Synthesis, characterization, and in vitro activity against &lt;em&gt;Candida&lt;/em&gt; spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)

Gómez-Sequeda, Nicolás; Torres, Rodrigo; Ortíz, Claudia

doi:10.2147/nsa.s96018

Cited by 20 publications

(9 citation statements)

References 69 publications

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“…By encapsulating both peptides in PLGA nanoparticles, the antibacterial activity was increased several times. These results were similar to those reported for the encapsulation of other antibiotics to protect them, increasing their antibacterial activity and decreasing their cytotoxicity [28,32].…”

Section: Determination Of Minimum Inhibitory Concentration (Mic) and supporting

confidence: 89%

“…It is possible that a fraction of the total peptide was embedded on the nanoparticle surface, being rapidly dissociated, while the residual peptide remains inside of the nanoparticle and it is slowly released once PLGA is hydrolyzed. This releasing profile was very similar to that obtained by other authors using different active principles encapsulated [18,32,35].…”

Section: In Vitro Release Of Antimicrobial Peptides From Plga-npsupporting

confidence: 89%

“…It has been proved that the cationic nanoparticles efficiently interact with the anionic lipids of bacterial membranes [18,30]. In this work, it was possible to obtain cationic nanoparticles (with zeta potential for G17NP = 7.26 mV and G19NP = 12.87 mV) without using cationic polymers such as polyethylenimine or chitosan for their coating, since these polymers have shown cytotoxic activity against eukaryotic cells [31,32].…”

Section: Physicochemical Properties Of Amp-npsmentioning

confidence: 97%

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Potent and Specific Antibacterial Activity against Escherichia coli O157:H7 and Methicillin Resistant Staphylococcus aureus (MRSA) of G17 and G19 Peptides Encapsulated into Poly-Lactic-Co-Glycolic Acid (PLGA) Nanoparticles

et al. 2020

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Antimicrobial peptides constitute an excellent alternative against conventional antibiotics because of their potent antimicrobial spectrum, unspecific action mechanism and low capacity to produce antibiotic resistance. However, a potential use of these biological molecules as therapeutic agents is threatened by their low stability and susceptibility to proteases. In order to overcome these limitations, encapsulation in biocompatible polymers as poly-lactic-glycolic-acid (PLGA) is a promising alternative for increasing their stability and bioavailability. In this work, the effect of new synthetic antimicrobial peptides GIBIM-P5S9K (G17) and GAM019 (G19) encapsulated on PLGA and acting against methicillin resistant Staphylococus aureus (MRSA) and Escherichia coli O157:H7 was studied. PLGA encapsulation allowed us to load around 7 µg AMPs/mg PLGA with an efficiency of 90.5%, capsule sizes around 290 nm and positive charges. Encapsulation improved antimicrobial activity, decreasing MIC50 from 1.5 to 0.2 (G17NP) and 0.7 (G19NP) µM against MRSA, and from 12.5 to 3.13 µM for E. coli O157:H7. Peptide loaded nanoparticles could be a bacteriostatic drug with potential application to treat these bacterial E. coli O157:H7 and MRSA infections, with a slow and gradual release.

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Section: Determination Of Minimum Inhibitory Concentration (Mic) and supporting

confidence: 89%

Section: In Vitro Release Of Antimicrobial Peptides From Plga-npsupporting

confidence: 89%

Section: Physicochemical Properties Of Amp-npsmentioning

confidence: 97%

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Potent and Specific Antibacterial Activity against Escherichia coli O157:H7 and Methicillin Resistant Staphylococcus aureus (MRSA) of G17 and G19 Peptides Encapsulated into Poly-Lactic-Co-Glycolic Acid (PLGA) Nanoparticles

et al. 2020

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“…The results showed that the use of nanoparticles was able to produce a total visual growth inhibition at lower concentrations than fluconazole, for both reference and clinical isolates ( Table 2 and Table 3 ). In fact, we must consider that the drug incorporated within SLN has advantages when compared to their unincorporated counterparts, such as a greater penetration into fungal cells, favored by the small size presented by the delivery system [ 50 , 53 ]. The same reason may justify the fact that 10-SLN-PHY has a MIC of 50% inhibition activity approximately 300 times lower when compared to the PHY in the assays containing Candida spp.…”

