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1.
Int J Pharm ; 665: 124702, 2024 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-39270761

RESUMO

The advent of drug-eluting contact lenses (DECLs) has opened up new avenues for the treatment of eye diseases. DECLs is expected to partially overcome the shortcomings of eye drops due to single-dose packaging, accurate dosing, prolonged drug elution behavior, and simplified dosing procedures. Currently, a significant proportion of the DECLs design effort has been directed towards enhancing the compatibility of contact lenses with drugs. The appropriate elution time for the drug remains unclear. Additionally, it is ambiguous for which ophthalmic diseases DECLs offers the greatest therapeutic advantage. To rationally design DECLs in practice, it is necessary to understand the acceptance of DECLs by patients and practitioners and to clarify the indications for DECLs. This review will first focus on the acceptance of DECLs by different patients and practitioners and discuss the factors that influence its acceptance. Secondly, this review presents an overview of the current effectiveness of DECLs treatments in animals and in the clinical phase, with a particular focus on the suitability of DECLs for the treatment of ophthalmic diseases. Overall, patients and practitioners expressed positive attitudes towards DECLs. However, this is related to factors such as DECLs' treatment cycle, safety, and price. In addition, DECLs has good application prospects for ocular wound healing, postoperative management, and treatment of contact lenses-related complications. Furthermore, chronic diseases such as glaucoma that necessitate long-term medication and intraocular diseases that require implants or injections represent additional potential applications for DECLs. It is hoped that this review will facilitate a deeper understanding of DECLs acceptance and indications, thereby supporting the rational design of DECLs. At the same time, this review provides a reference for the design of other drug-device combination products.

2.
Environ Sci Ecotechnol ; 22: 100475, 2024 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-39280591

RESUMO

The increase in bacterial antibiotic resistance poses a significant threat to the effectiveness of antibiotics, and there is growing evidence suggesting that global warming may speed up this process. However, the direct influence of temperature on the development of antibiotic resistance and the underlying mechanisms is not yet fully understood. Here we show that antibiotic resistance exhibits a nonlinear response to elevated temperatures under the combined stress of temperatures and antibiotics. We find that the effectiveness of gatifloxacin against Escherichia coli significantly diminishes at 42 °C, while resistance increases 256-fold at 27 °C. Additionally, the increased transcription levels of genes such as marA, ygfA, and ibpB with rising temperatures, along with gene mutations at different sites, explain the observed variability in resistance patterns. These findings highlight the complexity of antibiotic resistance evolution and the urgent need for comprehensive studies to understand and mitigate the effects of global warming on antibiotic resistance.

3.
Cureus ; 16(7): e64283, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-39131012

RESUMO

Corneal deposits associated with topical medications, particularly fluoroquinolones, are a recognized complication in ophthalmic practice. We present a case of a 66-year-old female with pseudophakic bullous keratopathy who developed corneal crystalline deposits following prolonged use of gatifloxacin and prednisolone eye drops post-penetrating keratoplasty. The patient presented with diminished vision and significant corneal opacity in the affected eye. Anterior segment examination and OCT imaging confirmed deposits extending from the epithelium to the anterior stroma. Management included corneal scrapping and transition to topical tobramycin and propylene glycol eye drops, resulting in the resolution of deposits and improvement in vision. This case underscores the importance of vigilant monitoring and judicious use of topical medications to mitigate adverse effects in high-risk ophthalmic patients undergoing corneal procedures.

