
METHODS
Computer combined with manual retrieval of China Academic Journals Full-text Database (CNKI), China Biomedical Literature Database (CBM), Chinese Science and Technology Journal Database (VIP), Wanfang Database, PubMed, Web of Science, Cochrane Library, Embase, Scopus retrieval for articles published before January 2023, basic information and required data were extracted according to the inclusion and exclusion criteria, and the Revman V5.4 software was used to conduct Meta-analysis of the included literature.
RESULTS
A total of 11 articles were included, 7 of which used nystatin as an antifungal drug, 2 of which were combined treatment of PDT and nystatin, 2 of the remaining 4 articles were treated with fluconazole, and 2 were treated with miconazole. Meta results showed that PDT was superior to nystatin in reducing the number of oral candida colonies in the palate of patients MD = -0.87, 95%CI = (-1.52,-0.23), P = 0.008, the difference was statistically significant, and the denture site MD = -1.03, 95%CI = (-2.21, -0.15), P = 0.09, the difference was not statistically significant; compared with the efficacy of fluconazole, RR = 1.01, 95%CI = (0.56,1.83), P = 0.96; compared with miconazole RR = 0.55, 95%CI = (0.38, 0.81), P = 0.002; PDT combined with nystatin RR = 1.27, 95%CI = (1.06, 1.52), P = 0.01; recurrence rate RR = 0.28, 95%CI = (0.09, 0.88), P = 0.03.
CONCLUSIONS
PDT was effective in the treatment of oral candidiasis; PDT was more effective than nystatin for the treatment of denture stomatitis in the palate, while there was no significant difference between the two for the denture site; The efficacy of PDT for oral candidiasis was similar to that of fluconazole; PDT was less effective than miconazole for oral candidiasis; Compared with nystatin alone, the combination of PDT and nystatin is more effective in treating oral candidiasis with less risk of recurrence.
Topics: Humans; Candidiasis, Oral; Antifungal Agents; Nystatin; Fluconazole; Miconazole; Photochemotherapy
PubMed: 37884914
DOI: 10.1186/s12903-023-03484-z