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This study found 0.7% olopatadine (Pataday Once Daily Relief Extra Strength) eye drops to provide better initial comfort than 0.3% pheniramine maleate/0.025% naphazoline hydrochloride (VISINE® Allergy Eye Relief Multi-Action Antihistamine and Redness Reliever) eye drops suggesting that patients may comply better with the Pataday than VISINE. To compare the ocular comfort at instillation of Pataday and VISINE allergy eye drops. Minimally symptomatic participants were recruited based upon Standard Patient Evaluation of Eye Dryness (SPEED) questionnaire scores (≤3 units); they also had minimal between-eye inter-ocular comfort differences as judged by visual analogue scale scores (VAS; ≤7 units). Baseline comfort was evaluated by eye with a VAS. One drop of Pataday or VISINE was then applied to the right eye with the alternative drop being applied to the left eye. The same VAS evaluated comfort by eye at drop instillation, and then at 30 seconds, 1 minute, and 2 minutes post-instillation. Drop experience was also evaluated with Likert questions. LogMAR visual acuities and bulbar conjunctival redness were evaluated pre- and post-drop instillation. A total of 159 participants were recruited (mean ± SD age = 26.2 ± 7.5). The VAS found that eyes treated with Pataday were significantly more comfortable at instillation than eyes treated with VISINE. Likert questions indicated that participants significantly preferred Pataday drops compared to the VISINE drops at instillation with regards to overall eye comfort, eye stinging, eye burning, and foreign body sensation. There were no between drop differences in visual acuity, though eyes treated with VISINE were less red than eyes treated with Pataday. Topically applied Pataday drops were more comfortable than VISINE drops. [ABSTRACT FROM AUTHOR]

A first order derivative UV-spectrophotometric method was developed to quantify naphazoline hydrochloride and phenylephrine hydrochloride in eye drops. Naphazoline hydrochloride and phenylephrine hydrochloride were estimated at 275.6nm (zero crossover point of phenylephrine hydrochloride) and 289.4nm (zero crossover point of naphazoline hydrochloride), respectively. The method was found to be linear in the concentration range of 10 - 25 µg/mL for naphazoline hydrochloride and 20 - 60 µg/mL for phenylephrine hydrochloride. The developed method was subjected to validation in accordance with ICH guidelines Q2(R1) for different validation parameters. The analytical method developed was found to be accurate and cost - effective and can be used for routine analysis of naphazoline hydrochloride and phenylephrine hydrochloride in eye drops. [ABSTRACT FROM AUTHOR]

• Hirshfeld surface analysis of NPZ was discussed. • The structural characteristics of dominant facets were analyzed. • The crystal morphologies of NPZ in different binary solvents were predicted by the MAE model. • Predicted crystal habits were compared with the experimental shapes. • Intermolecular interactions of solvent and crystal facets were revealed by molecular simulation. The crystal morphologies of naphazoline hydrochloride (NPZ) in vacuum and binary solvent conditions (methanol + ethyl acetate, methanol + ethanol, methanol + isopropanol and 2-moxyethanol + isopropanol) were investigated by the molecular dynamic (MD) simulation and experiments. The Hirshfeld surface (HS) analysis was employed to explore the interactions in the crystal structure of NPZ, and results revealed that H···H and H···Cl/Cl···H contacts were primary contributing interactions. The attachment energy (AE) model was utilized to simulate the crystal habit of NPZ in vacuum based on the single crystal data, resulting in the identification of six morphological crystal facets. Also, the structural characteristics of dominant crystal faces were analyzed. The crystal morphologies of NPZ in different binary solvents were predicted using the modified attachment energy (MAE) model. The simulation results indicated that the solvent adsorption processes on the crystal surfaces were exothermic, and {0 0 2} face had largest morphological importance in all solvent systems. Furthermore, the experimental morphology of NPZ obtained from the methanol + ethyl acetate system was consistent with the crystal habit predicted by MAE model, which was plate-shape. On this basis, the intermolecular interactions between solvent molecules and {0 0 2} as well as {1 1––1} facets were analyzed detailly by radial distribution function (RDF) and mean square displacement (MSD), respectively. The RDF analysis indicated that N atoms of {0 0 2} face formed hydrogen bonds with O atoms of solvent molecules, resulting in an evident change in the total facet area of this face. Moreover, MSD analysis demonstrated that the absorptions of solvent molecules on the {1 1––1} face were the main factor affecting the growth rate of this crystal surface. [ABSTRACT FROM AUTHOR]