4.
Biomed Chromatogr ; 38(8): e5928, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38924173

RESUMO

The literature reveals gaps in the availability of green analytical methods for assessing products containing gatifloxacin (GFX), a fluoroquinolone. Presently, method development is supported by tools such as the National Environmental Methods Index (NEMI) and Eco-Scale Assessment (ESA), which offer objective insights into the environmental friendliness of analytical procedures. The objective of this work was to develop and validate a green method by the NEMI and ESA to quantify GFX in eye drops using HPLC. The method utilized a C8 column (4.6 × 150 mm, 5 µm), with a mobile phase of purified water containing 2% acetic acid and ethanol (70:30, v/v). The injection volume was 10 µL and the flow rate was 0.7 mL/min in isocratic mode at 25°C, with detection performed at 292 nm. The method demonstrated linearity in the range of 2-20 µg/mL, and precision at intra-day (relative standard deviation [RSD] 1.44%), inter-day (RSD 3.45%), and inter-analyst (RSD 2.04%) levels. It was selective regarding the adjuvants of the final product (eye drops) and under forced degradation conditions. The method was accurate (recovery 101.07%) and robust. The retention time for GFX was approximately 3.5 min. The greenness of the method, as evaluated by the NEMI, showed four green quadrants, and by ESA, it achieved a score of 88.


Assuntos
Gatifloxacina , Química Verde , Limite de Detecção , Soluções Oftálmicas , Gatifloxacina/análise , Gatifloxacina/química , Cromatografia Líquida de Alta Pressão/métodos , Reprodutibilidade dos Testes , Química Verde/métodos , Modelos Lineares , Soluções Oftálmicas/química , Soluções Oftálmicas/análise , Fluoroquinolonas/análise , Fluoroquinolonas/química
5.
Curr Drug Deliv ; 2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38425110

RESUMO

OBJECTIVE: To prolong the ocular residence time of gatifloxacin and enhance its efficacy against bacterial keratitis, this study developed a velocity-controlled polyethylene glycol-dithiothreitol- boric acid (PDB) hydrogel loaded with gatifloxacin. MATERIALS AND METHODS: First, the basic properties of the synthesized PDB hydrogel and the gatifloxacin- loaded PDB hydrogel were assessed. Secondly, the in vitro degradation rate of the drugloaded PDB was measured in a simulated body fluid environment with pH 7.4/5.5. The release behavior of the drug-loaded PDB was studied using a dialysis method with PBS solution of pH 7.4/5.5 as the release medium. Finally, a mouse model of bacterial keratitis was established, and tissue morphology was observed using hematoxylin-eosin staining. Additionally, mouse tear fluid was extracted to observe the antibacterial effect of the gatifloxacin-loaded PDB hydrogel. RESULTS: The results showed that the PDB hydrogel had a particle size of 124.9 nm and a zeta potential of -23.3 mV, with good porosity, thermosensitivity, viscosity distribution, rheological properties, and high cell compatibility. The encapsulation of gatifloxacin did not alter the physical properties of the PDB hydrogel and maintained appropriate swelling and stability, with a high drug release rate in acidic conditions. Furthermore, animal experiments demonstrated that the gatifloxacin- loaded PDB hydrogel exhibited superior therapeutic effects compared to gatifloxacin eye drops and displayed strong antibacterial capabilities against bacterial keratitis. CONCLUSION: This study successfully synthesized PDB hydrogel and developed a gatifloxacin drug release system. The hydrogel exhibited good thermosensitivity, pH responsiveness, stability, and excellent biocompatibility, which can enhance drug retention, utilization, and therapeutic effects on the ocular surface.

6.
Carbohydr Polym ; 330: 121818, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38368100

RESUMO

Mono or dual chitosan oligosaccharide lactate (COL)-conjugated pluronic F127 polymers, FCOL1 and FCOL2 were prepared, self-assembled to form micelles, and loaded with gatifloxacin. The Gati@FCOL1/Gati@FCOL2 micelles preparation process was optimized by QbD analysis. Micelles were characterized thoroughly for size, CMC, drug compatibility, and viscosity by GPC, DLS, SEM, IR, DSC, and XRD. The micelles exhibited good cellular uptake in both monolayers and spheroids of HCEC. The antibacterial and anti-biofilm activities of the micelles were evaluated on P. aeruginosa and S. aureus. The anti-quorum sensing activity was explored in P. aeruginosa by analyzing micelles' ability to produce virulence factors, including AHLs, pyocyanin, and the motility behavior of the organism. Gati@FCOL2 Ms was mucoadhesive, cornea-penetrant, antibacterial, and inhibited the biofilm formation by P. aeruginosa and S. aureus significantly more than Gati@FCOL1. A significant reduction in bacterial load in mice cornea was observed after Gati@FCOL2 Ms-treatment to the P. aeruginosa-induced bacterial keratitis-infected mice.


