scholarly journals Enhanced Efficacy of Thiosemicarbazone Derivative-Encapsulated Fibrin Liposomes against Candidiasis in Murine Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 333
Author(s):  
Azmat Ali Khan ◽  
Amer M. Alanazi ◽  
Nawaf Alsaif ◽  
Nasser Algrain ◽  
Tanveer Ahmad Wani ◽  
...  
Keyword(s):  
Tissue Specificity ◽  
Inhibitory Concentration ◽  
Entrapment Efficiency ◽  
Antifungal Drugs ◽  
Serum Stability ◽  
Antifungal Effects ◽  
Apoptosis And Necrosis ◽  
Antifungal Efficacy ◽  
Mic Value

Candida albicans is the most studied species for the candidiasis infection and is becoming resistant towards existing antifungal drugs. Considering this, in the current study, we developed and characterized a fibrin liposome-based formulation encapsulating a novel thiosemicarbazone derivative, 2C, and evaluated its antifungal efficacy against murine candidiasis. The 2C-containing formulation was prepared by encapsulating 2C within the liposomes (2C-L) that were further encapsulated in the fibrin beads (2C-FL). The in-house synthesized 2C-FLs were spherical with a zeta potential of -34.12 ± 0.3 mV, an entrapment efficiency of 72.6 ± 4.7%, and a loading efficiency of 9.21 ± 2.3%, and they showed a slow and sustained release of 2C. Compared to free 2C, the formulation was non-toxic and exhibited serum stability, increased tissue specificity, and penetration. The 2C-FL formulation had a minimum inhibitory concentration (MIC) value of 4.92 ± 0.76 µg/mL and was able to induce apoptosis and necrosis in C. albicans in vitro. The administration of 2C-FL in C. albicans-infected mice prolonged their survival and antifungal effects when compared with the free 2C. The 2C-FL antifungal therapy significantly reduced the fungal burden and displayed an improved survival rate. In conclusion, the 2C thiosemicarbazone derivative possesses a potent antifungal activity that became more advantageous upon its encapsulation in the fibrin liposome delivery system.

scholarly journals Phenotypic aspects of oral strains of Candida albicans in children with down's syndrome

2006 ◽  
Vol 66 (3) ◽  
pp. 939-944 ◽  
Author(s):  
E. L. Ribeiro ◽  
M. L. Scroferneker ◽  
M. S. Cavalhaes ◽  
C. C. Campos ◽  
G. M. Nagato ◽  
...  
Keyword(s):  
Inhibitory Concentration ◽  
Down's Syndrome ◽  
Test Group ◽  
Down’S Syndrome ◽  
Antifungal Drugs ◽  
Control Group ◽  
Broth Microdilution ◽  
In Vitro Susceptibility ◽  
Biological Aspects

The aim of this article is to characterize the biological aspects of oral strains of C. albicans in children with Down's syndrome. These yeasts were analyzed as to their macromorphological and enzymatic aspects and were tested as to their in vitro susceptibility to antifungal drugs using broth microdilution to determine the minimum inhibitory concentration (MIC). The morphotyping revealed that all oral C. albicans isolates from children with Down's syndrome promoted the formation of fringes regardless of size, while the control group presented smaller fringes. All oral C. albicans strains produced proteinase, but those with phospholipolytic activity showed greater enzyme capacity in the test group. In vitro susceptibility showed that all oral C. albicans isolates were sensitive to the drugs used.

scholarly journals Eugenol and Isoeugenol In Association with Antifungal Against Cryptococcus neoformans

2017 ◽  
Vol 9 (4) ◽  
Author(s):  
Pinheiro L. S. ◽  
Sousa J. P. ◽  
Sousa J. P. ◽  
Barreto N. A. ◽  
Dantas T B ◽  
...  
Keyword(s):  
Cryptococcus Neoformans ◽  
Amphotericin B ◽  
Inhibitory Concentration ◽  
Synergistic Effects ◽  
Antagonistic Effect ◽  
Antifungal Drugs ◽  
Antifungal Effect ◽  
Beneficial Effects ◽  
Combined Use ◽  
Antifungal Effects

The antifungal therapy combined is used in clinical practice of several mycoses as it may increase the efficacy of the treatment. The use of natural products (phytochemicals) in combination with conventional antifungal drugs has been related to beneficial effects, mainly synergistic effects. The aim of this study was to evaluate the effect of the combined use of eugenol / isoeugenol, compounds with recognized antimicrobial activity, in association with antifungal amphotericin B against strains of Cryptococcus neoformans. The combined antifungal effect were be determined from the Fraction Inhibitory Concentration index - checkerboard technique. The results obtained in this study showed that eugenol in combination with amphotericin B had antagonistic effect against the strains of C. neoformans, LM 615 and INCQS 40221 (FIC index 6.0 and 4.0), respectively. The combination of the isoeugenol and amphotericin B also showed antagonistic effects for both the LM 615 strain and INCQS 40221 (FIC index 6.0 and 5.0), respectively. This study contributed to the understanding of the antifungal effects of the association of phenylpropanoids (eugenol / isoeugenol) with amphotericin B. Further studies are needed to evaluate and compare the effects of the association of these phytochemicals with other conventional antifungal drugs used against C. neoformans.

