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1.
Pharmaceuticals (Basel) ; 17(5)2024 Apr 24.
Artículo en Inglés | MEDLINE | ID: mdl-38794118

RESUMEN

Miconazole nitrate (MCNR), an antifungal drug, is used to treat superficial infections. The objective of the current study was to assess the antifungal effectiveness of MCNR-loaded transethosomal gel (MNTG) against Candida albicans in an in vivo rat model. The outcomes were compared with those of the miconazole nitrate gel (MNG) and marketed Daktarin® cream (2%) based on histopathological and hematological studies. The results of the skin irritation test revealed the safety profile of the MNTG. The MNTG demonstrated the greatest antifungal activity in the histological analysis and the visible restoration of the skin, and the rats revealed an apparent evidence of recovery. Compared to the untreated group, the treated group's lymphocyte and white blood cells counts increased, but their eosinophil counts decreased. In conclusion, MNTG exhibited the greatest antifungal activity, which might be connected to the improved skin permeability of the transethosome's nanosized vesicles. Therefore, it could be considered a promising carrier for topical usage and the treatment of cutaneous candidiasis. More clinical research needs to be performed in order to demonstrate its effectiveness and safe usage in humans.

2.
IMA Fungus ; 15(1): 5, 2024 Mar 08.
Artículo en Inglés | MEDLINE | ID: mdl-38454527

RESUMEN

BACKGROUND: Chromoblastomycosis is the World Health Organization (WHO)-recognized fungal implantation disease that eventually leads to severe mutilation. Cladophialophora carrionii (C. carrionii) is one of the agents. However, the pathogenesis of C. carrionii is not fully investigated yet. METHODS: We investigated the pathogenic potential of the fungus in a Galleria mellonella (G. mellonella) larvae infection model. Six strains of C. carrionii, and three of its environmental relative C. yegresii were tested. The G. mellonella model was also applied to determine antifungal efficacy of amphotericin B, itraconazole, voriconazole, posaconazole, and terbinafine. RESULTS: All strains were able to infect the larvae, but virulence potentials were strain-specific and showed no correlation with clinical background of the respective isolate. Survival of larvae also varied with infection dose, and with growth speed and melanization of the fungus. Posaconazole and voriconazole exhibited best activity against Cladophialophora, followed by itraconazole and terbinafine, while limited efficacy was seen for amphotericin B. CONCLUSION: Infection behavior deviates significantly between strains. In vitro antifungal susceptibility of tested strains only partly explained the limited treatment efficacy in vivo.

3.
Cureus ; 15(5): e38637, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-37284395

RESUMEN

INTRODUCTION: The oral cavity is considered to be one of the most intricate environments in the human body. It is known to harbor commensal microorganisms that do not cause diseases, such as Candida albicans, a yeast fungus that has a carriage rate that tends to increase with age. It is worth noting that C. albicans can be readily identified within the flora of the gastrointestinal tract in 80% of healthy patients. Traditional medicine has alternatively been shown to play a key role in various health amenities with a wide spectrum anti-microbial effect against various yeast molds. OBJECTIVES: To evaluate the antifungal efficacy of pure garlic, onion, and lemon juice extracts against C. albicans. Materials and methods: C. albicans (ATCC 10231) were sub-cultured in brain agar followed by anaerobic incubation for 48 hours at 37°C. Ten plates were used for each of the materials studied to evaluate their antifungal efficacy against C. albicans. The efficiency of commercially available fresh garlic, onion, and lemon was tested in isolation against C. albicans. One-way ANOVA and chi-square were used for comparison between the different materials. The inhibition zone was measured, and the level of statistical significance was set at ≤0.05. RESULTS: The diameter of inhibition zones has been measured along the vertical and horizontal axis. No inhibition zones were observed for the onion and lemon extracts used in this study whereas the garlic extract exhibited inhibition zones with altered sizes (4.89 ± 0.275). A highly significant difference was observed between groups (P = 0.000) and between garlic and the other materials (P = 0.000). CONCLUSIONS: Pure garlic showed a highly significant antifungal efficacy when compared to the onion and lemon juice extracts against C. albicans. Further studies are needed using different concentrations of onion, lemon, and lemon peel juice to confirm their antifungal efficacy in addition to their actual antimicrobial benefits.