Assuntos
Quitosana , Ceratite , Lactatos , Camundongos , Animais , Micelas , Poloxâmero , Quitosana/farmacologia , Staphylococcus aureus , Biofilmes , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Ácido Láctico/farmacologia , Ceratite/tratamento farmacológico , Pseudomonas aeruginosa
7.
Cureus ; 15(11): e49247, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-38143606

RESUMO

OBJECTIVE: This study aims to report the successful treatment of microsporidial keratoconjunctivitis (MKC) with the combination of topical drops of voriconazole (1%) and gatifloxacin (0.5%) in all 29 patients. Demography, clinical profile, and previous treatment history were also analyzed. METHODS: A retrospective, non-comparative case series of all Gram stain-proven MKC from September 2021 to October 2022 was included in this study. Patients were given antimicrobials such as topical drops of voriconazole 1%, gatifloxacin 0.5%, or a combination of both in 29 patients based on the treatment response. Topical steroids were added to 31 patients for corneal haziness. RESULTS: A total of 33 patients were found to be positive for microsporidiosis confirmed by Gram staining. Twenty-four (72.7%) were men and nine (27.3%) were women. The mean age was 34.45±12. The presenting symptoms were mainly redness in 30 patients (90.9%), followed by watering in 13 (39.4%), foreign body sensation in 10 (30.3%), etc. Among the 23 patients (69%), a history of risk factors was identified, with 17 patients (51.5%) specifically reporting dust exposure as a major cause. MKCs were successfully treated with antimicrobials such as voriconazole 1% in three patients, gatifloxacin 0.5% in one patient, and a combination of both in 29 patients. Topical steroids were added to 31 patients for corneal haziness. At the last follow-up, a visually insignificant nummular corneal scar was noted in six patients. No drop in vision was noted in any of these patients at the end of the follow-up. No cases progressed to stromal keratitis and no surgical intervention was required in any cases. CONCLUSIONS: We successfully treated all 29 cases with a combination of voriconazole and gatifloxacin without requiring any surgical intervention or encountering stromal complications. This successful treatment in all 29 cases offers valuable insights into the potential of this drug combination, possibly attributable to its additive action or broad-spectrum coverage across various species.

8.
Antibiotics (Basel) ; 12(8)2023 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-37627738

RESUMO

Bacterial conjunctivitis (BC) entails inflammation of the ocular mucous membrane. Early effective treatment of BC can prevent the spread of the infection to the intraocular tissues, which could lead to bacterial endophthalmitis or serious visual disability. In 2003, gatifloxacin (GTX) eyedrops were introduced as a new broad-spectrum fluoroquinolone to treat BC. Subsequently, GTX use was extended to other ocular bacterial infections. However, due to precorneal loss and poor ocular bioavailability, frequent administration of the commercial eyedrops is necessary, leading to poor patient compliance. Thus, the goal of the current investigation was to formulate GTX in a lipid-based drug delivery system to overcome the challenges with the existing marketed eyedrops and, thus, improve the management of bacterial conjunctivitis. GTX-NLCs and SLNs were formulated with a hot homogenization-probe sonication method. The lead GTX-NLC formulation was characterized and assessed for in vitro drug release, antimicrobial efficacy (against methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa), and ex vivo permeation. The lead formulation exhibited desired physicochemical characteristics, an extended release of GTX over a 12 h period, and was stable over three months at the three storage conditions (refrigerated, room temperature, and accelerated). The transcorneal flux and permeability of GTX from the GTX-NLC formulation were 5.5- and 6.0-fold higher in comparison to the commercial eyedrops and exhibited a similar in vitro antibacterial activity. Therefore, GTX-NLCs could serve as an alternative drug delivery platform to improve treatment outcomes in BC.