Section: Resultsmentioning

confidence: 99%

“…In addition to the cicatrizing activity cited below, the in vivo toxicity of this compound was also evaluated [ 57 ], and to date there are no reports of antifungal activity. Thus, we believe that through a synergistic activity between PHY and TG1 we are able to induce antifungal activity for the compound of natural origin [ 53 ].…”

Section: Resultsmentioning

confidence: 99%

Phytol-Loaded Solid Lipid Nanoparticles as a Novel Anticandidal Nanobiotechnological Approach

et al. 2020

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Phytol is a diterpene alcohol and can be found as a product of the metabolism of chlorophyll in plants. This compound has been explored as a potential antimicrobial agent, but it is insoluble in water. In this study, we describe a novel approach for an interesting anticandidal drug delivery system containing phytol. Different formulations of phytol-loaded solid lipid nanoparticles (SLN) were designed and tested using a natural lipid, 1,3-distearyl-2-oleyl-glycerol (TG1). Different compositions were considered to obtain three formulations with 1:10, 1:5, and 1:3 w/w phytol/TG1 ratios. All the formulations were prepared by emulsification solvent evaporation method and had their physicochemical properties assessed. The biocompatibility assay was performed in the HEK-293 cell line and the antifungal efficacy was demonstrated in different strains of Candida ssp., including different clinical isolates. Spherical and uniform SLN (<300 nm, PdI < 0.2) with phytol-loading efficiency >65% were achieved. Phytol-loaded SLN showed a dose-dependent cytotoxic effect in the HEK-293 cell line. The three tested formulations of phytol-loaded SLN considerably enhanced the minimal inhibitory concentration of phytol against 15 strains of Candida spp. Considering the clinical isolates, the formulations containing the highest phytol/TG1 ratios showed MICs at 100%. Thus, the feasibility and potential of phytol-loaded SLN was demonstrated in vitro, being a promising nanocarrier for phytol delivery from an anticandidal approach.

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Potent antifungal agents and use of nanocarriers to improve delivery to the infected site: A systematic review

2021

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There are four major classes of antifungals with the predominant mechanism of action being targeting of cell wall or cell membrane. As in other drugs, low solubility of these compounds has led to low bioavailability in target tissues. Enhanced drug dosages have effects such as toxicity, drug–drug interactions, and increased drug resistance by fungi. This article reviews the current state‐of‐the‐art of antifungals, structure, mechanism of action, other usages, and toxic side effects. The emergence of nanoformulations to transport and uniformly release cargo at the target site is a boon in antifungal treatment. The article details research that lead to the development of nanoformulations of antifungals and potential advantages and avoidance of the lacunae characterizing conventional drugs. A range of nanoformulations based on liposomes, polymers are in various stages of research and their potential advantages have been brought out. It could be observed that under similar dosages, test models, and duration, nanoformulations provided enhanced activity, reduced toxicity, higher uptake and higher immunostimulatory effects. In most instances, the mechanism of antifungal activity of nanoformulations was similar to that of regular antifungal. There are possibilities of coupling multiple antifungals on the same nano‐platform. Increased activity coupled with multiple mechanisms of action presents for nanoformulations a tremendous opportunity to overcome antifungal resistance. In the years to come, robust methods for the preparation of nanoformulations taking into account the repeatability and reproducibility in action, furthering the studies on nanoformulation toxicity and studies of human models are required before extensive use of nanoformulations as a prescribed drug.

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Synthesis, characterization, and in vitro activity against <em>Candida</em> spp. of fluconazole encapsulated on cationic and conventional nanoparticles of poly(lactic-co-glycolic acid)

Cited by 20 publications

References 69 publications

Potent and Specific Antibacterial Activity against Escherichia coli O157:H7 and Methicillin Resistant Staphylococcus aureus (MRSA) of G17 and G19 Peptides Encapsulated into Poly-Lactic-Co-Glycolic Acid (PLGA) Nanoparticles

Potent and Specific Antibacterial Activity against Escherichia coli O157:H7 and Methicillin Resistant Staphylococcus aureus (MRSA) of G17 and G19 Peptides Encapsulated into Poly-Lactic-Co-Glycolic Acid (PLGA) Nanoparticles

Phytol-Loaded Solid Lipid Nanoparticles as a Novel Anticandidal Nanobiotechnological Approach

Potent antifungal agents and use of nanocarriers to improve delivery to the infected site: A systematic review

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