4.
J Pharm Sci ; 112(2): 562-572, 2023 02.
Artículo en Inglés | MEDLINE | ID: mdl-36096286

RESUMEN

Vaginal candidiasis is a common form of infection in women caused by Candida species. Due to several drawbacks of conventional treatments, the current research is attempted to formulate and optimize a miconazole nitrate-loaded in situ spray gel for vaginal candidiasis. The stimuli-responsive (pH and thermo-responsive) polymers selected for the in situ gel were chitosan and poloxamer 407, respectively, whereas hydroxypropyl methylcellulose (HPMC) was introduced in the formulation to further improve the mucoadhesive property. The dispersion of each polymer was carried out using the cold method, whereas the optimization of the formulation was achieved using Box-Behnken statistical design considering viscosity and gelation temperature as dependent variables. Present design achieved the optimized outcome with HPMC, poloxamer and chitosan at 0.52% (w/v), 18.68% (w/v) and 0.41% (w/v), respectively. Evaluation of drug-excipients compatibility was performed using differential scanning calorimetry, Fourier transform infrared spectroscopy, and thermogravimetric analysis where the results showed the absence of any chemical interaction between the polymers and drug component. The optimized formulation showed gelation temperature at 31°C allowing in situ phase transition in a vaginal environment; pH of 4.21 is suitable for use in the vaginal cavity, and appropriate viscosity (290 cP) at storage temperature (below 30°C) would allow spraying at ease, whereas strong mucoadhesive force (22.4±0.513 g) would prevent leaking of the formulation after application. The drug release profile showed sustained release up to 24 h with a cumulative drug release of 81.72%, which is significantly better than the marketed miconazole nitrate cream. In addition, an improved antifungal activity could be correlated to the sustained release of the drug from the formulation. Finally, the safety of the formulation was established while tested on HaCaT cell lines. Based on our findings, it could be concluded that the in situ hydrogel formulation using stimuli-responsive polymers could be a viable alternative to the conventional dosage form that can help to reduce the frequency of administration with ease of application to the site of infection, thus will provide better patient compliance.


Asunto(s)
Candidiasis Vulvovaginal , Quitosano , Femenino , Humanos , Miconazol/química , Miconazol/uso terapéutico , Preparaciones de Acción Retardada/química , Quitosano/química , Candidiasis Vulvovaginal/tratamiento farmacológico , Antifúngicos/química , Poloxámero/química , Geles/química
5.
J Oral Maxillofac Pathol ; 27(4): 693-699, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-38304524

RESUMEN

Background: The oral health of individuals is undoubtedly affected by the fact that fungal microorganisms are currently resistant to the conventional antifungal drugs used. Still, there are numerous emerging therapeutic alternatives available like phytotherapy. The phytochemistry of various plant species has indicated that phytochemicals could be a better source of medicine with outstanding antifungal, healing, anti-inflammatory spectrum, and antioxidant properties. Aim: To evaluate the antifungal efficacy of silver nanoparticles of vanilla pods against Candida albicans, Candida glabrata, and Candida krusei and to compare with Fluconazole. Materials and Methods: The vanilla pods were procured from the organic store. The aqueous extracts were prepared. Ten percent of the vanilla extract was utilized to generate the silver nanoparticles. The generated silver nanoparticles were characterized visually based on color change and confirmed by UV spectroscopy. Disk diffusion method was used to determine the antifungal activity of the vanilla pods reinforced silver nanoparticles at different concentrations (20 µl, 40 µ, 40n µ, and 80 µand 80ratioC. albicans, C. glabrata, and C. krusei. The antifungal efficacy of the produced nanoparticles was evaluated against a standard of ketoconazole (30 µ30. Results: Vanillin silver nanoparticles exhibit commendable antifungal activity against C. albicans, C. glabrata which is equivalent to that of ketoconazole, and amplified activity against drug-resistant C. krusei was evident. Conclusion: Silver nanoparticles from vanilla pods were studied and their wider zones of inhibition indicated exemplary antifungal efficacy compared with conventional antifungal drugs like ketoconazole. Clinical significance: Future research on vanillin nanocarrier systems might enhance their stability, bioavailability, and bioactivity. As an outcome, with some promising advances in this area, it would be captivating to pursue a systematic investigation into the potential effects of vanillin at the cellular and molecular levels. This will enable us to further assess its applicability as an active biopharmaceutical ingredient in mouthwashes, probiotic lozenges, and denture resin for use as an effective strategy against the biofilm growth of various Candida species.