9.
Mikrochim Acta ; 190(7): 261, 2023 06 15.
Artigo em Inglês | MEDLINE | ID: mdl-37322368

RESUMO

A molecularly imprinted electrochemical sensor was designed for the selective determination of gatifloxacin (GTX) based on dual functional monomers. Multi-walled carbon nanotube (MWCNT) enhanced the current intensity and zeolitic imidazolate framework 8 (ZIF8) provided a large surface area to produce more imprinted cavities. In the electropolymerization of molecularly imprinted polymer (MIP), p-aminobenzoic acid (p-ABA) and nicotinamide (NA) were used as dual functional monomers, and GTX was the template molecule. Taking [Fe(CN)6]3-/4- as an electrochemical probe, an oxidation peak on the glassy carbon electrode was located at about 0.16 V (vs. saturated calomel electrode). Due to the diverse interactions among p-ABA, NA, and GTX, the MIP-dual sensor exhibited higher specificity towards GTX than MIP-p-ABA and MIP-NA sensors. The sensor had a wide linear range from 1.00 × 10-14 to 1.00 × 10-7 M with a low detection limit of 2.61 × 10-15 M. Satisfactory recovery between 96.5 and 105% with relative standard deviation from 2.4 to 3.7% in real water samples evidenced the potential of the method in antibiotic contaminant determination.


Assuntos
Impressão Molecular , Polímeros , Polímeros/química , Gatifloxacina , Técnicas Eletroquímicas/métodos , Impressão Molecular/métodos , Limite de Detecção , Polímeros Molecularmente Impressos , Ácido 4-Aminobenzoico
10.
Int J Biol Macromol ; 245: 125494, 2023 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-37348586

RESUMO

The demand for advanced wound care products is rapidly increasing nowadays. In this study, gellan gum/collagen (GG/C) hydrogel films containing gatifloxacin (GAT) were developed to investigate their properties as wound dressing materials. ATR-FTIR, swelling, water content, water vapor transmission rate (WVTR), and thermal properties were investigated. The mechanical properties of the materials were tested in dry and wet conditions to understand the performance of the materials after exposure to wound exudate. Drug release by Franz diffusion was measured with all samples showing 100 % cumulative drug release after 40 min. Strong antibacterial activities against Staphylococcus aureus and Staphylococcus epidermis were observed for Gram-positive bacteria, while Escherichia coli and Pseudomonas aeruginosa were observed for Gram-negative bacteria. The in-vivo cytotoxicity of GG/C-GAT was assessed by wound contraction in rats, which was 95 % for GG/C-GAT01. Hematoxylin and eosin and Masson's trichrome staining revealed the appearance of fresh full epidermis and granulation tissue, indicating that all wounds had passed through the proliferation phase. The results demonstrate the promising properties of the materials to be used as dressing materials.


Assuntos
Antibacterianos , Colágeno , Ratos , Animais , Gatifloxacina , Antibacterianos/farmacologia , Bandagens/microbiologia , Hidrogéis/farmacologia
11.
Chemosphere ; 332: 138838, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37150453

RESUMO

The dielectric barrier discharge (DBD) multi-component system containing plasma, α-Fe2O3/FeVO4, and peroxymonosulfate (PMS) with high catalytic activity was successfully constructed. Thereinto, α-Fe2O3/FeVO4 was loaded on the honeycomb ceramic plate (HCP) surface (α-Fe2O3/FeVO4/HCP) and placed under the water surface below the discharge area. The catalytic activity was evaluated by the removal rate of gatifloxacin (GAT), and the DBD+α-Fe2O3/FeVO4+PMS system exhibited the optimal catalytic activity. The enhanced catalytic activity can be attributed to the fact that the occurrence of synergistic catalysis that simultaneously includes plasma oxidation, photocatalysis, PMS oxidation, O3 catalysis, and Fenton reaction. The effect of various initial degradation parameters including input power, PMS dosage, pH, etc. On GAT removal was investigated. DBD+α-Fe2O3/FeVO4+PMS system has a significant increase in the concentration of H2O2 and O3, and the role played in the multi-component system was analyzed. The identification and analysis of organic matters during GAT degradation were visualized with the help of 3D EEMs. HPLC-MS and theoretical calculations identified the major intermediates and further deduced the possible GAT degradation pathways. Additionally, the acute toxicity of the major intermediates was predicted by the QSAR model. Finally, the possible mechanisms of synergistic catalysis to enhance catalytic activity were discussed based on the characteristics of several advanced oxidation processes (AOPs) and the results of experimental and characterization. This work provides a feasible technical route and theoretical basis for wastewater treatment by plasma combined with other AOPs.


