RESUMEN
In the current work, Response Surface Methodology (RSM)-a statistical method-is used to optimize procedures like photocatalysis with the least amount of laboratory testing. However, to determine the most effective model for achieving the maximum rate of removal efficiency, the Response Surface Methodology was employed. The Ba-doped BiFeO3 photocatalyst was synthesized by the co-precipitation method, and its intrinsic properties were investigated by utilizing a range of spectroscopic techniques, such as FESEM, EDX, XRD, FTIR, and UV-vis. Herein, four independent factors such as, pH, contact time, pollutant concentration, and catalyst dosage were chosen. The results revealed that under acidic conditions with a contact duration of 2 min, a moderate catalyst dosage, and higher pollutant concentration, a degradation rate of 89.8% was achieved. The regression coefficient (R2) and probability value (P) were determined to be 0.99551 and 0.0301, respectively, therefore confirming the excellent fit of the RSM model. Furthermore, this research investigated the potential photocatalytic degradation mechanisms of cefixime, demonstrating that the removal efficiency of cefixime is greatly influenced by the functional parameters.
Asunto(s)
Cefixima , Nanoestructuras , Contaminantes Químicos del Agua , Catálisis , Nanoestructuras/química , Contaminantes Químicos del Agua/química , Contaminantes Químicos del Agua/análisis , Cefixima/química , Bismuto/química , Fotólisis , Procesos Fotoquímicos , Compuestos Férricos/químicaRESUMEN
Composite bio-based hydrogels have been obtaining a significant attention in recent years as one of the most promising drug delivery systems. In the present study, the preparation of composite chitosan-starch hydrogel using maleic acid as a cross-linker was optimized with the help of response surface methodology. The synthesized hydrogel was fluorescent owing to clustering of large number of functional groups. Different analytical techniques, including XRD, FTIR, SEM, XPS, fluorescence and BET were utilized to characterize the prepared hydrogel. XRD analysis confirmed the formation of non-crystalline hydrogel with random arrangement of macromolecular chains. The composite hydrogel exhibited good swelling percentage with pH sensitivity, hemocompatibility and degradability. BET analysis confirmed that the variation in concentration of crosslinker significantly influences the pore volume of the hydrogel. The synthesized composite chitosan-starch hydrogel was utilized as a prospective candidate for controlling drug release. Cefixime as a model drug was loaded onto the synthesized hydrogel utilizing the swelling diffusion method. SEM micrographs showed uniform distribution of drug molecules in the drug loaded hydrogel. In vitro drug release experiments indicated the swelling dependent drug release behaviour of chitosan-starch hydrogel with higher drug release at pH 7.4 (93.08 %) compared to pH 1.2 (67.85 %). The composite chitosan-starch hydrogel was able to prolong and control the drug release up to 12 h. The drug release from the hydrogel followed Korsmeyer-Peppas and Makoid-Banakar model with Fickian diffusion mechanism. Further, the composite hydrogel displayed excitation dependent fluorescence emission with most intense blue emission band at 425 nm with an excitation wavelength of 350 nm. The inclusion of cefixime drug in the hydrogel matrix significantly reduced the fluorescence intensity; the decrease was linearly correlated to the concentration of the drug. Moreover, the fluorescence emission the chitosan-starch hydrogel was found to be dependent upon pH. The synthesized hydrogel is expected to be a potential candidate for controlled drug release as well as for fluorescent sensing applications.