6.
Microsc Res Tech ; 85(12): 3755-3760, 2022 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-36259632

RESUMEN

Candida albicans is a microorganism that causes root canal infections. However, it cannot be eliminated with conventional irrigation solutions. Recently, silver nanoparticles (AgNPs) have become popular for their superior antimicrobial effects. The purpose of this study was to evaluate the antifungal effect of AgNPs to C. albicans comparing with 5.25% sodium hypochlorite (NaOCl) and 2% chlorhexidine (CHX). Silver nanoparticles were synthesized by chemical reduction method. Minimum inhibitory concentration and minimum fungicidal concentration of AgNPs against C. albicans strain were determined according to microdilution method reported by Clinical Laboratory Standards Institute. C. albicans biofilm layer was formed on the dentin blocks for 10 days. The biofilm structure was observed by scanning electron microscopy. Statistical analysis was performed with one way analysis of variance analysis and group comparisons were performed with Tukey test. AgNPs showed the highest antifungal effect among the groups. 5.25% NaOCl showed the lowest antifungal effect among the groups. While the 2% CHX solution had a statistically lower antifungal effect than AgNPs, it was found to have a higher effect than NaOCl (p < .016). Nanoparticles present a wide research field as an alternative irrigation solution in root canal treatment. The antifungal effect of AgNPs against C. albicans was confirmed in this study. Further in vivo studies should evaluate the conditions of use and long-term prognosis of AgNPs.


Asunto(s)
Candida albicans , Nanopartículas del Metal , Antifúngicos/farmacología , Antifúngicos/química , Hipoclorito de Sodio/farmacología , Clorhexidina/farmacología , Plata/farmacología , Plata/química , Nanopartículas del Metal/química
7.
Nanomaterials (Basel) ; 12(17)2022 Sep 02.
Artículo en Inglés | MEDLINE | ID: mdl-36080085

RESUMEN

This study investigated the surface properties, biocompatibility, and antifungal activity against Candida albicans of a denture-relining material coated with zinc-bound phosphate-based glass. First, zinc-bound phosphate-based glass was fabricated. A polymerized denture-relining disk was coated with zinc-bound phosphate-based glass (2%, 4%, and 6%). The surface properties of the control and experimental groups were measured, including the wettability, microhardness, color difference, and gloss. The biocompatibility was evaluated using the MTT assay according to ISO 10993-5. The antifungal activity was investigated by counting the number of colony-forming units of Candida albicans. The results were analyzed using a one-way ANOVA and Tukey's test (p = 0.05). The results of this study indicate that, despite the antimicrobial effect of zinc-bound phosphate-based glass, a coated denture-relining material does not degrade the surface properties and biocompatibility. Therefore, this novel material is considered promising for use as a dental material with antimicrobial properties that can potentially prevent denture stomatitis.

8.
Cureus ; 14(7): e27226, 2022 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-36035048

RESUMEN

Background Most pulpal and periapical problems could be treated nonsurgically. However, in cases of infections, certain operations must be performed that require using materials with good antibacterial and antifungal efficacy. ProRoot mineral trioxide aggregate (MTA) was marketed as gray- and white-colored preparations, composed of 75% Portland cement, 20% bismuth oxide, and 5% gypsum by weight. MTA, composed of powder and liquid as distilled water, formed a colloidal gel that further solidified and formed a hard cement within approximately four hours. The new endodontic material Kids e-MTA (Kids-e-dental, Mumbai, India) was introduced recently. It was also available as powder and liquid. It was a bioactive cement consisting of very fine hydrophilic particles of several mineral oxides. Aim This study compares the antimicrobial and antifungal efficacy of e-MTA (mineral trioxide aggregate) (Kids-e-dental, Mumbai, India), ProRoot MTA (Dentsply Sirona, Tulsa Dental, OK, USA), and glass ionomer cement (GIC) (GC Asia Dental Pte Ltd, Singapore). Materials and methods The agar diffusion method was used to test the materials. e-MTA, ProRoot MTA, and GIC were tested for their antibacterial efficacy against Enterococcus faecalis and antifungal efficacy against Candida albicans. The zone of inhibition was calculated and measured using a precision ruler. The collected data was put through Student's unpaired t-test. Results and conclusions On conducting the tests and comparing the results, it was found that e-MTA had a slightly better antibacterial efficacy and almost similar antifungal efficacy compared to ProRoot MTA but significantly superior properties compared to GIC.

