Haloperidol is a widely used neuroleptic drug for the treatment of acute and chronic psychosis. The use of haloperidol is limited by extrapyramidal movement disorders such as Parkinsonism, akathesia, dystonia, and tardive dyskinesia (TD). Treatment with haloperidol increases oxyradicals which are implicated in TD. Spirulina is widely used as nutritional supplement rich in proteins and antioxidants. The present study is proposed to study the effect of spirulina on haloperidol induced TD and oxidative stress by studying TD, various enzymatic and nonenzymatic antioxidants and lipid peroxidation. Haloperidol 1 mg/kg/i.p was used to induce vacuous chewing movements in rats. Spirulina maxima suspended in 1% between 80 at a dose of 45, 90 and 180 mg/kg were administered by gavage along with haloperidol from 21st day to 49th day of treatment. Spirulina supplementation at a dose of 180 mg/kg significantly improved enzymatic and nonenzymatic antioxidants and decreased the tardive dyskinesia induced by haloperidol. In conclusion, the results of present investigation suggest that spirulina decreases haloperidol induced oxidative stress and TD by many mechanisms as it is cocktail of antioxidants. On chronic use it may inhibit haloperidol induced reduced expression of DNA thereby increases the expression of enzymatic and nonenzymatic antioxidants and protects against oxidative stress induced neurodegeneration and TD.
Flutamide (FLT) is an antiandrogen drug for the treatment of prostate cancer. It has the drawback of poor water solubility and needs enhancement of its dissolution rate in simulated gastric fluids. Hence, it is prepared as self-nanoemulsifying drug delivery systems (SNEDDS) with an aim to enhance its dissolution rate. The objectives of the study are to develop SNEDDS of FLT and to characterize for particle size, self-nanoemulsification, and dissolution enhancement. Solubility of FLT was determined in various oils, surfactants, and cosurfactants. Sesame oil was selected as an oil phase, Tween 20 as surfactant, and PEG400 as cosurfactant due to their higher solubilization effect. Various formulations were prepared by simple mixing followed by vortexing. From studies, the optimized SNEDDS formulation was composed of FLT (8.04% w/w), sesame oil (24.12% w/w), Tween 20 (53.38% w/w), and PEG400 (14.46% w/w). The selected SNEDDS could be self-emulsified without precipitation upon simple mixing. The mean particle size of the SNEDDS was 148.7 nm and percent drug content was 99.66. The dissolution rate of FLT from SNEDDS was faster and higher in three different dissolution media such as 2% sodium lauryl sulfate (97.85%), simulated gastric fluid (0.1 N HCl containing 0.5% Tween 20) (95.71%), and simulated intestinal fluid (pH 6.8 buffer) (96.21%).
The objective of the present study was to formulate and evaluate an oral, time-controlled drug delivery system of Zafirlukast. Zafirlukast belongs to BCS class II drugs as it has poor aqueous solubility and good permeability. Hence an attempt has been made to improve its aqueous solubility by solid dispersion technique so that its dissolution, bioavailability, and therapeutic effect can be optimized. The optimized solid dispersion was then formulated into a chronotherapeutic drug delivery system by compression coating technology. FT-IR study revealed that there was no chemical interaction between the drug and polymers used. Tablets were prepared by direct compression method using different super disintegrants and then followed by compression coating using natural polymers. Pre-compression and post-compression parameters complied with the Pharmacopoeia limit for the tablets. In vitro release studies were performed and the results indicated the formulation Z9F9 to be the optimized formulation.
The main aim of the study was to enhance dissolution rate of Fluoxetine and Sertraline hydrochloride by formulating as solid dispersions using solvent evaporation method. Fluoxetine and Sertraline solid dispersions were prepared using PEG 4000 as polymer. PEGylated conjugates were prepared in the weight ratios of 1:0.5, 1:1, 1:2, 1:3, and 1:4 using solvent evaporation method. Physicochemical properties were evaluated using solubility studies, FTIR, powder XRD, SEM, dissolution studies. From solubility studies F5, S5 showed highest solubility. From FTIR studies it was proved that there was no interaction between drug and polymer. From SEM and powder XRD studies it was observed that change of polymorphic form of Fluoxetine and Sertraline from crystalline to amorphous form within the solid dispersion. From dissolution studies data it was observed that F5 and S5 showed maximum drug release within 45, 60min respectively, hence they were considered as optimized formulations. Based on the results, it can be concluded that developed solid dispersions was successful to enhance dissolution rate of both the drugs.
Introduction: Cefadroxil is the most widely used antibiotic for many bacterial infections but has the drawback of poorly solubility. In an attempt to provide an easier technique which can be scaled up on large scale to provide a simple method to enhance its aqueous solubility, this present work has exploited polyethylene glycol conjugation to enhance its aqueous solubility of cefadroxil. Objective: The main aim of the work is preparation of Polyethylene glycol conjugates of cefadroxil by solvent evaporation technique and to evaluate its solubility enhancement by solubility analysis and to assess drug content uniformity, drug - excipient interaction studies by FTIR spectroscopy. Methodology: Polyethylene glycol conjugates of cefadroxil are prepared by solvent evaporation technique using PEG 6000. Five conjugates of Cefadroxil to PEG6000 taken in weight proportions of (1:0.5), (1:1), (1:2) (1:3) and (1:4) were prepared. Results: Reasonable enhancement of solubility of cefadroxil was evidenced from all the prepared polyethylene glycol conjugates of cefadroxil. Among all CFDL: PEG 6000 (1:4) evidenced high percentage solubility of 81±0.61. IR spectrum of CFDL: PEG6000 (1:4) evidenced disappearance of amide group of cefadroxil indicating conjugate formation which is reversible to release cefadroxil to exhibit its therapeutic effect Conclusion: Polyethylene glycol conjugates of cefadroxil can be prepared easily by solvent evaporation and the conjugate made by weight proportion of CFDL: PEG 6000 (1:4) enhances solubility of cefadroxil by 88% and is promising to be used in formulations cefadroxil with enhanced dissolution and bioavailability.
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