Asunto(s)
Quitosano , Portadores de Fármacos , Sistemas de Liberación de Medicamentos , Liberación de Fármacos , Hidrogeles , Almidón , Quitosano/química , Almidón/química , Hidrogeles/química , Portadores de Fármacos/química , Concentración de Iones de Hidrógeno , Cefixima/químicaRESUMEN
In this research, an upgraded and environmentally friendly process involving WO3/Co-ZIF nanocomposite was used for the removal of Cefixime from the aqueous solutions. Intelligent decision-making was employed using various models including Support Vector Regression (SVR), Genetic Algorithm (GA), Artificial Neural Network (ANN), Simulation Optimization Language for Visualized Excel Results (SOLVER), and Response Surface Methodology (RSM). SVR, ANN, and RSM models were used for modeling and predicting results, while GA and SOLVER models were employed to achieve the optimal conditions for Cefixime degradation. The primary goal of applying different models was to achieve the best conditions with high accuracy in Cefixime degradation. Based on R analysis, the quadratic factorial model in RSM was selected as the best model, and the regression coefficients obtained from it were used to evaluate the performance of artificial intelligence models. According to the quadratic factorial model, interactions between pH and time, pH and catalyst amount, as well as reaction time and catalyst amount were identified as the most significant factors in predicting results. In a comparison between the different models based on Mean Absolute Error (MAE), Root Mean Square Error (RMSE), and Coefficient of Determination (R2 Score) indices, the SVR model was selected as the best model for the prediction of the results, with a higher R2 Score (0.98), and lower MAE (1.54) and RMSE (3.91) compared to the ANN model. Both ANN and SVR models identified pH as the most important parameter in the prediction of the results. According to the Genetic Algorithm, interactions between the initial concentration of Cefixime with reaction time, as well as between the initial concentration of Cefixime and catalyst amount, had the greatest impact on selecting the optimal values. Using the Genetic Algorithm and SOLVER models, the optimum values for the initial concentration of Cefixime, pH, time, and catalyst amount were determined to be (6.14 mg L-1, 3.13, 117.65 min, and 0.19 g L-1) and (5 mg L-1, 3, 120 min, and 0.19 g L-1), respectively. Given the presented results, this research can contribute significantly to advancements in intelligent decision-making and optimization of the pollutant removal processes from the environment.
Asunto(s)
Cefixima , Aprendizaje Automático , Nanocompuestos , Óxidos , Tungsteno , Nanocompuestos/química , Óxidos/química , Tungsteno/química , Cefixima/química , Redes Neurales de la Computación , Cobalto/química , Algoritmos , Contaminantes Químicos del Agua/química , Antibacterianos/química , Purificación del Agua/métodosRESUMEN
The increase in antibiotic residues poses a serious threat to ecological and aquatic environments, necessitating the development of cost-effective, convenient, and recyclable adsorbents. In our study, we used cellulose-based layered double hydroxide (LDH) as an efficient adsorbent and nanocarrier for both sulfamethoxazole (SMX) and cefixime (CFX) residues due to their biodegradability and biocompatibility. Chemical processes are measured according to green chemistry metrics to identify which features adhere to the principles. A GREEnness Assessment (ESA), Analytical GREEnness Preparation (AGREEprep), and Analytical Eco-Scale Assessments (ESA) were used to assess the suitability of the proposed analytical method. We extensively analyzed the synthesized CoFe LDH/cellulose before and after the adsorption processes using XRD, FTIR, and SEM. We investigated the factors affecting the adsorption process, such as pH, adsorbent dose, concentrations of SMX and CFX and time. We studied six nonlinear adsorption isotherm models at pH 5 using CoFe LDH, which showed maximum adsorption capacities (qmax) of 272.13 mg/g for SMX and 208.00 mg/g for CFX. Kinetic studies were also conducted. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was performed on Vero cells in direct contact with LDH nanocomposites to evaluate the cytotoxicity and side effects of cellulose-based CoFe LDH. The cellulose-based CoFe LDH nanocomposite demonstrated excellent cytocompatibility and less cytotoxic effects on the tested cell line. These results validate the potential use of these unique LDH-based cellulose cytocompatible biomaterials for water treatment applications. The cost of the prepared adsorbents was investigated.
