Formulation and Evaluation of Ketoconazole Nanosponge gel

Ketoconazole Nanosponges were prepared by using Hyper cross linked β-cyclodextrin method by using different concentration of cross-linker. Diphenyl carbonate was used as the cross linking polymer. Nanosponge formulations were prepared by using β-CD: cross linker ratios of 1:15, 1:10, 1:5 and 1:3.Thepreparednanosponges were evaluated for percentage yield, incorporation efficiency, particle size, drug polymer compatibility, scanning electron microscopy andin-vitrodrugrelease.SEM studies confirmed their porous structure with number of nano channels. The FTIR spectra showed stable character of Ketoconazole in mixture of polymers and revealed the absence of drug polymer interactions. DSC study revealed that drug was involved in complexation with nanosponges. The average particle size of Ketoconazole nanoparticles was found to be in the range of 78.81± 0.20 nm to336.02 ± 0.124nm.The drug release from nanosponges was found to extended upto 8hr. 82 to 92%.The nano sponges were formulated into gel using Carbopol 940Batches G1 to G4 were prepared by incorporating nanosponges equivalent to 6%w/w of ketoconazole in different polymer concentrations respectively and evaluated for Percent drug content, Viscosity study, Spreadability study, In vitro diffusion studies. Nanosponge gel G1 showed the optimum pH, viscosity, Spread ability and In vitro release. Drug diffusion from the nanosponge loaded gel formulations was show sustained rate. A sustained release topical drug delivery of Ketoconazole developed as a nanosponge loaded gel offers solubilizing matrix for the drug, served as a local depot for sustained drug release and provided a rate limiting matrix barrier for modulation of drug release.

Possible association of stroke with higher whole blood viscosity: study in a high altitude (Cusco 3399 masl)

Background. Risk factors for stroke have been extensively studied, however, few studies have been carried out in high-altitude cities. Objectives. To evaluate the difference in blood viscosity, using direct methods, in stroke patients versus patients without stroke to discover any possible association. Design and setting. A cross-sectional study was carried out in the city of Cusco, Peru (3399 m.a.s.l). Methods: Participants included stroke patients with less than three days of illness and controls without stroke. Viscosity levels were measured in all patients using a cone-plate viscometer. Blood viscosity was evaluated at 10, 20, 30 and 40 revolutions per minute (RPM) because blood is considered a nonNewtonian fluid. Plasma viscosity was evaluated at 100RPM. All viscosity units are expressed as means standard deviations (SD) in centipoises (cP). Results: A total of 204 patients were included (61 cases/143 controls). The mean age was 67.5 (SD:15.9), and 88 (43%) were women. The means of blood viscosity for 10, 20, 30RPM in the stroke cases were 5.85cP (SD:1.21), 5.22cP (SD:1.09), and 4.91cP (SD:1.02), and 4.81cP (SD:1.02) respectively. For the controls were of 5.57cP (SD:1.19), 4.89cP (SD:4.85), 4.63cP (SD:0.97), 4.56cP (SD:0.95), respectively. All measured means were tested with significant differences (p <0.01). Plasma viscosities were 1.43cP (SD:0.17) for the stroke cases and 1.49cP (SD:0.23) for controls (p=0.05). Conclusions: This study found that blood viscosity is 0.3cP higher in stroke patients. This suggests that blood viscosity could play a role in the etiology. The results presented are preliminary and the study is still under development.

Determination of solute-solute and solute-solvent interaction of pyrimidine5-carbonitrile in aqueous DMSO at 298.15 K.

Introduction: In this reported work, we have used 80 % aqueous dimethyl sulphoxide (DMSO) for density and viscosity measurement of pyrimidine-5-carbonitrile at 298.15 K. The obtained experimental results shows that as concentration increases density and viscosity increases. From the results of density and viscosity, we have found apparent molar volume, limiting apparent molar volume, semi-empirical parameters, Falkenhagen coefficients and Jones Dole coefficients. Method: The apparent molar volume and limiting apparent molar volume having negative values indicated electostrictive solvation of ions and weak or absence of ion solvent interactions respectively. Result & Discussion : Falkenhagen coefficients is independent of concentration having positive value has shown strong solute-solute interactions and Jones-Dole coefficients having negative value has shown weak solute-solvent interactions. The strong solute-solute interactions were presents in A-1 as compared to A-2 compound because high electronegativity of oxygen atom. These parameters had given idea about molecular interactions such as solute-solute, solute-solvent and solvent-solvent. Conclusion: We have reported density and viscosity study of 4-amino-2-hydroxy-6-phenylpyrimidine-5-carbonitrile and 4- amino-2-mercapto-6-phenylpyrimidine-5-carbonitrile in 80 % aqueous DMSO solution at 298.15 K temperature. It has been observed that Strong molecular association in A-2 as compared to A-1 due to negative values of Øv.

