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Mild aqueous Zn batteries (AZBs) generally suffer a low-voltage/energy dilemma, which compromises their competitiveness for large-scale energy storage. Pushing Zn anode potential downshift is an admissible yet underappreciated approach for high-voltage/energy AZBs. Herein, with a mild hybrid electrolyte containing in situ-derived diluted strongly-coordinated Zn2+ -cosolvent pairs, a considerable Zn anode potential downshift is initially achieved for high-voltage Zn-based hybrid batteries. The chosen butylpyridine cosolvent not only strongly coordinates Zn2+ ions but also acts as a hydrogen-bond end-capping agent to inhibit hydrogen evolution reaction (HER). The electrolyte environment with hetero-solvation-diluted strongly-coordinated Zn2+ -cosolvent pairs remarkably lowers Zn2+ activity, responsible for the Zn electrode potential downshift (-0.330 V vs Zn), confirming to modified Nernst law (ΔE = R T n F $\frac{{RT}}{{nF}}$ ln[a(Zn2 + )/a(coordinated solvent)]). With the diluted Zn2+ -containing hybrid electrolyte, the Zn//Zn symmetric cell in the hybrid electrolyte shows a long lifespan over 1270 h at a stripping/plating capacity of 0.4 mA h cm-2 . Compared with in common hybrid electrolytes, the as-assembled Zn-MnO2 hybrid battery delivers a ca. 0.278 V enhanced voltage plateau (1.57 V) and a long-term cyclability of over 736 cycles. This work opens a new avenue toward Zn anode potential downshift for high-voltage AZBs, which can extend to other mild metal batteries.
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A fast, simple, accurate, precise, and cheap fluorimetric protocol has been proposed for analysis of a phosphodiesterase-IV inhibitor, namely drotaverine hydrochloride. Fluorimetric protocol is based on estimating the decrease in the eosin Y fluorescence intensity by quantitative addition of drotaverine at pH 3.1 (acetate buffer). An ion pair complex is formed, which leads to quenching in the fluorescence intensity of the dye without need of prior extraction at 534 nm (λex. 339 nm). Different reaction perimeters which influence the production of complex (ion pair between drotaverine and eosin) were deeply investigated and optimized. The developed fluorimetric protocol is capable for quantitative estimation of drotaverine in linear range of 0.4 to 2.5 µg mL-1. After method validation in respect to ICH guidelines, it was applied to determine drotaverine in its commercial preparation. By comparing with other reported method, the developed and validated fluorimetric protocol is capable for estimation of drotaverine in commercial preparation with good accuracy and excellent precision.
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The (R)-(6-Methoxyquinolin-4-yl)[(1S,2S,4S,5R)-5-vinylquinuclidin-2-yl]methanol (quinine)-tetraphenylborate complex was synthesized by reacting sodium tetraphenyl borate with quinine in deionized water at room temperature through an ion-pair reaction (green chemistry) at room temperature. The solid complex was characterized by several physicochemical methods. The formation of ion-pair complex between bio-active molecules and/or organic molecules is crucial to comprehending the relationships between bioactive molecules and receptor interactions. The complex under study was examined for antimicrobial activity. All theoretical calculations were carried out in vacuum and water using the B3LYP level 6-311G(d,p) levels of theory. The theoretical computation allowed for the prediction and visualization of ionic interactions, which explained the complex's stability. The results of energy optimization showed that the Q-TPB complex is stable with a negative complexation energy. The obtained geometries showed that the boron (B-) and nitrogen (N+) in piperidine of the two molecules tetraphenylborate and quinine are close to each other, which makes it possible for ions to interact. The modest energy gap between HOMO and LUMO showed that the compound was stable. The computation of the electron transitions of the two models by density functional theory (TD-DFT) in the solvent at the theoretical level B3LYP/6-311G(d,p) allowed for the detection of three UV/visible absorption bands for both models and the discovery of a charge transfer between the host and the guest. The UV absorption, infrared, and H NMR are comparable with the experimental part.