Asunto(s)
Cefixima , Celulosa , Sulfametoxazol , Contaminantes Químicos del Agua , Celulosa/química , Sulfametoxazol/química , Sulfametoxazol/toxicidad , Adsorción , Contaminantes Químicos del Agua/química , Contaminantes Químicos del Agua/toxicidad , Animales , Cefixima/química , Antibacterianos/química , Antibacterianos/toxicidad , Células Vero , Hidróxidos/química , Chlorocebus aethiops , Nanocompuestos/química , Nanocompuestos/toxicidad , Tecnología Química Verde/métodosRESUMEN
Effective drug delivery for is the foremost requirement for the complete recovery of the disease. Nanomedicine and nanoengineering has provided so many spaces and ideas for the drug delivery design, whether controlled, targeted, or sustained. Different types of nanocarriers or nanoparticles are aggressively designed for the drug delivery applications. Clay minerals are identified as a one of the potential nanocarrier for the drug delivery. Owing to their biocompatibility and very low cytotoxicity, clay minerals showing effective therapeutic applications. In the present investigation, clay mineral, i.e., Halloysite nano tubes are utilized as a nanocarrier for the delivery of antibiotic cefixime (CFX), a third-generation cephalosporin. The HNT was first functionalized with the sulfuric acid and then further treated with the 3-(aminopropyl)triethoxysilane (APTES). The drug is loaded on three different classifications of HNTs, i.e., Bare-CFX-HNT, Acid-CFX-HNT, and APTES-CFX-HNT and their comparative analysis is established. Different characterization techniques such as X-ray diffractometry (XRD), Fourier transform infra-red (FT-IR), Transmission electron microscopy TEM), Brunauer-Emmett-Teller (BET), adsorption studies, and Thermogravimetric analysis (TGA) were performed to evaluate their chemical, structural, morphological, and thermal properties. TGA confirmed the encapsulation efficiency of Bare-CFX-HNT, Acid-CFX-HNT, and APTES-CFX-HNT as 42.65, 52.19, and 53.43%, respectively. Disk diffusion and MTT assay confirmed that the drug loaded HNTs have potential antibacterial activities and less cytotoxicity. The adsorption capacity of CFX with different HNTs are evaluated and Different adsorption and kinetic models have been discussed. Drug release studies shows that APTES-CFX-HNT showing sustained release of cefixime as compared to Bare-CFX-HNT and Acid-CFX-HNT.
Asunto(s)
Antibacterianos , Cefixima , Arcilla , Cefixima/química , Antibacterianos/química , Arcilla/química , Portadores de Fármacos/química , Silicatos de Aluminio/química , Nanopartículas/química , Silanos/química , Espectroscopía Infrarroja por Transformada de Fourier , PropilaminasRESUMEN
Patients suffering from dysphagia have trouble in swallowing conventional oral dosage forms and there is also risk of choking, which may cause patient noncompliance. This study aimed to develop an orodispersible film (ODF) containing cefixime trihydrate (CFX) to cope with the above-mentioned problems as well as to enhance water solubility and masking the bitter taste of the drug. The freeze-drying and kneading methods were used for the formation of inclusion complexes. The physicochemical evaluation revealed that T7 was the best film for the incorporation of pure drug and inclusion complexes. Films were further characterized for physical and mechanical properties. Drug content, dissolving time of the film and drug release tests were performed. In vivo taste and disintegration time studies were also conducted in healthy human volunteers. FTIR spectra of the individual ingredients and prepared formulations have confirmed the chemical compatibilities of the ingredients. The solubility of CFX was increased by complexation with ß-CD and optimized freeze-dried inclusion complex (FD1) was selected for the formation of ODF. C4 was selected as an optimized film for the delivery of CFX as this film has released 95.52% drug at the end of 10 min. Dissolution kinetics of FD1 showed that it followed zero-order kinetics while drug release from films, exhibits first-order kinetics; however, both showed non-Fickian transport. In vivo taste evaluation revealed that taste was masked by inclusion complexation with ß-CD. However, selected ingredients and employed methodology enabled to formulate film, capable of delivering taste-masked CFX with improved solubility and better patient compliance.
Asunto(s)
Cefixima/química , Gusto , Administración Oral , Composición de Medicamentos , Liberación de Fármacos , Humanos , SolubilidadRESUMEN
BACKGROUND: Developing a new excipient and obtaining its market approval is an expensive, time-consuming and complex process. Compared to that, the co-processing of already approved excipients has emerged as a more attractive option for bringing better characteristic excipients to the market. The application of the Design of Experiments (DoE) approach for developing co-processed excipient can make the entire process cost-effective and rapid. OBJECTIVE: The aim of the present investigation was to demonstrate the applicability of the DoE approach, especially 32 full factorial design, to develop a multi-functional co-processed excipient for the direct compression of model drug - cefixime trihydrate using spray drying technique. METHODS: The preliminary studies proved the significant effect of atomization pressure (X1) and polymer ratio (microcrystalline cellulose: mannitol - X2) on critical product characteristics, so they were selected as independent variables. The angle of repose, Carr's index, Hausner's ratio, tensile strength and Kuno's constant were selected as response variables. RESULT: The statistical analysis proved a significant effect of both independent variables on all response variables with a significant p-value < 0.05. The desirability function available in Design Expert 11® software was used to prepare and select the optimized batch. The prepared co-processed excipient had better compressibility than individual excipients and their physical mixture and was able to accommodate more than 40 percent drug without compromising the flow property and compressibility. CONCLUSION: The present investigation successfully proved the applicability of 32 full factorial design as an effective tool for optimizing the spray drying process to prepare a multi-functional co-processed excipient.