Formulation and evaluation of Cassia tora phytosomal gel using central composite design.

2021 ◽  
Vol 14 ◽  
Author(s):  
Leander Corrie ◽  
Raghunandan Gundaram ◽  
Latha Kukatil
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Therapeutic Activity ◽  
In Vitro Drug Release ◽  
Cassia Tora ◽  
Dependent Variables ◽  
Antifungal Effects ◽  
Two Parameters ◽  
Central Composite

Background:: Cassia tora has been classified as an antifungal agent, but no optimized formulation for improved drug penetration has been developed. Objective:: The present work aimed to formulate Cassia tora extract (CTE) phytosomal gel that could be used for its antifungal effects and improved therapeutic activity. Materials and Methods: The CTE phytosomes were formulated by varying the concentration of lecithin (0.15-0.25% w/v) and speed of rotation (100-160 rpm). A 22 factorial design was applied by taking the above two parameters as independent variables and vesicular size and entrapment efficiency as dependent variables. The phytosomes were also evaluated for polydispersity index, zeta potential and in vitro drug release. The optimized phytosomes of CTE were further developed into a gel, the optimized gel was also evaluated and stability studies were conducted. Results and Discussion: The optimized CTE phytosome showed a vesicular size of ~ 124 nm and entrapment efficiency of 95%. The CTE phytosomes showed a drug release of 58.79% in 24 hours following Higuchi's order of release. The CTE phytosomes were formulated into a gel by using 1% Carbopol 934 and were evaluated for pH, viscosity and homogeneity. The formulated gel showed better penetration than conventional gel and stability changes indicated no major changes to the CTE phytosomal gel. Conclusion: The optimized gel had better penetration and drug release than the conventional gel. Its therapeutic activity, therefore can be estimated to be enhanced.

scholarly journals Antifungal effects of alantolactone on Candida albicans: an in vitro study

2021 ◽  
Author(s):  
Xin Liu ◽  
Lili Zhong ◽  
Zhiming Ma ◽  
Yujie Sui ◽  
Jia’nan Xie ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Medical Devices ◽  
Fungal Pathogen ◽  
Biofilm Formation ◽  
In Vitro Study ◽  
Antifungal Drugs ◽  
Promising Candidate ◽  
Human Fungal Pathogen ◽  
Antifungal Effects

AbstractThe human fungal pathogen Candida albicans can cause many kinds of infections, including biofilm infections on medical devices, while the available antifungal drugs are limited to only a few. In this study, alantolactone (Ala) demonstrated antifungal activities against C. albicans, as well as other Candida species, with a MIC of 72 μg/mL. Ala could also inhibit the adhesion, yeast-to-hyphal transition, biofilm formation and development of C. albicans. The exopolysaccharide of biofilm matrix and extracellular phospholipase production could also be reduced by Ala treatment. Ala could increase permeability of C. albicans cell membrane and ROS contribute to the antifungal activity of Ala. Overall, the present study suggests that Ala may provide a promising candidate for developing antifungal drugs against C. albicans infections.

scholarly journals In Vitro Activities of Retigeric Acid B Alone and in Combination with Azole Antifungal Agents against Candida albicans

2009 ◽  
Vol 53 (4) ◽  
pp. 1586-1591 ◽  
Author(s):  
Lingmei Sun ◽  
Shujuan Sun ◽  
Aixia Cheng ◽  
Xiuzhen Wu ◽  
Yu Zhang ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Inhibitory Concentration ◽  
Colorimetric Assay ◽  
Fungal Growth ◽  
Synergistic Interactions ◽  
Pentacyclic Triterpenoid ◽  
Antifungal Effects ◽  
Resistant Strains ◽  
The Difference

ABSTRACT The vitro antifungal activity of retigeric acid B (RAB), a pentacyclic triterpenoid from the lichen species Lobaria kurokawae, was evaluated alone and in combination with fluconazole, ketoconazole, and itraconazole against Candida albicans using checkerboard microdilution and time-killing tests. The MICs for RAB against 10 different C. albicans isolates ranged from 8 to 16 μg/ml. A synergistic action of RAB and azole was observed in azole-resistant strains, whereas synergistic or indifferent effects were observed in azole-sensitive strains when interpreted by a separate approach of the fractional inhibitory concentration index and ΔE model (the difference between the predicted and measured fungal growth percentages). In time-killing tests, we used both colony counts and a colorimetric assay to evaluate the combinational antifungal effects of RAB and azoles, which further confirmed their synergistic interactions. These findings suggest that the natural product RAB may play a certain role in increasing the susceptibilities of azole-resistant C. albicans strains.

