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    Development and characterization of polymeric-based nanoparticles for sustained release of amoxicillin - an antimicrobial drug
    (Taylor & Francis Ltd, 2018) Guncum, Enes; Isiklan, Nuran; Anlas, Ceren; Unal, Nilgun; Bulut, Elif; Bakirel, Tulay
    In this study, amoxicillin (AMO)-loaded poly(vinyl alcohol)/sodium alginate (PVA/NaAlg) nanoparticles were prepared as a polymer-based controlled release system. The physicochemical properties of the obtained nanoparticles were investigated by XRD, DSC/TGA, particle size analyses and zeta potential measurements. The average particle sizes were in the range from 336.3 +/- 25.66 to 558.3 +/- 31.39 nm with negative zeta potential values from -41.86 +/- 0.55 to-47.3 +/- 2.76 mV. The influences of PVA/NaAlg ratio, span 80 concentration, exposure time to glutaraldehyde (GA) and the drug/polymer ratio on AMO release profiles were evaluated. In vitro drug release studies showed a controlled and pH dependent AMO release with an initial burst effect. XRD patterns and DSC thermograms of AMO-loaded nanoparticles revealed that the drug in the nanoparticles was in amorphous form, which was more stable than the crystalline form. The antibacterial activity of the optimal formulation was also investigated. The minimum inhibitory concentration (MIC) values of this formulation had the comparable antibacterial activity with that of pure AMO. These results indicate that the developed nanoparticles could be a promising candidate drug delivery system for AMO.
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    Effects of feed intake and water hardness on fluralaner pharmacokinetics in layer chickens
    (Korean Soc Veterinary Science, 2022) Sari, Ataman Bilge; Gunes, Yigit; Anlas, Ceren; Alkan, Fulya Ustun; Guncum, Enes; Ustuner, Oya; Bakirel, Tulay
    Background: Fluralaner is a novel drug belonging to the isoxazoline class that acts on external parasites of domestic animals. It is used systemically via drinking water, especially against red poultry mite in layer chickens. Fluralaner is frequently used in layers infected with D. gallinae. However, no study to date has investigated the effects of feed intake and water hardness. Objectives: This study aimed to investigate the effects of variable water hardness and feed intake on the pharmacokinetic profile of fluralaner. Methods: Layer chickens were divided into four groups (n = 8): fed + purified water (Group 1), feed restricted + purified water (Group 2), feed restricted + hard water (Group 3), and feed restricted + soft water (Group 4). After administering a single dose of the drug with drinking water, the blood samples were collected for 21 days. Fluralaner concentrations in plasma samples were determined by liquid chromatography/tandem mass spectrometry. The maximum plasma concentration ( Cmax), time to reach maximum plasma concentration ( tmax), area under the concentration-time curve values (AUC(0-21d)), half-life ( t(1/2)), and other pharmacokinetic parameters were calculated. Results: Although the highest maximum plasma concentration ( C-max) was determined in Group 1 (fed + purified water), no statistically significant difference was found in the C-max, tmax, t(1/2), MRT0- inf_obs, Vz/ F-obs, and Cl/ F-_ obs parameters between the experimental groups. Conclusions: It was concluded that the feed intake or water hardness did not change the pharmacokinetic profile of fluralaner in layer chickens. Therefore, fluralaner could be used before or after feeding with the varying water hardness in poultry industry.
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    Öğe
    Preparation, characterization, and evaluation of antibacterial and cytotoxic activity of chitosan-polyethylene glycol nanoparticles loaded with amoxicillin as a novel drug delivery system
    (Taylor & Francis Ltd, 2023) Guncum, Enes; Isiklan, Nuran; Anlas, Ceren; Bulut, Elif; Bakirel, Tulay
    In this study, nanoparticles of amoxicillin (AMX) were prepared using chitosan (CHI) and polyethylene glycol (PEG). The physicochemical properties of the particles were investigated by FT-IR, DSC, SEM, and zeta potential analyses. The nanoparticles showed a spherical shape, and the average size of formulations was within the range of 696.20 +/- 24.86 - 359.53 +/- 7.41 nm. Zeta potential data demonstrated that the formulations had positive surface charges with a zeta potential range of 21.38 +/- 2.28 - 7.73 +/- 1.66 mV. FTIR analysis showed that the drug was successfully entrapped in the nanoparticles. DSC results suggested that the drug was present in amorphous form in the polymer matrix. In vitro release studies demonstrated that the release pattern consisted of two phases, with an initial burst release followed by a controlled and sustained release. The MTT assay results on mouse fibroblast cell line indicated that the prepared formulations did not affect the viability of the cells. In the in vitro antibacterial activity test, it was found that the drug-loaded nanoparticles have AMX-equivalent antibacterial activity against E. coli, and S. aureus. These findings revealed that the obtained nanoparticles might be a promising and safe nanocarrier system for efficient delivery of AMX.
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    Öğe
    The screening of the safety profile of polymeric based amoxicillin nanoparticles in various test systems
    (Elsevier Ireland Ltd, 2021) Guncum, Enes; Bakirel, Tulay; Anlas, Ceren; Isiklan, Nuran; Alkan, Fulya Ustun; Charehsaz, Mohammad; Aydin, Ahmet
    Nanotechnology-based drugs show superiority over conventional medicines because of increased bioavailability, lower accumulation in non-target tissues, and improved therapeutic index with increased accumulation at target sites. However, it is important to be aware of possible problems related to the toxicity of these products, which have therapeutically superior properties. Accordingly, the present study was designed to investigate the safety profile of amoxicillin nanoparticles (AmxNPs) that we developed to increase the oral bioavailability of amoxicillin (Amx) in poultry. In the first part of the study, the genotoxicity potential of AmxNPs was evaluated using the Ames test and the in vitro comet assay. The results of Ames test showed that none of the tested concentrations of Amx and AmxNPs cause a significant increase in the revertant number of Salmonella typhimurium strains TA98, and TA100, either with or without metabolic activation. Similarly, the comet assay revealed that AmxNPs did not induce DNA damage at any of the concentrations used, whereas high-dose (200 mu g/mL) of Amx caused a significant increase in the percentage of DNA in the tail. In the second part of the study, the toxicity potential of AmxNPs on broilers was investigated by measuring biochemical parameters. In vivo results demonstrated that AmxNps did not cause a significant change in biochemical parameters, whereas Amx increased ALT, glucose, and cholesterol levels at certain sampling times. The obtained findings suggest that AmxNPs could be a safe promising potential drug in drug delivery systems. (C) 2021 Elsevier B.V. All rights reserved.