Asunto(s)
Antibacterianos/química , Cefixima/química , Celulosa/química , Composición de Medicamentos , Humanos , Manitol/química , Resistencia a la TracciónRESUMEN
Two drugs (cefpirome, cefixime) as dual-action inhibitors could self-organize on copper surface forming bio-functional protective film, which effectively prevents copper corrosion in the picking process with an excellent performance on the resistance of Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus). Energy dispersive X-ray spectroscopy (EDS) and X-ray photoelectron spectroscopy (XPS) results showed that studied drugs can self-organize on copper surface successfully forming adsorption film to protect copper. The results also indicated that N/S atoms with the lone pair electrons in the drugs donated electrons to the vacant orbital of Cu occupying the active sites of copper surface. Electrochemistry and surface morphology study revealed that the corrosion inhibition efficiency of cefixime was better than cefpirome. Furthermore, adsorption isotherm study suggested that the adsorption was spontaneous chemical and physical adsorption, obeying Langmuir adsorption.
Asunto(s)
Antibacterianos/farmacología , Cefixima/farmacología , Cefalosporinas/farmacología , Cobre/química , Escherichia coli/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Adsorción , Antibacterianos/química , Cefixima/química , Cefalosporinas/química , Corrosión , Electrones , Pruebas de Sensibilidad Microbiana , Conformación Molecular , Tamaño de la Partícula , Acero/química , Propiedades de Superficie , CefpiromaRESUMEN
Antimicrobial resistance is a grave threat to human life. Currently used time-consuming antibiotic susceptibility test (AST) methods limit physicians in selecting proper antibiotics. Hence, we developed a rapid AST using electroanalysis with a 15 min assay time, called EAST, which is live-monitored by time-lapse microscopy video. The present work reports systematical electrochemical analysis and standardization of protocol for EAST measurement. The proposed EAST is successfully applied for Gram-positive Bacillus subtilis and Gram-negative Escherichia coli as model organisms to monitor bacterial concentration, decay kinetics in the presence of various antibiotics (ciprofloxacin, cefixime, and amoxycillin), drug efficacy, and IC50. Bacterial decay kinetics in the presence of antibiotics were validated by the colony counting method, field emission scanning electron microscopy, and atomic force microscopy image analysis. The EAST predicts the antibiotic susceptibility of bacteria within 15 min, which is a significant advantage over existing techniques that consume hours to days. The EAST was explored further by using bacteria-friendly l-lysine-functionalized cerium oxide nanoparticle coated indium tin oxide as a working electrode to observe the enhanced electron-transfer rate in the EAST. The results are very significant for future miniaturization and automation. The proposed EAST has huge potential in the development of a rapid AST device for applications in the clinical and pharmaceutical industries.