Assuntos
Peróxido de Hidrogênio , Peróxidos , Gatifloxacina , Peróxidos/química , Catálise
12.
Talanta ; 255: 124216, 2023 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-36587425

RESUMO

The current effort introduces a facile construction of peony-like CuO:Tb3+ nanostructure (P-L CuO:Tb3+ NS), whose characterization was determined via techniques of X-ray diffraction, scanning electron microscopy and energy dispersive X-ray spectroscopy. We investigated ofloxacin, pefloxacin and gatifloxacin oxidation electrochemically on P-L CuO:Tb3+ NS-modified glassy carbon electrode (P-L CuO:Tb3+ NS/GCE), the results of which revealed the irreversible oxidation of drugs through a two-electron oxidation process. An admirable resolution was found for this modified electrode between voltammetric peaks of ofloxacin, pefloxacin and gatifloxacin, suggesting its appropriateness for simultaneous detection of these drugs in pharmaceutical media. In addition, our nanostructure synergistically influenced the electro-catalytic oxidations of these three compounds. Differential pulse voltammetric measurements of ofloxacin, pefloxacin and gatifloxacin through our sensor showed a limit of detection of 1.9, 2.3 and 1.2 nM a as well as a linear dynamic range between 0.01 and 800.0 µM in phosphate buffered solution (0.1 M, pH = 6.0), respectively. Moreover, as-fabricated sensor could successfully co-detect these drugs in real serum and tablets specimens. In addition, since we use animal foods such as milk it is very important to detect their fluoroquinolone residues. For this purpose, the proposed sensor was tested to determine the residues of ofloxacin, pefloxacin and gatifloxacin in milk.


Assuntos
Ofloxacino , Pefloxacina , Ofloxacino/química , Gatifloxacina , Cobre/química , Térbio , Óxidos/química , Eletrodos , Técnicas Eletroquímicas/métodos
13.
Bioact Mater ; 20: 271-285, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35702608

RESUMO

Postoperative endophthalmitis (POE) has been the most threatening complication after cataract surgery, which perhaps can be solved by the antibiotic-loaded intraocular lens (IOL). However, most drug-loaded IOLs demonstrate insufficient drug quantity, short release time, increased implantation-related difficulties or other noticeable drawbacks. To prevent POE and to address these deficiencies, a drug-loaded copolymer IOL, prepared from poly (urethane acrylate) prepolymer, isobornyl methacrylate (IBOMA), N-vinyl-2-pyrrolidone (NVP), Irgacure 819, RUVA-93, and gatifloxacin (GAT), was rapidly fabricated via photocuring and by using a 3D-printed mold. This composite displayed an outstanding and controllable GAT release behavior in vitro, a high light transmittance, and a moderate refractive index. Also, it demonstrated improved strain stress and elongation compared with the reference commercial acrylic IOL material. In vivo tests demonstrated satisfying released drug concentration at the early treatment stage. In vitro and in vivo studies further confirmed the remarkable bacterial inhibition and prevention of POE by the proposed IOL, which also displayed good biocompatibility. These findings suggested that the GAT-loaded IOL could be a promising implant to prevent and cure POE, also the proposed methods could inspire more designs for various medical applications.