9.
J Xenobiot ; 12(2): 74-90, 2022 Apr 14.
Artículo en Inglés | MEDLINE | ID: mdl-35466214

RESUMEN

Biopolymers such as chitosan and gum acacia are used for nanotechnological applications due to their biosafety and ecofriendly nature. The commercial fungicide mancozeb (M) was loaded into chitosan-gum acacia (CSGA) polymers to form nanocomposite (NC) CSGA-M (mancozeb-loaded) measuring 363.6 nm via the ionic gelation and polyelectrolyte complexation method. The physico-chemical study of nano CSGA-M was accomplished using dynamic light scattering (DLS), scanning electron microscope (SEM), transmission electron microscope (TEM), X-ray diffraction (XRD), and thermogravimetric analysis (TGA). Nano CSGA-M-1.0 (containing 1.0 mg/mL mancozeb) at 1.5 ppm demonstrated a maximum inhibition (83.8 ± 0.7%) against Alternaria solani, while Sclerotinia sclerotiorum exhibited a 100% inhibition at 1.0 and 1.5 ppm through the mycelium inhibition method. Commercial mancozeb showed an inhibition of 84.6 ± 0% and 100%, respectively, for both fungi. In pot house conditions, NCs were found to exhibit good antimicrobial activity. Disease control efficiency (DCE, in %) in pathogen-treated plants for CSGA-M-1.0 was 64.6 ± 5.0 and 60.2 ± 1.4% against early blight and stem rot diseases, respectively. NCs showed lower cytotoxicity than commercial mancozeb at the given concentration. In conclusion, both in vitro and in vivo antifungal efficacy for nano CSGA-M was found to be quite comparable but less toxic than mancozeb to Vero cell lines; thus, in the future, this formulation may be used for sustainable agriculture.

10.
mBio ; 13(2): e0011522, 2022 04 26.
Artículo en Inglés | MEDLINE | ID: mdl-35380453

RESUMEN

The azole antifungals inhibit sterol 14α-demethylase (S14DM), which depletes cellular ergosterol and promotes synthesis of the dysfunctional lipid 14α-methylergosta-8,24(28)-dien-3ß,6α-diol, ultimately arresting growth. Mutations that inactivate sterol Δ5,6-desaturase (Erg3p), the enzyme that produces the sterol-diol upon S14DM inhibition, enhances Candida albicans growth in the presence of the azoles. However, erg3 null mutants are sensitive to some physiological stresses and can be less virulent than the wild type. These fitness defects may disfavor the selection of null mutants within patients. The objective of this study was to investigate the relationship between Erg3p activity, C. albicans pathogenicity, and the efficacy of azole therapy. An isogenic panel of strains was constructed that produce various levels of the ERG3 transcript. Analysis of the sterol composition confirmed a correspondingly wide range of Erg3p activity. Phenotypic analysis revealed that even moderate reductions in Erg3p activity are sufficient to greatly enhance C. albicans growth in the presence of fluconazole in vitro without impacting fitness. Moreover, even low levels of Erg3p activity are sufficient to support full virulence of C. albicans in the mouse model of disseminated infection. Finally, while the antifungal efficacy of fluconazole was similar for all strains in immunocompetent mice, there was an inverse correlation between Erg3p activity and the capacity of C. albicans to endure treatment in leukopenic mice. Collectively, these results establish that relative levels of Erg3p activity determine the antifungal efficacy of the azoles upon C. albicans and reveal the critical importance of host immunity in determining the clinical impact of this resistance mechanism. IMPORTANCE Mutations that completely inactivate Erg3p enable the prevalent human pathogen C. albicans to endure the azole antifungals in vitro. However, such null mutants are less frequently identified in azole-resistant clinical isolates than other resistance mechanisms, and previous studies have reported conflicting outcomes regarding antifungal resistance of these mutants in animal models of infection. The results of this study clearly establish a direct correlation between the level of Erg3p activity and the antifungal efficacy of fluconazole within a susceptible mammalian host. In addition, low levels of Erg3p activity are apparently more advantageous for C. albicans survival of azole therapy than complete loss of function. These findings suggest a more nuanced but more important role for Erg3p as a determinant of the clinical efficacy of the azole antifungals than previously appreciated. A revised model of the relationship between Erg3p activity, host immunity, and the antifungal susceptibility of C. albicans is proposed.