The aim of the current study was to investigate whether olopatadine and naphazoline hydrochloride reduce allergic conjunctivitis in mice through alterations in inflammation, NGF and VEGF. An allergic conjunctivitis mouse model was established using histamine or an antigen (ovalbumin), following which mice were treated with 1% olopatadine solution and/or 0.2 mg/ml of naphazoline hydrochloride. Histamine or antigen-induced conjunctival vascular hyperpermeability was examined and the levels ofinflammatory factors, cytokines, IgE, GMCSF and NGF were analyzed using ELISA in antigen-induced conjunctival vascular hyperpermeability mice. In addition, VEGF protein expression was measured using western blotting in antigen-induced mice. The results indicated that olopatadine and naphazoline hydrochloride significantly suppressed conjunctival dye leakage in mice with histamine or antigen-induced conjunctival vascular hyperpermeability. In addition, treatment with olopatadine and naphazoline hydrochloride was able to reduce the levels ofinflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF in antigen-induced conjunctival vascular hyperpermeability mice. The protein expression levels of VEGF in antigen-induced conjunctival vascular hyperpermeability mice were reduced following treatment with olopatadine and naphazoline hydrochloride. These results suggest that treatment with olopatadine and naphazoline hydrochloride reduces conjunctivitis in mice via effects on inflammation, NGF and VEGF. [ABSTRACT FROM AUTHOR]

Background A simple, rapid, and accurate stability-indicating reverse phase liquid chromatographic method was developed and validated for the simultaneous determination of pheniramine maleate and naphazoline hydrochloride in bulk drugs and pharmaceutical formulations. Results Optimum chromatographic separations among pheniramine maleate, naphazoline hydrochloride and stress-induced degradation products have been achieved within 10 minutes by using an Agilent zorbax eclipse XDB C18 column (150 mm × 4.6 mm, 5 μm) as the stationary phase with a mobile phase consisted of 10 mM phosphate buffer pH 2.8 containing 0.5% triethlamine and methanol (68:32, v/v) at a flow rate of 1 mL min-1. Detection was performed at 280 nm using a diode array detector. Theoretical plates for pheniramine maleate and naphazoline hydrochloride were calculated to be 6762 and 6475, respectively. The method was validated in accordance with ICH guidelines with respect to linearity, accuracy, precision, robustness, specificity, limit of detection and quantitation. Regression analysis showed good correlations (R2 > 0.999) for pheniramine maleate in the concentration range of 150-1200 μg mL-1 and naphazoline hydrochloride in 12.5-100 μg mL-1. The method results in excellent separation of both the analytes and degradation products. The peak purity factor is ⩽980 for both analytes after all types of stress, indicating complete separation of both analyte peaks from the stress induced degradation products. Conclusions Overall, the proposed stability-indicating method was suitable for routine quality control and drug analysis of pheniramine maleate and naphazoline hydrochloride in pharmaceutical formulations. [ABSTRACT FROM AUTHOR]

A simple, fast, and low-cost method was developed and validated for the separation and determination of neostigmine metilsulfate (Neo), naphazoline hydrochloride (Nap), chlorphenamine maleate (Chl), pyridoxine hydrochloride (Pyr), and dipotassium glycyrrhizinate (Dip) by capillary electrophoresis (CE) for the first time. The separation was achieved in 7 min with 10 mM borate of pH 10.0, ultraviolet detection at 205 nm, and 25 kV applied voltage. The proposed method demonstrates good linearity with r2between 0.9995 and 0.9998. The repeatability was in the range of 0.23–1.96% with migration time and 0.81–3.46% with peak area for the five components. The limits of detection were 0.10, 0.02, 0.08, 0.17, and 2.44 µg mL−1for Neo, Nap, Chl, Pyr, and Dip, respectively. The method was successfully applied to the quantitation of the five components in a commercial eye drops with recoveries in the range of 99.01–101.26%. Furthermore, a comparison of the results obtained by CE was made with those obtained by high-performance liquid chromatography (HPLC) described in Chinese Pharmacopoeia. The performance of the proposed method was comparable, and the quantitative results were in good agreement with those by HPLC, while the CE method has the advantages of shorter analysis time and lower cost than HPLC. [ABSTRACT FROM AUTHOR]