14.
Environ Sci Pollut Res Int ; 30(9): 23553-23567, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36327083

RESUMO

In the present study, chitosan (C), walnut (W), and almond shell (A) powder adsorbent (in different combinations as almond shells:walnut:chitosan 2:1:1 (AWC), chitosan:almond shell:walnut 2:1:1 (CAW), and walnut:almond shells:chitosan 2:1:1 (WAC)) powder were combined in different ratios to produce low-cost composite adsorbent beads for the removal of antibiotics gatifloxacin (GAT) from synthetic wastewater. The beads were characterized by a scanning electron microscope, Fourier transform infrared spectrum spectrophotometer, and energy-dispersive X-ray spectroscopy. The batch adsorption approach was employed to remove the antibiotic from the water. Moreover, isotherm and kinetics were conducted to illustrate the adsorption mechanism. Parameters like the effect of the adsorbent's dosage, pH, initial concentration, and contact time on antibiotic adsorption were evaluated. Adsorption percentage increased slightly with the increase in adsorbent dosage. The optimum pH for GAT adsorption on beads was 5-7. In addition, adsorption increased with initial antibiotic concentration and time rise. The adsorption isotherm data were successfully fitted to Langmuir isotherm for AWC and CAW beads, while WAC beads followed the Freundlich isotherm. The highest adsorption was attained at pH 5 on CAW beads and pH 7 on AWC and WAC beads. The optimal contact time for equilibrium studies was 120 min for all types of beads. The adsorption isotherm data in AWC beads fit well with the Langmuir model and Freundlich adsorption for CAW and WAC beads. The rate of adsorption on beads follows Lagergren pseudo-second-order kinetics. The results indicate that prepared combination beads can be used to remove antibiotics from wastewater.


Assuntos
Quitosana , Juglans , Prunus dulcis , Poluentes Químicos da Água , Antibacterianos , Gatifloxacina , Quitosana/química , Adsorção , Pós , Águas Residuárias , Água/química , Cinética , Concentração de Íons de Hidrogênio , Poluentes Químicos da Água/química , Espectroscopia de Infravermelho com Transformada de Fourier
15.
Chemosphere ; 307(Pt 1): 135619, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-35835247

RESUMO

A series of Ca-doped bismuth ferrite was prepared at various %w/w of Ca via a facile hydrothermal method to obtain Bi2XCa2(1-X)Fe4O9 (denoted as BFOCa-X, where X = 1, 0.95, 0.90, 0.80, 0.50). The BFOCa-X catalysts were characterized, and the results showed that they consist of pure phase BFO with nanosheet-like morphology. The as-prepared BFOCa-X catalysts were used as peroxymonosulfate (PMS) activator for gatifloxacin (GAT) removal. It was found that the catalytic activity decreased in the following order: BFOCa-0.8 (90.2% GAT removal efficiency in 45 min, kapp = 0.084 min-1)>BFOCa-0.95 > BFOCa-0.9 > BFOCa-0.5 > BFO indicating that BFOCa-0.8 has the optimized active sites for catalysis. The Ca dopant contributed to the increased oxygen vacancies and surface hydroxyl groups, promoting the catalytic PMS activation process. The kapp value increased gradually with increasing catalyst loading and PMS dosage while pH 9 presented the highest GAT removal rate. The GAT degradation rate was inhibited by PO43-, humic acid and NH4+ but promoted in the presence of Cl-, NO3- and HCO3-. It was also found that the GAT can undergo several degradation pathways in the catalytic PMS system, which eventually mineralized into innocuous compounds. The dominant reactive oxygen species (ROS) were identified using chemical scavengers, revealing that SO4•-, 1O2 and •OH contributed significantly to GAT degradation. Based on the XPS study, PMS was activated by the Fe2+/Fe3+ redox cycling and oxygen vacancies to produce SO4•-/•OH and 1O2, respectively. Overall, the BFOCa-0.8 also showed excellent reusability up to at least 4 cycles with low Bi and Fe leaching (<7 and 62 µg L-1, respectively), indicating that it has promising potential for application as PMS activator for antibiotics removal.