Therapeutic Efficacy of Moxifloxacin Mucoadhesive Hydrogel for Bacterial Keratitis

Bacterial keratitis is a hypothetically devastating corneal infection due to the opportunity of fast development; corneal devastation either to be completed in 24–48 hours with even more contagious bacterial aetiological agents. Moxifloxacin mucoadhesive Hydrogel was prepared by using polymer Hydroxy Propyl Methyl Cellulose E50 LV by hydration method. Moxifloxacin was dissolved in small quantity of water and Benzalkonium Chloride was added to the Polymer solution. The formulations were evaluated for clarity, pH measurement, spread-ability test, drug content estimation, viscosity study, in vitro diffusion study and antibacterial activity. The developed formulation exhibits the sustained release over a period of 10 hour. The optimized formulation was further evaluated with antimicrobial activity. The results of the in-vitro antimicrobial activity of hydrogel were satisfactory. Keywords: Corneal Infection, Hydrogel, Moxifloxacin, invitro release

Temperature dependences of surface tension, density and viscosity study of Sn-Ag-Cu with Bi additions using theoretical models

In this work, the kohler, Muggianu,Toop and Hillert geometric models were used to calculate the surface tension, molar volume and density of the liquid Sn-Ag-Cu-Bi quaternary alloys along three selected sections xSn:xAg:xCu = 1:1:1, 1:1:2 and 1:2:1 in the temperature range of 923 K–1423 K. The choice of this temperature range was made on the basis of the calculation results of the liquidus line of the alloys belonging to the three sections. The same properties have been estimated for five selected Sn2.7Ag0.86Cu3.86Bi, Sn3.13Ag0.48Cu4.02Bi, Sn2.95Ag0.53Cu6.81Bi, Sn2.68Ag1.01Cu6.62Bi and Sn3.24Ag0.75Cu1.76Bi quaternary alloys between 623 K and 1123 K for comparison with the available experimental data. Moreover, the surface tension and density of these five alloys have also been calculated on the basis of Guggenheim and theoretical equation, respectively. In addition, the Seetharaman-sichen and Kaptay equations were extended to estimate the viscosity of SAC + Bi alloys. We also discussed the influence of Bismuth addition in liquid Sn-Ag-Cu-Bi. Estimated values show that Bi increases molar volume and density but decreases the surface tension and viscosity. On the other hand, the surface tensions diminish with the temperature for the all studied models, with the exception of some concentration of Bismuth; an inverse tendency is observed (dσ/dT) > 0. While, the density diminishes with increasing temperature for all alloys (dσ/dT) < 0. These models have been shown to be a great alternative for calculating the thermo-physical properties of quaternary systems.

Тhe Viscosity Study of Naftifine Hydrochloride Solution with a Combination of Polyethylene Glycols

Introduction. Naftifin hydrochloride is an antifungal drug from the allylamine group, which is used as a drug for external use in the treatment of onychomycosis. Quickly penetrates the skin and nails. It has antifungal, antibacterial and anti-inflammatory effects. It has a wide range of actions against many fungi that cause onychomycosis (dermatophytes, molds and yeast). In addition, it has an antibacterial effect in the ratio of gram-positive and gram-negative bacteria, reduces the risk of complicated course of the disease. It has a pronounced anti-inflammatory effect. Polyethylene glycols belong to the class of organic polymers of ethylene glycol. Polyethylene glycols are safe and widely used in pharmaceutical production, due to the variety of applications. The object of the study is a number of solutions of naftifin hydrochloride in different combinations and with different ratios of polyethylene glycols.Aim. The purpose of the work is to choose the optimal composition of the solution of naftifin hydrochloride. Achieve due to the viscosity of the prolonging action of the solution. Depending on the molecular weight of polyethylene glycol to determine the flow time of solutions. Choose among a number of samples with different ratios of polyethylene glycols, a solution with maximum viscosity.Materials and methods. To determine the viscosity of this solution, a capillary viscometry method was used on the vpzh-2 apparatus. «Exoderil» solution was chosen as a reference formulation.Results and discussion. Alternating different combinations of polyethylene glycol, we have increased the viscosity of the fluid naftifine hydrochloride, which has achieved a more accurate method of application of medicinal substances. During the study, it was determined that the solution «Exoderil» has a minimum viscosity, compared with all samples of the studied solutions.Сonclusion. The optimal viscosity of the solution of naftifin hydrochloride provides a prolonged action of the drug, due to a longer stay on the nail plate. Viscosity allows for more accurate application to the damaged nail, and reduces the loss of concentration of the active substance. Moisturizing properties of polyethylene glycols will help to reduce the severity of side effects (dryness, rarefaction), and provide a longer and more comfortable treatment of onychomycosis.

Microwave-Assisted Synthesis, Characterisation, and DNA-Binding Properties of RuII Complexes Coordinated by Norfloxacin as Potential Tumour Inhibitors

Three novel norfloxacin-based ruthenium(ii) complexes, [Ru(bpy)2(NFLX)]Cl·2H2O (1), [Ru(phen)2(NFLX)]Cl·2H2O (2), and [Ru(dmbpy)2(NFLX)]Cl·2H2O (3) (bpy=2,2′-bipyridine, phen=1,10-phenanthroline, dmbpy=4,4′-dimethyl-2,2′-bipyridine, and NFLX=norfloxacin), were synthesised and characterised with electrospray ionisation mass spectrometry and 1H and 13C NMR spectroscopy. The antitumour properties were evaluated by MTT assay, and the data revealed that 2 can inhibit the growth of human lung adenocarcinoma A549 efficiently. Furthermore, the DNA-binding behaviours of these complexes were investigated by a multiple spectroscopy assay and viscosity study. The results indicated that these complexes interact with calf thymus DNA through electrostatic interactions with a strong binding affinity in the order 2&gt;3&gt;1. Therefore, these results suggested that 2 might be a suitable anticancer agent due to its excellent DNA-binding abilities.