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Rivastigmine hydrogen tartrate (RIV-HT) is given orally for Alzheimer's disease. However, oral therapy shows low brain bioavailability, short half-life and gastrointestinal-mediated adverse effects. RIV-HT intranasal delivery can avoid these side effects, but its low brain bioavailability remains challenging. These issues could be solved with hybrid lipid nanoparticles with enough drug loading to enhance RIV-HT brain bioavailability while avoiding oral route side effects. The RIV-HT and docosahexaenoic acid (DHA) ion-pair complex (RIV:DHA) was prepared to improve drug loading into lipid-polymer hybrid (LPH) nanoparticles. Two types of LPH, i.e., cationic (RIV:DHA LPH(+ve)) and anionic LPH (RIV:DHA LPH(-ve)) were developed. The effect of LPH surface charge on in-vitro amyloid inhibition, in-vivo brain concentrations and nose-to-brain drug targeting efficiency were investigated. LPH nanoparticles showed concentration dependant amyloid inhibition. RIV:DHA LPH(+ve) demonstrated relatively enhanced Aß1-42 peptide inhibition. The thermoresponsive gel embedded with LPH nanoparticles improved nasal drug retention. LPH nanoparticles gel significantly improved pharmacokinetic parameters compared to RIV-HT gel. RIV:DHA LPH(+ve) gel showed better brain concentrations than RIV:DHA LPH(-ve) gel. The histological examination of nasal mucosa treated with LPH nanoparticles gel showed that the delivery system was safe. In conclusion, the LPH nanoparticle gel was safe and efficient in improving the nose-to-brain targeting of RIV, which can potentially be utilized in managing Alzheimer's.
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Enfermedad de Alzheimer , Nanopartículas , Humanos , Rivastigmina , Enfermedad de Alzheimer/tratamiento farmacológico , Ácidos Docosahexaenoicos , Encéfalo , Administración Intranasal , Polímeros/farmacologíaRESUMEN
The detection of local anesthetic drugs is of great importance in the analysis of pharmaceutical, clinical and forensic samples. This paper reports a simple and sensitive potentiometric assay suitable for detecting general local anesthetics (LAs) of two types, namely: amino ester-anesthetics (procaine) and amino amide-anesthetics (lidocaine, articaine). As a detector, a new highly sensitive sensor based on a poly(vinyl chloride)-matrix membrane incorporating ion-pair complexes of protonated procaine with 2-[bis-octadecyl-sulfonic)-closo-decaborate is used. To improve the analytical characteristics of the sensor, the tetradodecylammonium - 2-[bis-octadecyl-sulfonic)-closo-decaborate associate as a lipophilic additive is proposed. The procedures for the synthesis of both electroactive membrane components are described. The dependence of potential response characteristics of the potentiometric system on the membrane composition, local anesthetic properties, and pH of the sample solutions is discussed. The difference in sensitivity and selectivity of the sensor was found to be responsible for the lipophilic property and pKa values of local anesthetic molecules. The developed sensor exhibited a near Nernstian response to cationic forms of procaine and some other anesthetics of higher lipophility, in particular lidocaine and articaine, over a wide linear concentration range. The limit of detection was varied from 2 × 10-8 to 5 × 10-7 µM, and it is the lowest value among the early published potentiometric analogs. The proposed method was successfully applied to the analysis of pharmaceutical formulations and spiked enzyme-free urine samples containing LAs at low concentration levels (0.5-100 µg mL-1). The recovery range (n = 5) was 98.0-101.5%, and the relative standard deviation was no more than 5.0%.
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Anestésicos Generales , Anestésicos Locales , Concentración de Iones de Hidrógeno , Membranas Artificiales , Potenciometría/métodosRESUMEN
As an antibody-free sensing membrane for the detection of the antibiotic tetracycline (TC), a liquid PVC membrane doped with the ion-pair tetracycline/θ-shaped anion [3,3'-Co(1,2-C2B9H11)2]- ([o-COSAN]-) was formulated and deposited on a SWCNT modified gold microelectrode. The chosen transduction technique was electrochemical impedance spectroscopy (EIS). The PVC membrane was composed of: the tetracycline/[o-COSAN]- ion-pair, a plasticizer. A detection limit of 0.3 pg/L was obtained with this membrane, using bis(2-ethylhexyl) sebacate as a plasticizer. The sensitivity of detection of tetracycline was five times higher than that of oxytetracycline and of terramycin, and 22 times higher than that of demeclocycline. A shelf-life of the prepared sensor was more than six months and was used for detection in spiked honey samples. These results open the way to having continuous monitoring sensors with a high detection capacity, are easy to clean, avoid the use of antibodies, and produce a direct measurement.