Nanosuspension as an Efficient Carrier for Improved Ocular Permeation of Voriconazole

2020 ◽  
Vol 21 ◽  
Author(s):  
Tang Qin ◽  
Zhu Dai ◽  
Xiaodi Xu ◽  
Zilin Zhang ◽  
Xiangyu You ◽  
...  
Keyword(s):  
Physical Stability ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Antifungal Drugs ◽  
In Vivo Experiments ◽  
Transmission Electron ◽  
Solvent Evaporation Process ◽  
High Entrapment Efficiency

Background: The present limitations related to the ocular administration of antifungal drugs for the treatment of fungal keratitis include poor ocular bioavailability, limited retention time, and low ocular tissues penetration. Methods: This study aimed to prepare a novel ophthalmic voriconazole-loaded nanosuspension based on Eudragit RS 100. Pharmasolve® was explored as a corneal permeation enhancer in voriconazole ophthalmic formulation using in vitro and in vivo experiments. Briefly, 1% voriconazole-loaded nanosuspension was prepared using the quasi-emulsion solvent evaporation process. Results: Characterizations of the voriconazole-loaded nanosuspension by Zetasizer Nano ZS and transmission electron microscope (TEM) showed a uniform spherical shape without any agglomeration. The well-discreted nanoparticle with size of 138 ± 1.3 nm was achieved with high entrapment efficiency (98.6 ± 2.5 %) and a positive zeta potential in the range of 22.5 - 31.2 mV, indicating excellent physical stability. Discussion: Voriconazole-loaded nanosuspension containing the penetration enhancer displayed good permeability both in vitro and in vivocompared with the commercial voriconazole injection. The voriconazole-loaded nanosuspension exhibited good antifungal activity, significantly inhibiting the growth of Candida albicans at a lower concentrations of voriconazole (2.5 μg/mL, p < 0.05). Conclusion: In conclusion, the voriconazole-loaded nanosuspension containing Pharmasolve® can be used as an effective ophthalmic formu-lation for the topical ocular delivery of voriconazole.

scholarly journals IN VITRO ANTIMYCOTIC EVALUATION AND PRELIMINARY COMBINATORIAL STUDIES OF IBUPROFEN WITH STANDARD ANTIFUNGAL DRUGS AGAINST ASPERGILLUS SPP.

2017 ◽  
Vol 10 (8) ◽  
pp. 113
Author(s):  
Mrridula Dangi Narwal ◽  
Meenakshi Balhara ◽  
Renu Chaudhary ◽  
Anil Kumar Chhillar
Keyword(s):  
Spore Germination ◽  
Inhibitory Concentration ◽  
Antifungal Drugs ◽  
Germination Inhibition ◽  
Zone Of Inhibition ◽  
Dilution Assay ◽  
Invasive Mycoses ◽  
Diffusion Assay ◽  
Microbroth Dilution

Objective: The prevalence of invasive mycoses is increased in the immunocompromised patients with an increase in resistance developed againstcurrent antifungal drugs. This has led to the need for discovering novel combinations of the antifungal drugs to combat against resistant pathogenic spp.This study mainly targets to evaluate the antifungal activity of ibuprofen (IBU) alone and in combination with the standard antifungal drugs (polyenesand azoles) against eight isolates of Aspergillus fumigatus, Aspergillus flavus, and Aspergillus niger.Methods: The study was performed using the disc diffusion assay (DDA), microbroth dilution assay and spore germination inhibition assay. Moreover,cytotoxicity was checked by heamolytic assay.Results: Minimum inhibitory concentration (MIC) of IBU against A. fumigatus and A. flavus using DDA is found to be in the range of 250-275 μg/disc while for A. niger isolates, the range was 500-575 μg/disc. Likewise, by broth microdilution assay and spore germination inhibitory assay, MICdetermined, were in the range of 500-750 μg/ml against A. fumigatus and A. flavus while for A. niger, it was 1000-1500 μg/ml.Conclusion: IBU demonstrated its antimycotic potential against all the eight isolates of Aspergillus spp. Moreover, preliminary combinatorialevaluation of IBU with the standard antifungal drugs reported by DDA revealed an increase in zone of inhibition as compared to the drugs alone.Further research regarding the confirmation of synergistic interaction between the selected drugs is in progress.