Abstract: The fluorescence and ultraviolet spectroscopy were explored to study the interaction between Naphazoline hydrochloride (Naphcon) and bovine serum albumin (BSA) at three different temperatures (292, 301, and 310K) under imitated physiological conditions. The quenching mechanism of BSA by Naphacon was interpreted using the Stern–Volmer mechanism, and a combined quenching (dynamic and static quenching). The binding constants, binding sites and the corresponding thermodynamic parameters (ΔG, ΔH, and ΔS) of the interaction system were calculated at different temperatures. According to Förster non-radiation energy transfer theory, the binding distance between BSA and Naphcon was found to be 4.71nm. Synchronous fluorescence spectroscopy showed the conformation of BSA changed in the presence of Naphacon. In addition, the effect of some common metal ions (Mg2+, Ca2+, Ni2+, Cu2+, and Fe2+) on the binding constant between Naphcon and BSA was examined. [Copyright &y& Elsevier]

Abstract: New naphazoline (NPZ) ion selective membrane electrodes of both conventional and coated graphite types were prepared based on the ion-pair of naphazoline tetraphenylborate (NPZ–TPB). The conventional type electrode was fully characterized in terms of membrane composition, life span, pH, ionic strength and temperature. The electrode exhibited a Nernstian response for naphazoline in the concentration range 1.0×10−5 to 5.0×10−2 and 5.0×10−6 to 5.0×10−2 M with a slope of 58.4±1.1 and 57.0±0.1mV/concentration decade and a limit of detection of 4.0×10−6 and 2.5×10−6 M for conventional and coated graphite types, respectively. It could be used in the pH range 3.0–8.0. It was applied to potentiometric determination of naphazoline in pure state and pharmaceutical preparation under batch conditions. The selectivity of the electrode toward a large number of inorganic cations, sugars and amino acids was tested. The solubility product of the ion-pair and the formation constant of the precipitation reaction leading to the ion-pair formation were determined conductometrically. [Copyright &y& Elsevier]

The new PdII complex using Naphcon as ligand, was synthesized and characterized. DNA and BSA interactions of Naphcon and its PdII complex were investigated by several spectroscopic methods. Theoretical investigation of DNA/BSA interaction was done by molecular docking simulation. Also, Nuclease and protease cleavage ability were assessed by gel electrophoresis. Investigation of cytotoxicity of compounds on two cancer cell lines including MCF-7 and HeLa, confirmed anticancer potential of the PdII complex. [Display omitted] Throughout this study, a new palladium (II) complex, trans -[Pd(Naph) 2 Cl 2 ], with naphazoline hydrochloride (Naphcon) as an imidazole derivative, 2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole;hydrochloride, was synthesized and characterized by elemental analysis, spectroscopic methods (UV–Vis, IR, and 1H NMR) and single crystal X-ray structure analysis. The cytotoxicity of Naphcon and the PdII complex were investigated in vitro against human breast (MCF-7) and cervical epithelial carcinoma (HeLa) cancer cells. The results revealed the higher anticancer activity of complex rather that of Naphcon against MCF-7 cell line. The findings of in vitro studies including fluorescence and UV–Vis spectroscopy, circular dichroism (CD), thermal denaturation and viscosity measurement indicated the interaction of the PdII complex with calf-thymus DNA (CT-DNA) via a combination of covalent and non-covalent interactions, whereas the free Naphcon interacted with CT-DNA mainly through the groove binding mode. Moreover, the ability of Naphcon and the PdII complex to cleave pUC57 plasmid DNA was investigated. In addition, the interaction of both Naphcon and its PdII complex was explored with bovine serum albumin (BSA) by means of absorption and fluorescence spectroscopy. The binding constant (K b) could be calculated for compounds through these spectroscopic methods. Based on the competitive binding studies using Eosin, Ibuprofen and Digoxin as site markers, the binding site of the PdII complex and Naphcon was found to be located on site-III and I of BSA, respectively. Furthermore, protease activity of compounds was examined under physiological conditions. Finally, to validate all data obtained from biophysical studies, the molecular docking simulation was employed as a computational method. [ABSTRACT FROM AUTHOR]