Assuntos
Bismuto , Substâncias Húmicas , Antibacterianos/farmacologia , Gatifloxacina , Oxigênio , Peróxidos/química , Espécies Reativas de Oxigênio
16.
Materials (Basel) ; 15(9)2022 May 08.
Artigo em Inglês | MEDLINE | ID: mdl-35591708

RESUMO

The objective of this study was to enhance the corneal permeation of gatifloxacin (GTX) using cubosomal nanoparticle as a delivery system. Cubosomal nanoparticle loaded with GTX was prepared and subjected for in vitro and in vivo investigations. The prepared GTX-loaded cubosomal particles exhibited nanoparticle size of 197.46 ± 9.40 nm and entrapment efficiency of 52.8% ± 2.93. The results of ex vivo corneal permeation of GTX-loaded cubosomal dispersion show approximately 1.3-fold increase compared to GTX aqueous dispersion. The incorporation of GTX into cubosomal particles resulted in a fourfold reduction in the minimum inhibitory concentration (MIC) value for the GTX cubosomal particles relative to GTX aqueous dispersion. Furthermore, the enhanced corneal penetration of GTX-loaded cubosomal dispersion compared was evident by a significant decrease in the area % of corneal opacity in MRSA infected rats. Moreover, these results were confirmed by photomicrographs of histological structures of corneal tissues from rats treated with GTX-cubosomal dispersion which did not present any change compared to that of the normal rat corneas. In conclusion, treatment of ocular bacterial infections and reduction in the probability of development of new resistant strains of MRSA could be accomplished with GTX-loaded cubosomal nanoparticles.

17.
Antibiotics (Basel) ; 11(4)2022 Apr 10.
Artigo em Inglês | MEDLINE | ID: mdl-35453253

RESUMO

Few articles have reported drug concentrations of different ophthalmic dosage forms in the ocular tissues. This study aimed to determine the ocular pharmacokinetics of gatifloxacin 0.3% eye gel (GTX-Gel) and gatifloxacin 0.3% eye solution (GTX-Sol) at different time intervals after topical instillation in rabbits. A total of 126 healthy New Zealand rabbits were included, of which six rabbits did not receive antibiotics (control group). The remaining rabbits were randomly divided into four groups. GTX-Gel and GTX-Sol (50 µL) were topically instilled every hour in groups A1 and B1, respectively, and every two hours in groups A2 and B2, respectively, for 12 h. Ocular tissues were collected 2, 4, 8, 12, and 24 h after administration. Gatifloxacin concentration was measured using high-performance liquid chromatography coupled with tandem mass spectrometry. The drug reached peak concentrations (Cmax) in all tissues at 8−12 h. With the same administration frequency, the Cmax was higher with GTX-Gel than with GTX-Sol (p < 0.05). Except for the iris-ciliary body, other ocular tissues did not show significant difference (p > 0.05) in gatifloxacin concentration between either pair of groups. Gatifloxacin ophthalmic gel was found to attain significantly higher concentrations than the ophthalmic solution in ocular tissues.

18.
Sci Total Environ ; 817: 152808, 2022 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-34982991

RESUMO

At present, the effect of multiple antibiotics on aerobic composting process and its mechanism are not clear. So in this study, broiler manure containing different doses of Doxycycline (DOX) and Gatifloxacin (GAT) were used as raw materials and mixed with rice hull for aerobic composting, and the effects of the combination of multiple antibiotics on the process parameters of broiler manure composting and the succession of bacterial and fungal community structures were systematically analyzed. Our results showed that at the initial period of composting, the combination of multiple antibiotics led to a delayed temperature and pH increase (T1: 57.0 °C, T2: 48.3 °C, T3: 45.5 °C on Day 3 for temperature and T1: 7.44, T2: 7.1, T3: 6.88 on Day 5 for pH), and a slow total nitrogen decrease (T1: 1.56%, T2: 1.82%, T3: 1.74% on Day 5). Although these effects decreased gradually with the degradation of antibiotics, the relative abundance of Actinobacteriota (T1: 13.29%, T2: 10.57%, T3: 8.99%) and Bacteroidota (T1:27.52%, T2:40.03%, T3:39.81%)) were still influenced by multiple antibiotic residuals until the end of composting period. Higher levels of antibiotics had more lasting effects on the bacterial community (T3 > T2). However, the combination of these two antibiotics did not significantly promote or inhibit the succession of the fungal community structure. The heatmaps showed that composting stage had a greater effect on the microbial community structures than antibiotics. The results provided a theoretical reference for composting broiler manure containing DOX and GAT.


