Synthesis and in vitro antifungal efficacy of Cu–chitosan nanoparticles against pathogenic fungi of tomato

The use of nanotechnology could play a significant role in the agriculture sector, especially in the preparation of new-generation agronanochemicals. Currently, the economically important plant of Malaysia, the oil palm, faces the threat of a devastating disease which is particularly caused by a pathogenic fungus, Ganoderma boninense. For the development of an effective antifungal agent, a series of chitosan nanoparticles loaded with a fumigant, dazomet, were prepared using various concentrations of sodium tripolyphosphate (TPP)—2.5, 5, 10, and 20 mg/mL, abbreviated as CDEN2.5, CDEN5, CDEN10, and CDEN20, respectively. The effect of TPP as a crosslinking agent on the resulting particle size of the synthesized nanoparticles was investigated using a particle size analyzer and high-resolution transmission electron microscopy (HRTEM). Both methods confirmed that increasing the TPP concentration resulted in smaller particles. In addition, in vitro fumigant release at pH 5.5 showed that the release of the fumigant from the nanoparticles was of a sustained manner, with a prolonged release time up to 24 h. Furthermore, the relationship between the chitosan-dazomet nanoparticles and the in vitro antifungal activity against G. boninense was also explored, where the nanoparticles of the smallest size, CDEN20, gave the highest antifungal efficacy with the lowest half maximum effective concentration (EC50) value of 13.7 ± 1.76 ppb. This indicates that the smaller-sized agronanoparticles were more effective as an antifungal agent. The size can be altered, which plays a crucial role in combatting the Ganoderma disease. The agronanoparticles have controlled release properties and high antifungal efficacy on G. boninense, thus making them a promising candidate to be applied in the field for Ganoderma treatment.

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In vitro antifungal efficacy of copper nanoparticles against selected crop pathogenic fungi

Materials Letters ◽

10.1016/j.matlet.2013.10.011 ◽

2014 ◽

Vol 115 ◽

pp. 13-17 ◽

Cited By ~ 163

Author(s):

Prachi Kanhed ◽

Sonal Birla ◽

Swapnil Gaikwad ◽

Aniket Gade ◽

Amedea B. Seabra ◽

...

Keyword(s):

Copper Nanoparticles ◽

Pathogenic Fungi ◽

Antifungal Efficacy

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Biological preparation of chitosan nanoparticles and its in vitro antifungal efficacy against some phytopathogenic fungi

Carbohydrate Polymers ◽

10.1016/j.carbpol.2016.05.033 ◽

2016 ◽

Vol 151 ◽

pp. 321-325 ◽

Cited By ~ 72

Author(s):

M. Sathiyabama ◽

R. Parthasarathy

Keyword(s):

Chitosan Nanoparticles ◽

Phytopathogenic Fungi ◽

Biological Preparation ◽

Antifungal Efficacy

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In Vitro and In Vivo Assessment of FK506 Analogs as Novel Antifungal Drug Candidates

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.01627-18 ◽

2018 ◽

Vol 62 (11) ◽

Cited By ~ 14

Author(s):

Yeonseon Lee ◽

Kyung-Tae Lee ◽

Soo Jung Lee ◽

Ji Yoon Beom ◽

Areum Hwangbo ◽

...

Keyword(s):