The purpose of this work was to measure the equilibrium solubility of naphazoline hydrochloride (NPZ) in different mono-solvents ranged from 278.15 K to 323.15 K by a laser monitoring method. In this research, N -methyl pyrrolidone (NMP), n -propanol, 2-butoxyethanol, ethanol, 2-methoxyethanol, N , N -dimethylformamide (DMF), methanol, ethylene glycol (EG), isopropanol, 2-propoxyethanol and 2-ethoxyethanol were selected as the experimental solvents. The results indicated that solubility data of NPZ in 11 neat solvents increased with the increase of temperature. At 298.15 K, the maximum solubility was observed in EG (5.028e-2), followed by 2-methoxyethanol (2.460e-2), methanol (2.429e-2), 2-ethoxyethanol (7.788e-3), ethanol (6.391e-3), 2-propoxyethanol (4.216e-3), n -propanol (3.373e-3), 2-butoxyethanol (3.144e-3), DMF (2.348e-3), NMP (2.002e-3) and isopropanol (1.689e-3). Moreover, the solvent polarity, radial distribution function (RDF) and solvent effect (KAT-LSER model) were implemented to investigate the impact of solute-solvent interactions on solubility behavior of NPZ. The results demonstrated that the whole dissolution behavior of NPZ in organic solvents was a complicated process, and the solvent-solute interactions were associated with hydrogen bond acidity and dipolarity/polarizability of solvent. Besides, the NRTL-SAC, Two-Suffix Margules, Wilson, NRTL and UNIQUAC models were employed to fit experimental solubility data. Deviation analysis revealed that the Wilson model reflected the best agreement between measured data and calculated values with the minimum mean values of average relative deviation (100ARD, 0.9144) and root-mean square deviation (104RMSD, 1.062). Furthermore, the positive entropy changes and negative values of Gibbs energy changes showed that mixing and dissolution process of NPZ in 11 neat solvents were confirmed to entropy-driven and spontaneous. • The solubility of NPZ was studied in eleven neat solvents. • Molecular dynamic simulation and KAT-LSER model were implemented to investigate the solute-solvent interactions. • Five thermodynamic models were used to fit experimental solubility data. • Thermodynamic properties of NPZ were calculated and discussed. [ABSTRACT FROM AUTHOR]

Laser monitoring technique was used for the determination of solid-liquid equilibrium solubility of naphazoline hydrochloride (NPZ) in four binary solvents (methanol + ethanol, methanol + isopropanol, 2-methoxyethanol + isopropanol and methanol + ethyl acetate) at T = (278.15–323.15) K and pressure p = 0.1 MPa. In all cases, solubility of NPZ raised with the increment of temperature. The results also indicated that the addition of positive solvents (methanol or 2-methoxyethanol) on the solution of binary solvent mixtures led to increasing solubility of NPZ in all studied binary solvents. The solute-solvent interaction and solvent-solvent interaction were investigated using radial distribution function (RDF). The RDF results revealed that the change of solvent composition varied as the solute-solvent interplay and solvent-solvent interaction, thereby causing the difference of NPZ solubility. Additionally, the measured data was successfully correlated with the Margules, NRTL and UNIQUAC model to investigate theoretically the solubility of NPZ. Computational results proved that the lower mean values of average relative deviation (100 ARD) and root-mean square deviation (104 RMSD) were obtained to be (1.675) and (2.338) for calculating the solubility of NPZ in investigated systems, further implying that the UNIQUAC model reflected the most accurate descriptions. Using the experimental solubility data, the changes of thermodynamic properties as enthalpy (Δ mix H and Δ dis H), entropy (Δ mix S and Δ dis S) and Gibbs free energy (Δ mix G and Δ dis G) of mixing and dissolution processes were calculated to investigate the solvation behavior of NPZ in studied systems. It was concluded from positive values of entropy and negative values of Gibbs energy change that the mixing and dissolution processes of NPZ in all studied mixed solvents were entropy-driven and spontaneous. • Solubility of naphazoline hydrochloride in four binary solvents was measured. • Solubility values were fitted with NRTL, Margules and UNIQUAC models. • Molecular simulations were provided to explain the solubility behavior in (methanol + ethyl acetate) system. • Thermodynamic properties were calculated by UNIQUAC model. [ABSTRACT FROM AUTHOR]

The article presents a case study of an 89-year-old male patient who developed eczema after he repeatedly use an over-the-counter antiseptics. The antiseptic that the patient used contained benzalkonium chloride, dibucaine, hydrocholoride, chlorpeheniramine maleate, and a mixture of fragrance ingredients. It discusses the dermatological aspects of three chemical substances which are relevant to the patient's allergenic contact dermatitis.