Asunto(s)
Antifúngicos , Candida albicans , Animales , Antifúngicos/farmacología , Antifúngicos/uso terapéutico , Azoles/farmacología , Fluconazol/farmacología , Fluconazol/uso terapéutico , Humanos , Mamíferos , Ratones , Pruebas de Sensibilidad Microbiana , Oxidorreductasas , Esteroles , Virulencia
11.
J Contemp Dent Pract ; 22(2): 162-165, 2021 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-34257176

RESUMEN

AIM: The study aimed to investigate the antifungal effects of herbal extracts and fluconazole on heat-polymerized acrylic denture base resin as a denture cleanser. MATERIALS AND METHODS: Several essential oils, such as origanum oil and grape seed oil and commercially available antifungal agent fluconazole were used as denture cleansers and their antifungal efficacy was evaluated using a spectrophotometer. Overall, 68 samples were obtained and were divided into four groups, each containing 17 samples. These samples were immersed in Sabouraud dextrose broth consisting of Candida albicans for 16 hours and later in these antifungal solutions for 8 hours and their antifungal efficacy was measured. Data were subjected to an ANOVA test. RESULTS: Among the study groups origanum oil showed the maximum antifungal activity with a mean optical density at 0.072 ± 0.014 followed by fluconazole (0.094 ± 0.155), and least by grape seed oil (0.190 ± 0.071). CONCLUSION: Results of this in vitro study showed that origanum oil was more effective than commercially available antifungal agents, and among the tested groups oregano oil was a potential agent in lowering the C. albicans colony. CLINICAL SIGNIFICANCE: Origanum oil, being a herbal product, can be considered as a denture cleanser and also be used as an effective alternative to commercially available antifungal agents without any side effects.


Asunto(s)
Antifúngicos , Fluconazol , Resinas Acrílicas , Antifúngicos/farmacología , Bases para Dentadura , Limpiadores de Dentadura , Fluconazol/farmacología , Calor , Extractos Vegetales/farmacología
12.
Molecules ; 26(5)2021 Mar 07.
Artículo en Inglés | MEDLINE | ID: mdl-33799919

RESUMEN

Herein, we investigated the surface characterization and biocompatibility of a denture-lining material containing Cnidium officinale extracts and its antifungal efficacy against Candida albicans. To achieve this, a denture-lining material containing various concentrations of C. officinale extract and a control group without C. officinale extract were prepared. The surface characterization and biocompatibility of the samples were investigated. In addition, the antifungal efficacy of the samples on C. albicans was investigated using spectrophotometric growth and a LIVE/DEAD assay. The results revealed that there was no significant difference between the biocompatibility of the experimental and control groups (p > 0.05). However, there was a significant difference between the antifungal efficiency of the denture material on C. albicans and that of the control group (p < 0.05), which was confirmed by the LIVE/DEAD assay. These results indicate the promising potential of the C. officinale extract-containing denture-lining material as an antifungal dental material.


Asunto(s)
Antifúngicos/farmacología , Candida albicans/efectos de los fármacos , Cnidium/química , Alineadores Dentales , Extractos Vegetales/farmacología , Antifúngicos/química , Antifúngicos/toxicidad , Línea Celular , Color , Alineadores Dentales/microbiología , Fibroblastos/efectos de los fármacos , Humanos , Ensayo de Materiales , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Extractos Vegetales/toxicidad , Propiedades de Superficie
13.
Artículo en Inglés | MEDLINE | ID: mdl-33468480

RESUMEN

We analyzed the relationship between itraconazole (ITZ) and hydroxy-itraconazole (OH-ITZ) levels in 1,223 human samples. Overall, there was a statistically significant correlation between ITZ and OH-ITZ levels (Pearson's r, 0.7838), and OH-ITZ levels were generally higher than ITZ levels (median OH-ITZ:ITZ ratio, 1.73; range, 0.13 to 8.96). However, marked variability was observed throughout the range of ITZ concentrations. Thus, it is difficult to predict OH-ITZ concentrations based solely on ITZ levels.


Asunto(s)
Antifúngicos , Itraconazol , Antifúngicos/uso terapéutico , Humanos
14.
J Contemp Dent Pract ; 22(11): 1227-1231, 2021 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-35343445