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Oxitetraciclina , Plastificantes , Tetraciclina , Antibacterianos , Microelectrodos , AnticuerposRESUMEN
The developed spectrofluorimetric method was successfully applied to the analysis of brigatinib (BRG) in its bulk powder form, and human urine sample. It is based on the investigation of the fluorescence spectrum behavior of the BRG-eosin Y complex. The relative fluorescence intensity (RFI) was recorded at 560 nm after excitation at 480 nm. The principle of the proposed method was thoroughly explained. All experimental parameters affecting method development were optimized. Moreover, the obtained results were fully discussed and statistically analyzed. The molar ratio method was applied to study the stoichiometric relationship between BRG and eosin Y complex. The method revealed a ratio of 1:3 for BRG-eosin Y afforded the highest RFI. The developed method was validated over the concentration range of 62.5-4000 ng mL-1. The results were compared positively with the reported method.
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Compuestos Organofosforados , Eosina Amarillenta-(YS) , Humanos , Concentración de Iones de Hidrógeno , Polvos , Pirimidinas , Espectrometría de FluorescenciaRESUMEN
OBJECTIVES: The present study aims to develop and validate four simple, sensitive, reproducible, and low-cost spectrophotometric methods for the determination of antimigraine drug (eletriptan hydrobromide) in pure form and pharmaceutical formulations. METHODS: The methods are based on the formation of yellow colored ion-pair complex between eletriptan hydrobromide and four acid dyes, namely, bromocresol purple (BCP), bromocresol green (BCG), bromophenol blue (BPB), and bromothymol blue (BTB) with absorption maxima at 410, 420, 414 and 416nm, respectively. Several parameters such as pH, buffer type and volume, reagent volume, sequence of addition and effect of extracting solvent were optimized. RESULTS: Under the optimum experimental conditions, beer's law is obeyed over the concentration ranges of 1.0-20 and 1.0-16µgmL-1 for (BCP or BCG) and (BPB or BTB), respectively with good correlation coefficients (0.9995-0.9999). The apparent molar absorptivity and Sandell's sensitivity values are reported for all methods. The limit of detection (LOD) and the limit of quantification (LOQ) values are found to be 0.27, 0.28, 0.25, and 0.30µgmL-1 and 0.90, 0.93, 0.83, and 1.0µgmL-1 for BCP, BCG, BPB and BTB, respectively. The stoichiometric ratio of the formed ion-pair complexes was found to be 1:1 (drug: reagent) for all methods. CONCLUSION: The developed methods were successfully applied for the determination of eletriptan hydrobromide in pharmaceutical formulations with good accuracy and precision. Statistical comparison of the results was performed using Student's t-test and variance ratio F-test at the 95% confidence level and there was no significant difference between the reported and proposed methods regarding accuracy and precision. Further, the validity of the proposed methods was confirmed by recovery studies via standard addition method.
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Azul de Bromofenol , Preparaciones Farmacéuticas , Composición de Medicamentos , Humanos , Pirrolidinas , Espectrofotometría , TriptaminasRESUMEN
OBJECTIVES: The present work aims to develop and validate a simple, rapid, cost-effective, sensitive and extractive spectrophotometric methods for the determination of phosphodiesterase type 5-inhibitor; vardenafil HCl (VARD) in pure and in dosage forms. METHODS: The developed methods are based on the formation of ion-pair complexes between vardenafil HCl and dyes, namely, bromocresol green (BCG), bromocresol purple (BCP), bromophenol blue (BPB), bromothymol blue (BTB) and eriochrom black T (EBT) in acidic buffer solutions. Different factors affecting the reactions between VARD and the dyes were studied and optimized. RESULTS: The formed complexes were extracted with methylene chloride and measured at 418, 410, 415, 417 and 520nm using BCG, BCP, BPB, BTB and EBT, respectively. The beer's law was obeyed in the ranges 1.0-10, 1.0-16, 0.5-8.0, 2.0-20 and 1.0-14µgmL-1 for BCG, BCP, BPB, BTB and EBT, respectively under the optimum conditions. The composition of the ion-pairs was found 1:1. The molar absorptivity's, Sandell's sensitivity, limits of detection and the limits of quantification were calculated. Other method validation parameters, such as accuracy, intra-day and inter-day precision, robustness, ruggedness and selectivity, have been evaluated. CONCLUSION: The proposed methods have been applied successfully for the analysis of vardenafil HCl in pure and dosage forms. The reliability of the methods was further ascertained by performing recovery studies using the standard addition method. Statistical comparison of the results with the reported method was performed by applying student's t- and F-tests and no significant statistical differences were obtained.