Antifungal Activity ◽

Pathogenic Fungi ◽

Antifungal Drugs ◽

Antifungal Drug ◽

Immunosuppressive Activity ◽

Activated T Cells ◽

Content Type ◽

Antifungal Efficacy

ABSTRACT FK506 (tacrolimus) is an FDA-approved immunosuppressant indicated for the prevention of allograft rejections in patients undergoing organ transplants. In mammals, FK506 inhibits the calcineurin-nuclear factor of activated T cells (NFAT) pathway to prevent T-cell proliferation by forming a ternary complex with its binding protein, FKBP12, and calcineurin. FK506 also exerts antifungal activity by inhibiting calcineurin, which is essential for the virulence of human-pathogenic fungi. Nevertheless, FK506 cannot be used directly as an antifungal drug due to its immunosuppressive action. In this study, we analyzed the cytotoxicity, immunosuppressive activity, and antifungal activity of four FK506 analogs, 31-O-demethyl-FK506, 9-deoxo-FK506, 9-deoxo-31-O-demethyl-FK506, and 9-deoxo-prolyl-FK506, in comparison with that of FK506. The four FK506 analogs generally possessed lower cytotoxicity and immunosuppressive activity than FK506. The FK506 analogs, except for 9-deoxo-prolyl-FK506, had strong antifungal activity against Cryptococcus neoformans and Candida albicans, which are two major invasive pathogenic yeasts, due to the inhibition of the calcineurin pathway. Furthermore, the FK506 analogs, except for 9-deoxo-prolyl-FK506, had strong antifungal activity against the invasive filamentous fungus Aspergillus fumigatus. Notably, 9-deoxo-31-O-demethyl-FK506 and 31-O-demethyl-FK506 exhibited robust synergistic antifungal activity with fluconazole, similar to FK506. Considering the antifungal efficacy, cytotoxicity, immunosuppressive activity, and synergistic effect with commercial antifungal drugs, we selected 9-deoxo-31-O-demethyl-FK506 for further evaluation of its in vivo antifungal efficacy in a murine model of systemic cryptococcosis. Although 9-deoxo-31-O-demethyl-FK506 alone was not sufficient to treat the cryptococcal infection, when it was used in combination with fluconazole, it significantly extended the survival of C. neoformans-infected mice, confirming the synergistic in vivo antifungal efficacy between these two agents.

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Investigation of in vitro antifungal efficacy of selected extracts of Greek natural products on Malassezia sps

Planta Medica ◽

10.1055/s-0036-1596899 ◽

2016 ◽

Vol 81 (S 01) ◽

pp. S1-S381

Author(s):

A Velegraki ◽

K Graikou ◽

S Kritikou ◽

M Varsani ◽

I Chinou

Keyword(s):

Natural Products ◽

Antifungal Efficacy

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Formulation of Modified Release Atorvastatin Nanoparticles by Emulsion Interfacial Reaction Method

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.3.7 ◽

2015 ◽

Vol 8 (3) ◽

pp. 2937-2940

Author(s):

Sudhakar Sekar ◽

Shee Sim May

Keyword(s):

Interfacial Reaction ◽

Therapeutic Potential ◽

Chitosan Nanoparticles ◽

In Vitro Release ◽

Morphological Characteristics ◽

Preparation Technique ◽

Modified Release ◽

Reaction Method ◽

Vitro Release

The aim of the study is to formulate a modified release chitosan nanoparticles for the oral delivery of atorvastatin and to study the in vitro release of atorvastatin from chitosan nanoparticles. Atorvastatin-loaded chitosan nanoparticles were prepared with different concentration of cross-linking agent (glutaraldehyde) by emulsion interfacial reaction method. The formed nanoparticles were characterized in terms of size and morphological characteristics by scanning electron microscopy (SEM) and transmission electron microscope (TEM). Spherical and regular nanoparticles with the size range of 100-250nm were formed. Atorvastatin encapsulation efficiency of nanoparticles was found to be highest in ANP3, followed by ANP2 and ANP1. The in vitro release of atorvastatin was studied by membrane diffusion technique. The resulted cumulative percentage of drug released for ANP1, ANP2 and ANP3 were 60.08%, 34.81% and 20.39% respectively. Through this study, the nanoparticles preparation technique has shown to be a promising approach for enhancing the dissolution of hydrophobic drugs like atorvastatin calcium. The application of this novel delivery system offers good therapeutic potential in the management of hypercholesterolemia and dyslipidemia.

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Improved Production of Two Anti-Candida Lipopeptide Homologues Co- Produced by the Wild-Type Bacillus subtilis RLID 12.1 under Optimized Conditions

Current Pharmaceutical Biotechnology ◽

10.2174/1389201020666191205115008 ◽

2020 ◽

Vol 21 (5) ◽

pp. 438-450

Author(s):

Ramya Ramchandran ◽

Swetha Ramesh ◽

Anviksha A ◽

RamLal Thakur ◽

Arunaloke Chakrabarti ◽

...