RESUMEN

AIM AND OBJECTIVE: This paper aims to compare the antifungal efficacy of four concentrations of Minthostachys mollis essential oil (MEO) against Candida albicans ATCC 10231. MATERIALS AND METHODS: This study was conducted in vitro. Ten kilograms of M. mollis (Muña) were collected in the city of Tarma, Peru. The plant was then dried in the shade at room temperature (21°C), and the essential oil was obtained through distillation. C. albicans ATCC 10231 was cultured at a MacFarland scale of 0.5, which corresponds to a concentration of 3 × 108 CFU/mL. Each plate was filled with one of the four MEO concentrations (25, 50, 75, or 100%), dimethyl sulfoxide (negative control), or fluconazole (positive control), a known antifungal agent. After incubation, each plate was examined using the Kirby-Bauer method. RESULTS: Compared to MEO 25%, MEO 50%, and MEO 75%, MEO 100% had the highest antifungal efficacy at 24, 48, and 72 hours of evaluation, with an average of 18.9 ± 0.7, 18.2 ± 0.7, and 17.0 ± 0.4 mm, respectively. However, fluconazole had higher efficacy (27.9 ± 0.5, 27.5 ± 0.5, and 23.7 ± 0.7 mm, respectively). Post hoc analysis showed that there were significant differences between all concentrations of the MEO groups and their respective positive and negative control groups (p <0.001). CONCLUSION: Among the MEO groups, the pure concentration (MEO 100%) had the highest antifungal efficacy. However, fluconazole presented greater efficacy, and the differences were statistically significant. CLINICAL SIGNIFICANCE: This research allowed to know the efficacy of this natural resource against one of the most prevalent fungi in the oral cavity. Therefore, a line of research could be opened to deepen its potential benefits for oral health.


Asunto(s)
Candida albicans , Aceites Volátiles , Antifúngicos/farmacología , Fluconazol/farmacología , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/farmacología
15.
ACS Infect Dis ; 6(8): 2029-2044, 2020 08 14.
Artículo en Inglés | MEDLINE | ID: mdl-32598131

RESUMEN

Amphotericin B (AmB, 1) is the drug of choice for treating the most serious systemic fungal or protozoan infections. Nevertheless, its application is limited by low solubility in aqueous media and serious side effects such as infusion-related reactions, hemolytic toxicity, and nephrotoxicity. Owing to these limitations, it is essential to search for the polyene derivatives with better chemotherapeutic properties. With the objective of obtaining AmB derivatives with lower self-aggregation and improved solubility, we synthesized a series of amides of AmB bearing an additional basic group in the introduced residue. The screening of antifungal activity in vitro revealed that N-(2-aminoethyl)amide of AmB (amphamide, 6) had superior antifungal activity compared to that of the paternal AmB. Preclinical studies in mice confirmed that compound 6 had a much lower acute toxicity and higher antifungal efficacy in the model of mice candidosis sepsis compared with that of AmB (1). Thus, the discovered amphamide is a promising drug candidate for the second generation of polyene antibiotics and is also prospective for in-depth preclinical and clinical evaluation.


Asunto(s)
Antibacterianos , Preparaciones Farmacéuticas , Anfotericina B/farmacología , Animales , Antibacterianos/farmacología , Antifúngicos/farmacología , Antifúngicos/uso terapéutico , Ratones , Polienos/farmacología , Estudios Prospectivos
16.
Mycoses ; 63(8): 869-875, 2020 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-32406142

RESUMEN

BACKGROUND: Matrix-assisted laser desorption ionisation mass spectrometry imaging (MALDI-MSI) is a mass spectrometry-based technique, which can be applied for compound-specific imaging of pharmaceuticals in tissues samples. MALDI-MSI technology is widely used to visualise penetration and distribution profile through different tissues but has never been used with nail tissue. OBJECTIVES: This study used MALDI-MSI technology to visualise distribution profile and penetration into ex vivo human mycosis-infected toenails of three antifungal active ingredients amorolfine, ciclopirox and naftifine contained in topical onychomycosis nail treatment preparations, marketed as Loceryl® , Ciclopoli® and Exoderil® . METHODS: Three mycosis-infected toenails were used for each treatment condition. Six and twenty-four hours after one single topical application of antifungal drugs, excess of formulation was removed, nails were cryo-sectioned at a thickness of 20 µm, and MALDI matrix was deposited on each nail slice. Penetration and distribution profile of amorolfine, ciclopirox and naftifine in the nails were analysed by MALDI-MSI. RESULTS: All antifungal actives have been visualised in the nail by MALDI-MSI. Ciclopirox and naftifine molecules showed a highly localised distribution in the uppermost layer of the nail plate. In comparison, amorolfine diffuses through the nail plate to the deep layers already 6 hours after application and keeps diffusing towards the lowest nail layers within 24 hours. CONCLUSIONS: This study shows for the first-time distribution and penetration of certain antifungal actives into human nails using MALDI-MSI analysis. The results showed a more homogeneous distribution of amorolfine to nail and a better penetration through the infected nails than ciclopirox and naftifine.