Asunto(s)
Antibacterianos/farmacología , Bacillus subtilis/efectos de los fármacos , Bacillus subtilis/metabolismo , Técnicas Electroquímicas , Escherichia coli/efectos de los fármacos , Escherichia coli/metabolismo , Amoxicilina/química , Amoxicilina/farmacología , Antibacterianos/química , Cefixima/química , Cefixima/farmacología , Ciprofloxacina/química , Ciprofloxacina/farmacología , Pruebas de Sensibilidad Microbiana , Factores de TiempoRESUMEN
Cefixime is a third generation orally administered cephalosporin that is frequently used as a broad spectrum antibiotic against various gram-negative and gram-positive bacteria. In this study, a simple and sensitive fluorescent sensor for the determination of the cefixime and ctDNA was established based on the CdTe:Zn2+ quantum dots (QDs). The fluorescence of CdTe:Zn2+ QDs can be effectively quenched by cefixime in virtue of the surface binding of cefixime on CdTe:Zn2+ QDs and the subsequent photoinduced electron transfer process from CdTe:Zn2+ QDs to cefixime, in particular, the high sensitivity of QDs fluorescence emission to cefixime at the micromole per liter level, which render the cefixime-CdTe:Zn2+ QDs system into fluorescence "OFF" status, then turn on in the presence of ctDNA. Furthermore, the Fourier transform infrared (FTIR) spectra of characteristic bands of C-N and N-H groups of cefixime endow evidence for the interaction of cefixime with CdTe:Zn2+ QDs. The relative electrochemical behavior of the affinity of CdTe:Zn2+ QDs for cefixime and ctDNA reveals the potential molecular binding mechanism.
Asunto(s)
Técnicas Biosensibles , Compuestos de Cadmio/química , Cefixima/aislamiento & purificación , ADN Tumoral Circulante/aislamiento & purificación , Telurio/química , Cefixima/sangre , Cefixima/química , ADN Tumoral Circulante/sangre , ADN Tumoral Circulante/química , Transporte de Electrón/efectos de los fármacos , Fluorescencia , Humanos , Puntos Cuánticos/química , Espectrometría de Fluorescencia , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
The over-use of antibiotics has caused a number of problems such as contamination of antibiotic residues and virus resistance, and therefore has attracted global attention. In this study, spectroscopic techniques and molecular docking were employed to predict conformational changes and binding interaction between two cephalosporins (cefaclor and cefixime) and calf thymus DNA (ctDNA). Fluorescence and UV-vis spectra suggested that static quenching was predominant and cephalosporin bound to the groove region of ctDNA. Binding parameters calculated by the Stern-Volmer and Scatchard equations showed that cephalosporin bound to ctDNA with a binding affinity in the order of 103 L mol-1 . Thermodynamic parameters further indicated that the reaction was a spontaneous process driven by enthalpy and entropy, and that the main binding force was an electrostatic force. The effects of iodide, denaturant, thermal denaturation and pH on a cephalosporin-Hoechst-DNA complex were also studied, and the results confirmed that cephalosporin bound to the groove area of DNA. Finally, these results were further confirmed by molecular docking and electrochemical studies.
Asunto(s)
Antibacterianos/química , Cefaclor/química , Cefixima/química , ADN/química , Técnicas Electroquímicas , Simulación del Acoplamiento Molecular , Animales , Sitios de Unión , Bovinos , Concentración de Iones de Hidrógeno , Conformación Molecular , Espectrometría de Fluorescencia , Espectrofotometría Ultravioleta , TermodinámicaRESUMEN
Chitosan (biopolymer) and polyvinyl pyrolidone (PVP) with aminopropyletriethoxy silane (cross linker) based hydrogels were prepared and tested for controlled drug release. The drug release and kinetics were studied as a function of pH. Formulations were characterized by Fourier Transform Infrared (FTIR) and Thermogravimetric (TGA) analysis and TAP 32 hydrogel formulation was the most stable and hydrogel samples showed promising antibacterial activity against E. coli strain. The maximum swelling (4386%) was observed for TAP 32 formulation in distilled water, which was decreased with the concentration of ions. The diffusion exponent (n) values of all hydrogel formulations were recorded to be <0.5, which is an indication of Quasi-Fickian diffusion. The maximum swelling was observed at pHâ¯2 and decreased at higher pH. The pH sensitivity of hydrogels found to be promising for their use in drug delivery, which was tested for cefixime drug. Drug release of 81.6% was observed for the period of 12â¯h in a simulated gastric fluid (SGF). The values of R2 for zero order, first order, Higuchi, Hixson, Korsmeyer-Peppas and Baker-Lonsdale were 0.97, 0.9818, 0.99, 0.99, 0.88 and 0.80, respectively. The hydrogels based on chitosan and PVP revealed potential for controlled cefixime drug release in gastric pH medium.