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Inhibidores de Fosfodiesterasa 5/análisis , Diclorhidrato de Vardenafil/análisis , Colorantes , Formas de Dosificación , Composición de Medicamentos , Indicadores y Reactivos , Inhibidores de Fosfodiesterasa 5/administración & dosificación , Estándares de Referencia , Reproducibilidad de los Resultados , Sensibilidad y Especificidad , Soluciones , Espectrofotometría Ultravioleta , Comprimidos , Diclorhidrato de Vardenafil/administración & dosificaciónRESUMEN
Three rapid spectrophotometric methods were developed for the determination of sunitinib based on the formation of ion-pair complex in acidic medium with bromocresol purple, bromothymol blue, and bromophenol blue. The formed ion-pair complexes, extractable with chloroform, were measured at 422 nm for bromocresol purple, 425 nm for bromothymol blue and 427 nm for bromophenol blue. All these methods were optimized for the pH of buffer and the volume of the reagent. The methods were linear over the range of 1-200 µg/mL for bromocresol purple, 1-150 µg/mL for bromothymol blue, and 2-200 µg/mL for bromophenol blue with a very low limit of quantification and acceptable accuracy and precision. Using the proposed methods for determination of sunitinib in pharmaceutical dosage forms showed reliable results comparable to previously published method.
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BACKGROUND AND AIM: Since the pharmacological effects of diclofenac (DF) are short-lived because of its short half-life, prolongation of the pharmacological effect in a topical formulation is needed for more appropriate clinical use. For the enhancement of dermal accumulation and prolongation of the pharmacological effect of drugs, the aim of this study was to develop a simple gel formulation containing an ion-pair complex of DF and phenylephrine (PHE), which induce constriction of the vascular smooth muscles. MATERIALS AND METHODS: The ion-pair complex was prepared by mixing sodium DF and an ethanolic solution of PHE. The formed complex was characterized by powder X-ray diffraction (PXRD) and Fourier-transform infrared (FT-IR) spectroscopy. The ion-pair complex for the gel formulation was prepared by mixing an equimolar concentration of 50% 1,3-butylene glycol and distilled aqueous solution of 2% xanthan gum, which was characterized by proton nuclear magnetic resonance (1H-NMR). Skin permeation and accumulation of DF and PHE were evaluated by in vitro and in vivo studies. RESULTS: From the results of PXRD and FT-IR, it was suggested that new crystalline peaks formed by the ion-pair complex and their complex interacted with the carboxyl group in DF and the amino group in PHE. In the gel formulation, the ion-pair complexes were detected by 1H-NMR. The ion-pair complex enhanced the accumulation of DF in the skin in the in vitro study. On the other hand, PHE accumulation in the dermis increased with the ion-pair complex, as exhibited by the in vivo study. CONCLUSION: A new gel formulation containing the ion-pair complex of DF and PHE was developed, which improved the accumulation of DF in skin.
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Antiinflamatorios no Esteroideos/administración & dosificación , Diclofenaco/administración & dosificación , Portadores de Fármacos/administración & dosificación , Fenilefrina/administración & dosificación , Vasoconstrictores/administración & dosificación , Administración Cutánea , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/farmacocinética , Diclofenaco/química , Diclofenaco/farmacocinética , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Femenino , Geles , Técnicas In Vitro , Masculino , Fenilefrina/química , Fenilefrina/farmacocinética , Difracción de Polvo , Espectroscopía de Protones por Resonancia Magnética , Ratas Wistar , Piel/metabolismo , Absorción Cutánea/efectos de los fármacos , Espectroscopía Infrarroja por Transformada de Fourier , Porcinos , Porcinos Enanos , Vasoconstrictores/química , Vasoconstrictores/farmacocinética , Difracción de Rayos XRESUMEN
Sustained pulmonary delivery of tobramycin from microparticles composed of drug/polymer nanocomplexes offers several advantages against traditional delivery methods. Namely, in patients with cystic fibrosis, microparticle delivery can protect the tobramycin being delivered from strong mucoadhesive interactions, thus avoiding effects on its diffusion toward the infection site. Polymeric ion-pair complexes were obtained starting from two synthetic polyanions, through impregnation of their solid dissociated forms with tobramycin in aqueous solution. The structure of these polymeric systems was characterized, and their activities were examined against various biofilm-forming Pseudomonas aeruginosa. Once dried, the nanocomplexes can change their aggregation state, to form microparticle-based aggregates with a spherical shape and a micrometer size. In aqueous dispersions, the ion-pair complexes produced had nanometric size, negative ζ potential, and high biocompatibility toward human bronchial epithelium cells. The antibiofilm activity of these formulations was more efficient than for free tobramycin, with the antibiofilm activity against P. aeruginosa mucoid and nonmucoid end-stage strains isolated from cystic fibrosis lungs being of particular relevance.