Assuntos
Compostagem , Animais , Antibacterianos , Galinhas , Esterco , Solo
19.
International Eye Science ; (12): 265-269, 2022.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-913035

RESUMO

@#AIM: To compare the clinical efficacy and safety of gatifloxacin eye drops and levofloxacin eye drops in the treatment of acute bacterial conjunctivitis using Meta-analysis.<p>METHODS: According to the Cochrane systematic evaluation method, “gatifloxacin” “levofloxacin” and “acute bacterial conjunctivitis” were used as keywords for literature search in Embase, Cochrane library, Pubmed, Medline, CNKI, Wanfang, VIP and CBMdisc from the establishment of the database to March 1, 2021. Randomized controlled trials(RCTs)gatifloxacin eye drops and levofloxacin eye drops in the treatment of acute bacterial conjunctivitis were included. Cochrane bias risk assessment tool was used to evaluate the quality of the included studies. RevMan5.3 software was used for combined analysis. Egger's test in Stata12 was used to assess publication bias, and the level of evidence was evaluated according to the GRADE system.<p>RESULTS: A total of 10 RCTs were included in this study with 1 149 patients. The control group was treated with levofloxacin and the experimental group was treated with gatifloxacin. The results of Meta-analysis showed that the clinical effective rate of acute bacterial conjunctivitis in gatifloxacin group was higher than that in levofloxacin group(<i>OR</i>=3.75, 95%<i>CI</i>: 2.52-5.58, <i>P</i><0.00001). Egger's test suggested there was publication bias among studies. And GRADE rating results indicated, the level of evidence was VERY LOW. The incidence of adverse drug reactions in the gatifloxacin group was lower than that in levofloxacin group(<i>OR</i>=0.37, 95%<i>CI</i>: 0.19-0.71, <i>P</i>=0.003). No publication bias was observed in Egger's test and GRADE showed the level of evidence was LOW.<p>CONCLUSION: Gatifloxacin eye drops is more effective than levofloxacin eye drops in the treatment of acute bacterial conjunctivitis, and has lower adverse effect rates. And due to the low levels of evidence included, more multicenter, randomized double-blind clinical trials are needed to improve the strength of evidence for the clinical efficacy of gatifloxacin eye drops in the treatment of acute bacterial conjunctivitis.

20.
Int J Infect Dis ; 115: 142-148, 2022 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-34861398

RESUMO

SETTING: The shorter treatment regimen (STR) for multidrug- or rifampicin-resistant tuberculosis (MDR/RR-TB) has achieved successful outcomes in many countries. However, there are few studies on high-dose gatifloxacin-based STR with adverse drug reactions (ADRs) and management. DESIGN: A prospective observational study was conducted with MDR/RR-TB patients who were treated with a standardized 9 or 12 - month regimen: including gatifloxacin (Gfx), clofazimine (Cfz), ethambutol (EMB), and pyrazinamide (PZA), and supplemented by amikacin (Am), isoniazid (INH), and prothionamide (Pto) during an intensive phase of 4 or 6 - month. Monitored ADRs monthly until treatment completion and then followed up every three months for one year. RESULTS: Among the 42 eligible patients, 35 (83.3%) completed treatment successfully, 1 (2.4%) lost to follow-up (LTFU), and 6 (14.3%) failed due to ADRs, with no death. The most important ADR was drug-induced liver damage, which occurred in 24 out of 42 (57.1%) patients and resulted in 4 (9.5%) failed treatments and 4 (9.5%) adjusted treatments. QT interval prolongation occurred in 17 out of 42 (40.5%) patients, 9 (21.4%) of them with the corrected QT interval according to Fridericia (QTcF) > 500 ms resulting in 7 (16.7%) adjusted treatments. CONCLUSIONS: This study confirmed the effectiveness of the high-dose gatifloxacin-based STR but severe ADRs, especially hepatotoxicity and QT interval prolongation should never be ignored.


Assuntos
Antituberculosos , Tuberculose Resistente a Múltiplos Medicamentos , Antituberculosos/efeitos adversos , Gatifloxacina , Humanos , Isoniazida/efeitos adversos , Pirazinamida/efeitos adversos , Resultado do Tratamento , Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológico
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