Asunto(s)
Antibacterianos/administración & dosificación , Cefixima/administración & dosificación , Quitosano/química , Hidrogeles/química , Antibacterianos/química , Cefixima/química , Preparaciones de Acción Retardada , Difusión , Liberación de Fármacos , Escherichia coli/efectos de los fármacos , Concentración de Iones de Hidrógeno , Cinética , Espectroscopía Infrarroja por Transformada de Fourier , TermogravimetríaRESUMEN
Aim: The present work focused on the development of sustained-release microsphere formulation of cefixime to provide reduction in dosing frequency, improved antibacterial activity and patient compliance. Methodology & results: Microspheres were prepared by modified emulsion solvent evaporation method and evaluated by in vitro and in vivo studies. Optimized formulation (FK-07) was found to have entrapment efficiency of 81.12 ± 0.93% and particle size of 166.82 ± 0.86 µm. FK-07 sustained release up to 24 h as demonstrated by in vitro drug release and in vivo pharmacokinetic study in rats. FK-07 showed approximately twofold increase in bioavailability and twofold decrease in MIC90 value against Escherichia coli, Klebsiella pneumoniae and Salmonella typhi in comparison to marketed formulation. Conclusion: Sustaining the release of cefixime using microspheres enhanced its bioavailability, antibacterial efficacy and will help in reducing its dosing frequency.
Asunto(s)
Antibacterianos/química , Cefixima/química , Microesferas , Administración Oral , Animales , Antibacterianos/metabolismo , Antibacterianos/farmacología , Cefixima/metabolismo , Cefixima/farmacología , Portadores de Fármacos/química , Composición de Medicamentos , Liberación de Fármacos , Escherichia coli/efectos de los fármacos , Semivida , Klebsiella pneumoniae/efectos de los fármacos , Tamaño de la Partícula , Ratas , Salmonella typhi/efectos de los fármacosRESUMEN
This study aimed to investigate the effect of different polymers (polyethylene glycol 4000 and 6000 and Soluplus®) on the enhancement of solubility, dissolution, and stability of cefixime trihydrate as a selected class II model drug. Different solid dispersions have been prepared using conventional methods and supercritical fluid technology. The effect of co-solvent incorporation in supercritical fluid technology was also studied. Physicochemical properties for solid dispersions were investigated using Fourier transform infrared analysis, differential scanning calorimetry, thermogravimetric analysis, powder X-ray diffraction, and scanning electron microscopy. The solubility of the prepared solid dispersions increased except for those prepared with Soluplus® using supercritical fluid technology without co-solvent. The best enhancement in the release profile was recorded by Soluplus®-based solid dispersions prepared using a conventional method. The conventional methods of preparation and the presence of co-solvent in supercritical fluid technology converted cefixime into its amorphous form.
Asunto(s)
Antibacterianos/química , Cefixima/química , Polietilenglicoles/química , Polivinilos/química , Antibacterianos/análisis , Rastreo Diferencial de Calorimetría/métodos , Cefixima/análisis , Cromatografía con Fluido Supercrítico/métodos , Polietilenglicoles/análisis , Polivinilos/análisis , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Difracción de Rayos XRESUMEN
This study reports a colorimetric sensor with excellent sensitivity to detect Cefixime base on gold nanoparticles. Cefixime is an antibiotic which has a wide range of applications in medicine. Cefixime did not change the surface plasmon resonance bond in gold nanoparticles solution; therefore, there was no change in the color solution of gold nanoparticles. The presence of Alizarin Red S in the system was necessary for the degradation of Cefixime, resulting in the aggregation of gold nanoparticles and a color change from red to blue. As a result of aggregation, the localized surface plasmon resonance band of gold nanoparticles decreased to around 525â¯nm and a new red-shifted band at 640â¯nm appeared which increases gradually as the function of Cefixime concentration. A unique detection limit (2.5â¯ngâ¯mL-1) was achieved for Cefixime in comparison with other colorimetric methods. Relative standard deviations (RSD) for 40.0 and 140.0â¯ngâ¯mL-1 of Cefixime were 2.6 and 1.8% for intra-day respectively. A possible mechanism was discussed for the surface plasmon resonance changes of AuNPs in the presence of Cefixime. The proposed method was applied to detect Cefixime in pharmaceutical samples with satisfactory results. This system is low-cost and is highly sensitive with no need for any preconcentration steps or using any expensive or sophisticated instrumentation.