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Antibacterianos/administración & dosificación , Fibrosis Quística/tratamiento farmacológico , Portadores de Fármacos/administración & dosificación , Nanopartículas/administración & dosificación , Péptidos/administración & dosificación , Infecciones por Pseudomonas/tratamiento farmacológico , Tobramicina/administración & dosificación , Biopelículas , Línea Celular , Humanos , Moco/metabolismo , Pseudomonas aeruginosa/efectos de los fármacos , Pseudomonas aeruginosa/fisiologíaRESUMEN
We report on the structures of Li-ion complexes in salt-concentrated aqueous electrolytes based on lithium bis(trifluoromethanesulfonyl)amide (LiTFSA), particularly focusing on the anion coordination behavior of the ion-pair complexes in the high concentration region cLi > 3.0 mol dm-3. Quantitative data analysis of the Raman spectra revealed the following. (1) Li ions do not coordinate with TFSA anions at lower cLi (<3.0 mol dm-3) to exist as ion pair-free ions. (2) In the concentrated region (cLi = 3.0 - 4.0 mol dm-3), the TFSA anions coordinate as monodentate ligands (mono-TFSA) with Li ions to form ion-pair complexes and coexist with free TFSA in the bulk. (3) Further increasing the cLi (4.0 - 5.2 mol dm-3) results in both monodentate and bidentate coordination (bi-TFSA) modes of TFSA anions to Li ions, yielding complicated ion-pair complexes in the first coordination sphere. The Walden plots, based on ionic conductivity and viscosity data, implied that the ion-conducting mechanism in the highly salt-concentrated region was considerably different from that in the dilute region (i.e., vehicle mechanism).
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Though ion-pair strategy has been widely used in transdermal drug delivery system, knowledge about the molecular mechanisms involved in the skin permeation processes of ion-pair complexes is still limited. In the present study, a homologous series of fatty acids were chosen to form model ion-pair complexes with bisoprolol (BSP) to rule out the influence of functional groups on polar surface area, stability and other physicochemical properties of ion-pair complexes. The ion-pair complexes were characterized by FTIR, thermal analysis, and 1H NMR. The skin permeability of BSP as well as its ion-pair complexes was investigated by in vitro skin permeation experiments then visualized by CLSM. The skin permeability coefficient (kp) of BSP ion-pair complex was negatively related to its n-octanol/water apparent partition coefficient (P'o/w) in the hydrophobic vehicle caprylic/capric triglyceride, (log kp=-1.657-1.229 log P'o/w), suggesting that the instability of ion-pair complexes due to their dissociation in the viable epidermis (VED) played an important role in controlling the skin permeability of BSP, which was further proved by 1H NMR and molecular docking. These findings broadened our understanding about the molecular mechanisms involved in the skin permeation processes of ion-pair complexes.