Keyword(s):

Bacillus Subtilis ◽

Pathogenic Fungi ◽

Fold Increase ◽

Production Yield ◽

Yield Enhancement ◽

Bioactive Metabolites ◽

Candida Auris ◽

Media Formulation ◽

Static Conditions

Background:: Antifungal cyclic lipopeptides, bioactive metabolites produced by many species of the genus Bacillus, are promising alternatives to synthetic fungicides and antibiotics for the biocontrol of human pathogenic fungi. In a previous study, the co- production of five antifungal lipopeptides homologues (designated as AF1, AF2, AF3, AF4 and AF5) by the producer strain Bacillus subtilis RLID 12.1 using unoptimized medium was reported; though the two homologues AF3 and AF5 differed by 14 Da and in fatty acid chain length were found effective in antifungal action, the production/ yield rate of these two lipopeptides determined by High-Performance Liquid Chromatography was less in the unoptimized media. Methods:: In this study, the production/yield enhancement of the two compounds AF3 and AF5 was specifically targeted. Following the statistical optimization (Plackett-Burman and Box-Behnken designs) of media formulation, temperature and growth conditions, the production of AF3 and AF5 was improved by about 25.8- and 7.4-folds, respectively under static conditions. Results:: To boost the production of these two homologous lipopeptides in the optimized media, heat-inactivated Candida albicans cells were used as a supplement resulting in 34- and 14-fold increase of AF3 and AF5, respectively. Four clinical Candida auris isolates had AF3 and AF5 MICs (100 % inhibition) ranging between 4 and 16 μg/ml indicating the lipopeptide’s clinical potential. To determine the in vitro pharmacodynamic potential of AF3 and AF5, time-kill assays were conducted which showed that AF3 (at 4X and 8X concentrations) at 48h exhibited mean log reductions of 2.31 and 3.14 CFU/ml of C. albicans SC 5314, respectively whereas AF5 at 8X concentration showed a mean log reduction of 2.14 CFU/ml. Conclusion:: With the increasing threat of multidrug-resistant yeasts and fungi, these antifungal lipopeptides produced by optimized method promise to aid in the development of novel antifungal that targets disease-causing fungi with improved efficacy.

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Quality-by-Design Enabled Chitosan Nanoparticles for Antitubercular Therapy: Formulation, Statistical Optimization, and In vitro Characterization

Current Drug Therapy ◽

10.2174/1574885515666200722150305 ◽

2020 ◽

Vol 15 ◽

Author(s):

Manasi M. Chogale ◽

Sujay S. Gaikwad ◽

Savita P. Kulkarni ◽

Vandana B. Patravale

Keyword(s):

Side Effects ◽

Treatment Regimen ◽

Research Work ◽

Chitosan Nanoparticles ◽

In Vitro Release ◽

Antitubercular Therapy ◽

Prolonged Treatment ◽

High Dose ◽

Average Size

Background: Tuberculosis (TB) continues to be among the leading causes for high mortality among developing countries. Though a seemingly effective treatment regimen against TB is in place, there has been no significant improvement in the therapeutic rates. This is primarily owing to the high drug doses, their associated sideeffects, and prolonged treatment regimen. Discontinuation of therapy due to the severe side effects of the drugs results in the progression of the infection to the more severe drug-resistant TB. Objectives: Reformulation of the current existing anti TB drugs into more efficient dosage forms could be an ideal way out. Nanoformulations have been known to mitigate the side effects of toxic, high-dose drugs. Hence, the current research work involves the formulation of Isoniazid (INH; a first-line anti TB molecule) loaded chitosan nanoparticles for pulmonary administration. Methods: INH loaded chitosan nanoparticles were prepared by ionic gelation method using an anionic crosslinker. Drugexcipient compatibility was evaluated using DSC and FT-IR. The formulation was optimized on the principles of Qualityby-Design using a full factorial design. Results: The obtained nanoparticles were spherical in shape having an average size of 620±10.97 nm and zeta potential +16.87±0.79 mV. Solid state characterization revealed partial encapsulation and amorphization of INH into the nanoparticulate system. In vitro release study confirmed an extended release of INH from the system. In vitro cell line based safety and efficacy studies revealed satisfactory results. Conclusion: The developed nanosystem is thus an efficient approach for antitubercular therapy.

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