Asunto(s)
Cefixima/análisis , Colorimetría/métodos , Nanopartículas del Metal/química , Resonancia por Plasmón de Superficie/métodos , Antraquinonas/química , Cefixima/química , Colorantes/química , Oro/química , Concentración de Iones de Hidrógeno , Límite de Detección , Comprimidos/análisisRESUMEN
Chitosan-alginate microspheres (MS) were developed for cefixime vaginal administration, to overcome problems associated with its oral administration. The effect of increasing drug-loading amount, by keeping the chitosan-alginate content constant, was investigated. Mucoadhesion studies indicated that all formulations assured in situ permanence longer than 2â¯h. Entrapment efficiency increased with drug loading concentration in the starting solution, reaching a plateau at 30â¯mg/mL indicative of the achievement of an optimal drug-to-polymer ratio. MS swelling properties increased with the entrapped drug amount, and, interestingly, water-uptake reached its maximum value at the same drug loading concentration of 30â¯mg/mL. The relationship found between MS water-uptake and drug release rate confirmed MS prepared with 30â¯mg/mL cefixime as the best formulation. Microbiological studies showed a relation between cefixime release rate from MS and Escherichia coli viability reduction, definitely indicating the selected MS formulation as the best for an effective local treatment of urogenital infections.
Asunto(s)
Alginatos/química , Cefixima/química , Cefixima/farmacología , Quitosano/química , Portadores de Fármacos/química , Microesferas , Adhesividad , Administración Intravaginal , Antiinfecciosos/administración & dosificación , Antiinfecciosos/química , Antiinfecciosos/farmacología , Cefixima/administración & dosificación , Liberación de Fármacos , Escherichia coli/efectos de los fármacos , Ácido Glucurónico/química , Ácidos Hexurónicos/química , Membrana Mucosa/químicaRESUMEN
Solution based method for the formation of chemically modified silver nanoparticles (CX-AgNPs) using Cefixime as stabilizing and reducing agent was developed. The CX-AgNPs were characterized by AFM, UV-visible, FT-IR and MALDI-TOF MS. Bactericidal efficiency of CX-AgNPs and Cefixime against Streptococcus pyogenes was evaluated. Afterwards, susceptibility differences of Streptococcus pyogenes due to accumulation of Hg(II) against CX-AgNPs and Cefixime were estimated and validated through Atomic force microscopy. Selectivity and sensitivity of CX-AgNPs against Hg(II) was evaluated in a systematic manner. The CX-AgNPs was titrated against optically silent Hg(II) which induced enhancement in the SPR band of CX-AgNPs. The increase in intensity of SPR band of CX-AgNPs was determined to be proportionate to the concentration of Hg(II) in the range of 33.3-700µM obeying linear regression equation of y = 0.125x + 8.962 with the detection limit of 0.10µM and the coefficient of determination equals to 0.985 (n = 3). The association constant Ka of CX-AgNPs-Hg(II) was found to be 386.0095mol-1dm3 by using the Benesi Hildebrand plot.
Asunto(s)
Antibacterianos/farmacología , Cefixima/farmacología , Mercurio/metabolismo , Nanopartículas del Metal/química , Nanoconjugados/química , Plata/farmacología , Streptococcus pyogenes/efectos de los fármacos , Antibacterianos/química , Cefixima/química , Límite de Detección , Pruebas de Sensibilidad Microbiana , Microscopía de Fuerza Atómica , Plata/química , Espectroscopía Infrarroja por Transformada de Fourier , Streptococcus pyogenes/metabolismoRESUMEN
Cephalosporins belong the largest class of antibiotics used in the treatment of a wide range of infectious diseases caused by susceptible organisms. In the present study, we chose two typical antibiotics cefalexin/cefixime based on their structure, and investigated the interaction of cephalexin/cefixime with bovine serum albumin (BSA) using UV-vis absorption spectra, fluorescence spectroscopy, circular dichroism (CD) spectroscopy and molecular modeling approaches. Spectroscopic experiments revealed the formation of a BSA - cefalexin/cefixime complex. The binding parameters calculated using a modified Stern - Volmer method and the Scatchard method reached 103 -104 L·mol-1 . Thermodynamic parameter studies revealed that binding characteristics by negative enthalpy and positive entropy changes, and electrostatic interactions play a major role. Site marker competitive displacement experiments and molecular modeling approaches demonstrated that cefalexin and cefixime bind with appropriate affinity to site I (subdomain IIA) of BSA. Furthermore, synchronous fluorescence spectra, CD spectra and molecular modeling results indicated that the secondary structure of BSA was changed in the presence of cefalexin and cefixime. Additionally, the effects of metal ions on the BSA - cefalexin/cefixime system were also assessed.