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Antihipertensivos/administración & dosificación , Bisoprolol/administración & dosificación , Ácidos Grasos/administración & dosificación , Administración Cutánea , Animales , Antihipertensivos/química , Antihipertensivos/farmacocinética , Bisoprolol/química , Bisoprolol/farmacocinética , Ácidos Grasos/química , Ácidos Grasos/farmacocinética , Masculino , Microscopía Confocal , Simulación del Acoplamiento Molecular , Ratas Wistar , Piel/metabolismo , Absorción Cutánea/efectos de los fármacos , Solubilidad , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
In order to achieve high drug loading and high entrapment efficiency, a doxorubicin-cholesteryl hemisuccinate ion-pair complex (DCHIP) was formed, and the ion-pair complex liposomes (DCHIP-Lip) were prepared based on conventional thin-film dispersion method. Firstly, DCHIP was fabricated and confirmed with FTIR, 1H-NMR, DSC, and XRD techniques. Afterwards, DCHIP-Lip were prepared and evaluated in terms of particle size, zeta potential, entrapment efficiency, and drug loading content. Finally, the in vitro and in vivo behavior of liposomes was further investigated. The DCHIP-Lip had a nanoscale particle size of about 120 nm with a negative zeta potential of about -22 mV. In addition, the entrapment efficiency and drug loading content of DOX reached 6.4 ± 0.05 and 99.29 ± 0.3%, respectively. Importantly, the release of DCHIP-Lip was pH sensitive and increased cell toxicity against MCF-7 cells was achieved. Upon dilution, the liposomes were fairly stable under physiological conditions. The in vivo pharmacokinetic study indicated that the AUC of DOX in DCHIP-Lip was 11.48-fold higher than that of DOX-HCl solution and the in vivo antitumor activity of DCHIP-Lip showed less body weight loss and a significant prohibition effect of tumor growth. Based on these findings, it can be seen that the ion-pairing technology combined with conventional liposome drug loading method could be used to achieve high drug loading and it could be valuable for the study of liposomal delivery system.
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Ésteres del Colesterol/farmacología , Doxorrubicina/análogos & derivados , Sistemas de Liberación de Medicamentos/métodos , Liposomas , Animales , Antibióticos Antineoplásicos/administración & dosificación , Antibióticos Antineoplásicos/farmacología , Ésteres del Colesterol/administración & dosificación , Doxorrubicina/administración & dosificación , Doxorrubicina/farmacología , Combinación de Medicamentos , Humanos , Liposomas/química , Liposomas/farmacología , Células MCF-7/efectos de los fármacos , Células MCF-7/fisiología , Fusión de Membrana/efectos de los fármacos , Tamaño de la Partícula , Polietilenglicoles/administración & dosificación , Polietilenglicoles/farmacologíaRESUMEN
Nerve Growth Factor (NGF) is one of the members of the neurotrophin family with multifaceted functions. However, clinical application of NGF is hurdled by the challenge on formulation development. The objective of this study was to develop novel high-density lipoproteins (HDL)-mimicking nanoparticles (NPs) coated with α-tocopherol to incorporate NGF by a self-assembly approach. The NPs were prepared by an optimized self-assembly method that is simple and scalable. The composition of HDL-mimicking NPs was optimized. The prototype of the HDL-mimicking α-tocopherol-coated NPs contained phosphatidylserine (a negative charged phospholipid) and d-α-Tocopheryl polyethylene glycol succinate (a source of vitamin E) to enhance the entrapment efficiency of apolipoprotein A-I in the NPs. The entrapment efficiency of apolipoprotein A-I was about 30%. The NPs had particle size about 200nm with a relatively narrow size distribution. Finally, cationic ion-pair agents were optimized to form ion-pairs with NGF to facilitate the incorporation of NGF into the NPs. Protamine sodium salt USP formed an optimal ion-pair complex with NGF. The results showed that the novel HDL-mimicking α-tocopherol-coated NPs successfully encapsulated NGF with over 65% entrapment efficiency by using this ion-pair strategy. In vitro release studies demonstrated a slow release of NGF from NGF NPs in PBS containing 5% BSA at 37°C for 72 h. Further biodistribution studies showed that intravenously injected NGF NPs significantly increased NGF concentration in plasma and decreased the uptake in liver, spleen and kidney, compared to free NGF in mice.
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Lipoproteínas HDL/química , Nanopartículas/química , Factor de Crecimiento Nervioso/química , alfa-Tocoferol/química , Animales , Apolipoproteína A-I/química , Cationes , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Iones , Masculino , Ratones , Tamaño de la Partícula , Fosfatidilserinas/química , Fosfolípidos/química , Protaminas/química , Temperatura , Distribución Tisular , Vitamina E/químicaRESUMEN
Cefixime trihydrate is a broad spectrum cephalosporin antibiotic, effective against gram-positive and gram-negative bacterial infections. Simple and rapid method has been developed for the determination of cefixime trihydrate in bulk and pharmaceutical formulations. This method was based on the formation of bluish-green ion-pair complex of cefixime trihydrate with bromophenol blue in dimethyl sulfoxide (DMSO)-acetonitrile medium. Different parameters were studied and optimized. A 2:1 complex was formed between the drug and reagent almost instantaneously at room temperature which has λmax of 610 nm. Under optimum conditions, calibration curve was found to be linear over the range of 10-130 µg mL(-1). The method was subjected to analytical quality control. The limit of detection was found to be 1.08 µg mL(-1). Recovery studies and interference studies were carried out. The proposed method was successfully applied to the determination of cefixime trihydrate in bulk and pharmaceutical formulations with high precision and accuracy.