Asunto(s)
Antifúngicos/farmacología , Onicomicosis/diagnóstico por imagen , Espectrometría de Masa por Láser de Matriz Asistida de Ionización Desorción/métodos , Administración Tópica , Alilamina/administración & dosificación , Alilamina/análogos & derivados , Alilamina/farmacología , Alilamina/uso terapéutico , Antifúngicos/administración & dosificación , Antifúngicos/uso terapéutico , Ciclopirox/administración & dosificación , Ciclopirox/farmacología , Ciclopirox/uso terapéutico , Humanos , Laca , Morfolinas/administración & dosificación , Morfolinas/farmacología , Morfolinas/uso terapéutico , Uñas/microbiología , Uñas/patología , Onicomicosis/tratamiento farmacológico
17.
BMC Microbiol ; 20(1): 95, 2020 04 15.
Artículo en Inglés | MEDLINE | ID: mdl-32295517

RESUMEN

BACKGROUND: The microbiome of Severe-Early Childhood Caries (S-ECC), is characterized by an ecosystem comprising bacterial and fungal species, with a predominance of Candida species. Hence, an anti-cariogen effective against both bacteria and fungi would be valuable in the management of S-ECC. Here we evaluate the antifungal effect of silver diamine fluoride (SDF) against 35-clinical yeast isolates (Ten-each of C. albicans, C. krusei, C. tropicalis and five C. glabrata strains) from dentinal caries-lesions from S-ECC. RESULTS: Disc-diffusion and time-kill assays as well as MIC50 and MIC90 evaluations against therapeutic concentrations confirmed the broad-spectrum anti-candidal potency of SDF. Ultrastructural images revealed morphologic aberrations of yeast-cell walls on exposure to SDF. All C. krusei and C. glabrata isolates were significantly more sensitive to SDF, relative to the standard antifungal fluconazole. Further, SDF appears to effectively abrogate filamentation of C. albicans even at very low concentrations. CONCLUSIONS: Our data, for the first time, elucidate the antifungal potency of SDF, in addition to its known antibacterial activity, in the management of S-ECC.


Asunto(s)
Antifúngicos/farmacología , Candida/crecimiento & desarrollo , Caries Dental/prevención & control , Compuestos de Amonio Cuaternario/farmacología , Compuestos de Plata/farmacología , Biopelículas/efectos de los fármacos , Candida/clasificación , Candida/efectos de los fármacos , Candida/ultraestructura , Pared Celular/efectos de los fármacos , Pared Celular/ultraestructura , Niño , Farmacorresistencia Fúngica/efectos de los fármacos , Fluoruros Tópicos/farmacología , Humanos , Pruebas de Sensibilidad Microbiana
18.
J Int Soc Prev Community Dent ; 10(6): 724-730, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-33437705

RESUMEN

OBJECTIVE: The objective of this study was to compare in vitro the antifungal efficacy of the essential oil of Cinnamomum zeylanicum (Canela) (EOC) at 25%, 50%, 75%, and 100% against strains of Candida albicans ATCC 10231. MATERIALS AND METHODS: The design was experimental, in vitro, prospective, and longitudinal study, having a sample of n = 30 petri dishes per six groups. The test was conducted in the microbiology laboratory of the Universidad Nacional Federico Villarreal. The essential oil was prepared by steam distillation, which means that the pressure steam enters in connection with the plant cells and breaks them, releasing the essence and trapping it in drops of water. Cinnamon essential oil was obtained using the hydrodistillation method, subsequently the oil obtained was dehydrated with sodium sulfate and then filtered at 0.22 µm. Then the vials were stored at a temperature of 4°C. Finally, Candida albicans ATCC 10231 was used as the biological material. Antifungal efficacy was measured by the Kirby-Bauer method (disk diffusion). RESULTS: It was found that in the 24-h group the concentration that had the greatest antifungal effect was 100% EOC with a mean of 22.1 ± 11 mm; however, the lowest antifungal activity was seen in the 25% EOC with 17.9 ± 1.6 mm. On the contrary, in the 48-h group, it was shown that the highest antifungal efficacy was also observed in the 100% EOC with an average of 31.2 ± 3.2 mm, but the lowest antifungal activity was in the 25% EOC with 22.6 ± 1.7 mm. Although in both groups, both at 24 and 48h, nystatin was the one with the lowest antifungal efficacy 15.1 ± 1.0 and 19.9 ± 0.1 mm, respectively. CONCLUSIONS: EOC had a better statistically significant antifungal effect compared to nystatin. Otherwise, on analysis of the results in different concentrations, the EOC showed a directly proportional antifungal effectiveness as the concentration against the strains of C. albicans ATCC 10231 increased, compared to nystatin, suggesting its potential use as a possible attractive therapeutic alternative for the control of diseases caused by strains of C. albicans resistant to nystatin.