Asunto(s)
Cefixima/química , Cefalexina/química , Albúmina Sérica Bovina/química , Animales , Bovinos , Dicroismo Circular , Modelos Moleculares , Conformación Molecular , Estructura Molecular , Espectrometría de Fluorescencia , Espectrofotometría Ultravioleta , TermodinámicaRESUMEN
In this study, three novel, sensitive, simple and validated spectrophotometric and spectrofluorimetric methods have been proposed for estimation of some important antimicrobial drugs. The first two methods have been proposed for estimation of two important third-generation cephalosporin antibiotics namely, cefixime and cefdinir. Both methods were based on condensation of the primary amino group of the studied drugs with acetyl acetone and formaldehyde in acidic medium. The resulting products were measured by spectrophotometric (Method I) and spectrofluorimetric (Method II) tools. Regarding method I, the absorbance was measured at 315nm and 403nm with linearity ranges of 5.0-140.0 and 10.0-100.0µg/mL for cefixime and cefdinir, respectively. Meanwhile in method II, the produced fluorophore was measured at λem 488nm or 491nm after excitation at λex 410nm with linearity ranges of 0.20-10.0 and 0.20-36.0µg/mL for cefixime and cefdinir, respectively. On the other hand, method III was devoted to estimate nifuroxazide spectrofluorimetrically depending on formation of highly fluorescent product upon reduction of the studied drug with Zinc powder in acidic medium. Measurement of the fluorescent product was carried out at λem 335nm following excitation at λex 255nm with linearity range of 0.05 to 1.6µg/mL. The developed methods were subjected to detailed validation procedure, moreover they were used for the estimation of the concerned drugs in their pharmaceuticals. It was found that there is a good agreement between the obtained results and those obtained by the reported methods.
Asunto(s)
Antiinfecciosos/análisis , Preparaciones Farmacéuticas/análisis , Espectrometría de Fluorescencia/métodos , Espectrofotometría/métodos , Cefdinir , Cefixima/análisis , Cefixima/química , Cefalosporinas/análisis , Cefalosporinas/química , Ácido Clorhídrico/química , Polvos , Solventes/química , Temperatura , Factores de Tiempo , Zinc/químicaRESUMEN
Novel, safe, efficient, and cost effective surfactants from renewable resources has attracted attention for enhancing solubility and bioavailability of hydrophobic dugs. We report the synthesis, characterization, and biocompatibility of a novel non-ionic acyl glycoside double-tailed surfactant for niosomal drug delivery system. Structure of the surfactant was confirmed by 1H NMR and mass spectroscopy. Applications of surfactant in niosomal drug delivery were explored using Cefixime as model. The shape, size, and polydispersity index (PDI) of drug loaded vesicles were investigated with atomic force microscope (AFM) and dynamic light scattering (DLS). Drug entrapping efficiency (EE%) was determined using HPLC. Biocompatibility of the surfactant was evaluated by in vitro cytotoxicity, blood hemolysis, and in vivo acute toxicity. Bioavailability of the surfactant based formulation was investigated in rabbits using HPLC. Vesicles were found to be 159.76 ± 6.54 nm with narrow size distribution and spherical shape. EE% was found to be 71.39 ± 3.52%. Novel surfactant was non-cytotoxicity and hemo-compatible even at 1000 µg/mL concentration and was safe up to 2000 mg/kg body weight. The in vivo bioavailability of niosomal formulation showed elevated plasma concentration and decreased clearance of Cefixime. Current findings reveal that this novel surfactant is biocompatible and could be employed for niosomal drug delivery.