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In this study a sensitive, simple and accurate spectrophotometric method was suggested for determination of tamsulosin in bulk powder and pharmaceutical dosage form based on the formation of an ion-pair complex between the drug and bromocresol green in a buffer solution at pH 3.5. The formed yellow color complex was extracted with chloroform and measured at 415 nm. The optimum reaction conditions such as pH, reagent amount, extracting solvent and the stoichiometry of the ion-pair complex were investigated. Under the optimized conditions, the Beer's law was obeyed in the concentration range of 1-160 g/mL with acceptable correlation coefficient (r(2) > 0.9997) and precision (CV < 3%) and accuracy (error < 2%). The proposed method was successfully used for the determination of tamsulosin in pharmaceutical capsule with nosignificant interferences of excipients.
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PURPOSE: Ambrisentan (ABS) is an antihypertensive drug used in the treatment of pulmonary atrial hypertension. The survey of literature for ABS revealed only two spectrophotometric methods for its quantification. The reported methods lack the sensitivity. This study is aimed at developing two sensitive extractive spectrophotometric methods for the determination of ABS in bulk and in tablets. METHODS: The proposed methods are based on the formation of colored chloroform extractable ion-pair complexes of ABS with methylene blue (MB method) and safranine O (SO method) in buffered solution at pH 9.8. The extracted complexes showed maximum absorbance at 525 and 515 nm for methylene blue and safranine O, respectively. RESULTS: In both the methods, the calibration curve was linear from 1-15 µg mL(-1) of drug. Apparent molar absorpitivities were 1.7911 x 10(5), 2.3272 x 10(5) L mol(-1) cm(-1); Sandell's sensitivities were 0.0215, 0.0162 µg cm(-2); LOD were 0.182, 0.175 µg mL(-1); LOQ were 0.551, 0.531 µg mL(-1) for methods MB and SO, respectively. The relative standard deviation and percent recovery ranged from 0.206-1.310% and 99.0-101.5%, respectively. CONCLUSION: The results demonstrate that the proposed methods are sensitive, precise, accurate and inexpensive. These methods can easily be used for the assay of ABS in quality control laboratories.
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BACKGROUND: Vincristine (VCR), which is a widely used antineoplastic drug, was integrated with a submicron-emulsion drug-delivery system to enhance the anticancer effect. METHODS: After the formation of a VCR-oleic acid ion-pair complex (VCR-OA), the VCR-OA-loaded submicron emulsion (VCR-OA-SME), prepared by classical high-pressure homogenization, was characterized and its in vitro anticancer effects were evaluated. RESULTS: The submicron-emulsion formulation exhibited a homogeneous round shape. The mean particle size, zeta potential, and encapsulation efficiency were 157.6 ± 12.6 nm, -26.5 ± 5.0 mV and 78.64% ± 3.44%, respectively. An in vitro release study of the VCR-OA-SME revealed that 12.4% of the VCR was released within the first 2 hours (initial burst-release phase) and the rest of the drug was detected in the subsequent sustained-release phase. Compared with VCR solution, the pharmacokinetic study of VCR-OA-SME showed relatively longer mean residence time (mean residence time [0-∞] increased from 187.19 to 227.56 minutes), higher maximum concentration (from 252.13 ng/mL to 533.34 ng/mL), and greater area under the curve (area under the curve [0-∞] from 11,417.77 µg/L/minute to 17,164.34 µg/L/minute. Moreover, the VCR-OA-SME exhibited higher cytotoxicity (P < 0.05) on tumor cells by inducing cell arrest in the G2/M phase or even apoptosis (P < 0.05). CONCLUSION: The VCR-OA-SME formulation in our study displayed great potential for an anticancer effect for VCR.