19.
Indian J Community Med ; 44(Suppl 1): S77-S80, 2019 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31728098

RESUMEN

BACKGROUND: Candida species are normal commensals and are isolated intra-orally in 17%-75% of healthy individuals and all debilitated people. Eradication of candidiasis is complicated by the emergence of Candida strains that are resistant to the currently used antifungal agents. Plants as remedies are gaining popularity in developed countries. Although many plants have already been investigated against Candida albicans, the search is still to find a long-term prevention or cure for oral candidiasis. OBJECTIVES: The objective of this study was (1) to evaluate the antifungal activity of black pepper, bay leaf, cinnamon, and cumin against C. albicans and (2) to determine the minimum inhibitory concentration (MIC) of spice extracts against C. albicans. MATERIALS AND METHODS: Spices obtained from the local market were dried and powdered. Solvent extracts were obtained by maceration with methanol followed by filtration and evaporation. The antifungal efficacy was assessed using cup-plate diffusion method followed by the determination of MIC by serial tube dilution technique. Statistical analysis was done using one-way analysis of variance followed by Tukey's post hoc test. P < 0.05 was considered as statistically significant. RESULTS: All the extracts evaluated showed variable degree of inhibition zones against C. albicans with cinnamon showing the highest inhibition (49.3 ± 0.52) mm and also with least MIC against C. albicans (<0.05 mg/ml). CONCLUSION: These results exhibit the antifungal activity of the spice extracts against C. albicans, which may be useful in the treatment of oral candidiasis.

20.
AAPS PharmSciTech ; 20(5): 175, 2019 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-31028492

RESUMEN

Clotrimazole is widely used for the management of cutaneous candidiasis infection. The low solubility of clotrimazole and excipient-related topical side effects (of currently available marketed products) cause the compromised efficacy of the therapy with poor patient compliance. In the present investigation, a clotrimazole nanocrystal-based nanogel was developed. Clotrimazole nanocrystals were optimized with studying the impact of individual process parameters of the media milling technique. The optimum level of individual process parameters was considered in the development of optimized batches. A promising result was obtained with a non-ionic stabilizer, polysorbate 80, at a concentration of 1.5%w/v, showing a distinct reduction in the particle size from above 31 µm to 264 nm and a polydispersity index of 0.211 with media milling at 1500 rpm for 6 h. This result was found to be in concordance with the TEM images, revealing a sharp diminution in particle morphology. Powder X-ray diffraction and differential scanning calorimetry results revealed crystallinity of clotrimazole (CTZ) in nanocrystal form. The optimized nanocrystal suspension was formulated into nanogel with carbopol 934, having a viscosity of 86.43 ± 2.06 Pa s at 25°C, which enhanced the ease of application of CTZ nanocrystals topically. A diffusion study showed around 82% of CTZ is transported across the membrane with the flux of 110.07 µg cm-2 h-1. In vivo results of the nanogel revealed improvement in CTZ release with 52% CTZ retention in different strata of the skin. The developed nanogel showed a significant improvement in the eradication of fungal infection within 10 days of application over Candida albicans-induced Wistar rat model. In a nutshell, the CTZ nanocrystal-loaded nanogel could achieve the goal of retaining CTZ in skin layers providing a prolonged effect and was able to treat cutaneous candidiasis in a short span with improved compliance for the candidiasis patients.


Asunto(s)
Antifúngicos/administración & dosificación , Antifúngicos/uso terapéutico , Candidiasis Cutánea/tratamiento farmacológico , Clotrimazol/administración & dosificación , Clotrimazol/uso terapéutico , Animales , Antifúngicos/efectos adversos , Candida albicans/efectos de los fármacos , Candidiasis Cutánea/microbiología , Clotrimazol/efectos adversos , Difusión , Composición de Medicamentos , Irritantes , Nanopartículas , Tamaño de la Partícula , Ratas , Ratas Wistar , Absorción Cutánea , Difracción de Rayos X
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