scholarly journals Antimicrobial Activity of the Dichloromethane Extract from in vitro Cultured Roots of Morinda royoc and Its Main Constituents

2010 ◽  
Vol 5 (5) ◽  
pp. 1934578X1000500
Author(s):  
Janetsy Borroto ◽  
Ricardo Salazar ◽  
Alejandro Pérez ◽  
Yemeys Quiros ◽  
Martha Hernandez ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Bacterial Strains ◽  
Yeast Strains ◽  
Mic Value

The dichloromethane extract and seven anthraquinones isolated from in vitro cultured roots of Morinda royoc L. were tested for their antimicrobial activity against seven yeast and seven bacterial strains. The extract showed a minimum inhibitory concentration (MIC) value of 15.6 μg/m against all species of Candida tested; except C. glabrata (MIC 1.95 μg/mL), and it inhibited the growth of oxacillin-resistant Staphylococcus aureus (MIC 31.2 μg/mL). Only morindone showed activity against all yeast strains (MIC 1.9 μg/mL), and against oxacillin-resistant Staphylococcus aureus (MIC 15 μg/mL).

scholarly journals Antifungal Effects of Saponin Extract from Rhizomes of Dioscorea panthaica Prain et Burk against Candida albicans

2018 ◽  
Vol 2018 ◽  
pp. 1-13 ◽  
Author(s):  
Longfei Yang ◽  
Xin Liu ◽  
Xinming Zhuang ◽  
Xuechao Feng ◽  
Lili Zhong ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Fungal Pathogen ◽  
Biofilm Formation ◽  
Inhibitory Concentration ◽  
Antifungal Drugs ◽  
Ros Production ◽  
Oxygen Species ◽  
Planktonic Cells ◽  
Endogenous Reactive Oxygen Species ◽  
Antifungal Effects

Candida albicans is the most common fungal pathogen causing serious diseases, while there are only a paucity of antifungal drugs. Therefore, the present study was performed to investigate the antifungal effects of saponin extract from rhizomes of Dioscorea panthaica Prain et Burk (Huangshanyao Saponin extract, HSE) against C. albicans. HSE inhibits the planktonic growth and biofilm formation and development of C. albicans. 16–64 μg/mL of HSE could inhibit adhesion to polystyrene surfaces, transition from yeast to filamentous growth, and production of secreted phospholipase and could also induce endogenous reactive oxygen species (ROS) production and disrupt cell membrane in planktonic cells. Inhibitory activities against extracellular exopolysaccharide (EPS) production and ROS production in preformed biofilms could be inhibited by 64–256 μg/mL of HSE. Cytotoxicity against human Chang’s liver cells is low, with a half maximal inhibitory concentration (IC50) of about 256 μg/mL. In sum, our study suggested that HSE might be used as a potential antifungal therapeutic against C. albicans.

scholarly journals ANTIFUNGAL ACTIVITY OF THE ASSOCIATION OF CARVACROL WITH AMPHOTERICIN B OR WITH KETOCONAZOLE

2019 ◽  
Vol 16 (31) ◽  
pp. 12-17
Author(s):  
Gustavo Lima SOARES ◽  
Brenda Lavínia Calixto dos SANTOS ◽  
Brenna Ravena Araújo LUZ ◽  
Wylly Araújo de OLIVEIRA
Keyword(s):  
Antifungal Activity ◽  
Amphotericin B ◽  
Inhibitory Concentration ◽  
Fungal Infections ◽  
Antifungal Drugs ◽  
Aspergillus Species ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Antifungal Action

Aspergillus species are a cause of a high number of fungal infections of difficult treatment, presenting an expressive number of deaths due to the complications in the severe cases of infection. The objective was to evaluate the antifungal action of carvacrol against Aspergillus species, as well as to evaluate the interactions when associated with amphotericin B or ketoconazole. The antifungal activity of carvacrol was evaluated by the broth microdilution method. The combinations of the substances were performed by the checkerboard methodology, to determine the Index of Fractional Inhibitory Concentration. Carvacrol showed antifungal activity against all Aspergillus strains used in the trials. In combinations of substances, only a combination of carvacrol and amphotericin B presented satisfactory results. Combinations of carvacrol and ketoconazole have not shown good. It is concluded that carvacrol is a good candidate for the antifungal drug because of its good activity against Aspergillus demonstrated in the present study, as well as in other studies in the literature. Their combination in vitro with amphotericin B or ketoconazole did not present any advantages over the use of antifungal drugs alone.

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